Heterocyclic Building Blocks-piperidine

Lin, Kingson published the artcileHaloselective Cross-Coupling via Ni/Photoredox Dual Catalysis, Application In Synthesis of 219543-09-6, the publication is ACS Catalysis (2017), 7(8), 5129-5133, database is CAplus and MEDLINE.

The chemoselective functionalization of polyfunctional aryl linchpins is crucial for rapid diversification. Although well-explored for C_sp² and C_sp nucleophiles, the chemoselective introduction of C_sp³ groups remains notoriously difficult and is virtually undocumented using Ni catalysts. To fill this methodol. gap, a “haloselective” cross-coupling process of arenes bearing two halogens, I and Br, using ammonium alkylbis(catecholato)silicates, has been developed. Utilizing Ni/photoredox dual catalysis, C_sp³-C_sp² bonds can be forged selectively at the iodine-bearing carbon of bromo(iodo)arenes. The described high-yielding, base-free strategy accommodates various protic functional groups. Selective electrophile activation enables installation of a second C_sp³ center and can be done without the need for purification of the intermediate monoalkylated product.

ACS Catalysis published new progress about 219543-09-6. 219543-09-6 belongs to piperidines, auxiliary class Piperidine,Fluoride,Salt,Amine,Amide, name is 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, and the molecular formula is C11H21BF4N2O2, Application In Synthesis of 219543-09-6.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Lien, Evan C. published the artcileLow glycaemic diets alter lipid metabolism to influence tumour growth, Recommanded Product: 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide, the publication is Nature (London, United Kingdom) (2021), 599(7884), 302-307, database is CAplus and MEDLINE.

Dietary interventions can change metabolite levels in the tumor microenvironment, which might then affect cancer cell metabolism to alter tumor growth1-5. Although caloric restriction (CR) and a ketogenic diet (KD) are often thought to limit tumor progression by lowering blood glucose and insulin levels6-8, we found that only CR inhibits the growth of select tumor allografts in mice, suggesting that other mechanisms contribute to tumor growth inhibition. A change in nutrient availability observed with CR, but not with KD, is lower lipid levels in the plasma and tumors. Upregulation of stearoyl-CoA desaturase (SCD), which synthesizes monounsaturated fatty acids, is required for cancer cells to proliferate in a lipid-depleted environment, and CR also impairs tumor SCD activity to cause an imbalance between unsaturated and saturated fatty acids to slow tumor growth. Enforcing cancer cell SCD expression or raising circulating lipid levels through a higher-fat CR diet confers resistance to the effects of CR. By contrast, although KD also impairs tumor SCD activity, KD-driven increases in lipid availability maintain the unsaturated to saturated fatty acid ratios in tumors, and changing the KD fat composition to increase tumor saturated fatty acid levels cooperates with decreased tumor SCD activity to slow tumor growth. These data suggest that diet-induced mismatches between tumor fatty acid desaturation activity and the availability of specific fatty acid species determine whether low glycemic diets impair tumor growth.

Nature (London, United Kingdom) published new progress about 1032229-33-6. 1032229-33-6 belongs to piperidines, auxiliary class Metabolic Enzyme,SCD, name is 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide, and the molecular formula is C20H22ClN3O3, Recommanded Product: 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Gardner, T. S. published the artcileSynthesis of compounds for chemotherapy of tuberculosis. VII. Pyridine N-oxides with sulfur-containing groups, Application of Piperidine-4-carbothioamide, the publication is Journal of Organic Chemistry (1957), 984-6, database is CAplus.

cf. C.A. 51, 3610b. A number of C₅H₅N derivatives containing a CSNH moiety were prepared Isonicotinamide 1-oxide (Ia) (147 g.) refluxed 0.5 h. with 1.5 kg. POCl₃, the solution concentrated, poured on ice, and made alk., and the separated nitrile collected, the solution was extracted 5 times with CHCl₃, the solids also extracted with CHCl₃, and the combined extracts yielded 85 g. isonicotinonitrile 1-oxide (I), m. 229-30°. I (30 g.) in 300 mL. MeOH containing 30% NH₃ by weight and the solution left 2 days saturated with H₂S gave 12 g. thioisonicotinamide 1-oxide, m. 205-6° (H₂O). Thioisonicotinamide-HCl, orange colored solid, m. 231-2°(alc.). Nicotinonitrile 1-oxide (II) was obtained in 55% yield from nicotinamide 1-oxide by refluxing 0.5 h. with POCl₃. II (28 g.) in 300 mL. MeOH containing 20% NH₃ left 18 h. with H₂S gave 14 g. thionicotinamide 1-oxide, m. 161-4° (H₂O). Picolinamide (70 g.) heated 6 h. at 80° in a solution of 100 g. 40% AcO₂H and 300 mL. AcOH gave 51 g. picolinamide 1-oxide (III), m. 165-6° (MeOH). The investigation of the picolino-type N-oxide gave several anomalies. Thus P₂S₅ and K₂S in C₅H₅N with III deoxygenated the N-oxide and gave only thiopicolinamide. A mixture of 70 g. diatomaceous earth and 150 g. P₂O₅ refluxed 4 h. with 25 g. III in 500 mL. PhMe, the gummy mixture filtered on a dry Hyflo bed, the residue treated with H₂O and concentrated NH₄OH and extracted with CHCl₃, and the combined PhMe and CHCl₃ solutions concentrated gave 5 g. picolinonitrile 1-oxide, m. 122-3° (Et₂O). The reaction of refluxing POCl₃ on III rapidly deoxygenated the compound to give 2-picolinonitrile. In contrast, more than 6 h. refluxing POCl₃ was required to deoxygenate Ia to give isonicotinonitrile. 4-Aminopyridine 1-oxide-HCl (20 g.) refluxed 6 h. with 12.5 g. NH₄SCN in 250 mL. alc. gave 20 g. 4-pyridylthiourea 1-oxide, m. 126-7° (Me₂CO). 3-Bromopyridine 1-oxide-HCl (53.5 g.) in 100 mL. H₂O neutralized with dilute NaOH and extracted with CHCl₃ gave the free 3-bromopyridine 1-oxide which when refluxed 5 h. in 300 mL. alc. with 19 g. CS(NH₂)₂ gave 50 g. 2-(3′-pyridyl)-2-thiopseudourea 1′-oxide-HBr (IV), m. 145-7° (alc.). IV could not be decomposed to give 3-pyridinethiol 1-oxide using NaOH solution N-Ethylnicotinamide (60 g.) treated at 10-15° with 120 g. 40% AcO₂H in AcOH and concentrated at 80° gave 35 g. N-ethylnicotinamide 1-oxide, m. 123-4°. 3,5-Dibromopyridine (42 g.), 80 g. 40% AcO₂H in AcOH, and 300 mL. AcOH heated 3 h. at 80° and then 12 h. at 50° gave 30 g. 3,5-dibromopyridine 1-oxide (V), m. 143-4° (alc.). V (20 g.) refluxed 5 h. in 300 mL. alc. and 15 g. CS(NH₂)₂ gave 20 g. 2-(5′-bromo-3′-pyridyl)-2-thiopseudourea 1′-oxide-HBr, m. 162-3° (alc.). Thioisonicotinamide (Va) (25 g.) in 1 l. H₂O treated with 30 mL. 37% HCHO, the pH adjusted to 7.5 by KOH solution, the mixture left 6 h., and the pH adjusted to 7 by HCO₂H, and the mixture cooled to 4° gave 24 g. N,N’-methylenebis(thioisonicotinamide)-H₂O (VI), m. 146-7° (H₂O). VI was less active than the parent compound in tuberculosis in mice. The assignment of the linear structure was based on analyses and the fact that IR analyses gave none of the characteristic absorption bands for the triazine structure. Isonipecotamide (100 g.) in 450 g. POCl₃ refluxed 2 h. and concentrated in vacuo and poured on ice gave 37 g. 4-cyanopiperidine (VII), b₇ 100°, n²³_D 1.4741. VII (35 g.) left 48 h. at 25° in 300 mL. 30% NH₃ saturated with H₂S gave 30 g. thioisonipecotamide (VIII), m. 173-4° (H₂O). Attempts to convert the isonipecotamide to VIII using P₂S₅ failed with or without K₂S and only Va was obtained in 25-40% yields. Va (50 g.) and 56 g. α-bromopropionic acid heated 6 h. in PhMe gave 25 g. 5-methyl-2-(4-pyridyl)-4(5H)-thiazolone-HBr, m. above 250° (alc.). Va (50 g.) refluxed in 250 mL. AcCH₂Cl gave 11.5 g. 4-methyl-2-(4-pyridyl)thiazole-HCl, m. 219-20° (decomposition) (MeOH). Reduction of the C₅H₅N ring eliminated activity; N-oxidation reduced activity, and separation from the ring of the CSNH group eliminated activity as did also the conversion of the group into a ring system.

Journal of Organic Chemistry published new progress about 112401-09-9. 112401-09-9 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carbothioamide, and the molecular formula is C6H12N2S, Application of Piperidine-4-carbothioamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Shapiro, Seymour L. published the artcile3-Oxypiperidine derivatives, Formula: C7H15NO, the publication is Journal of the American Chemical Society (1959), 5146-9, database is CAplus.

cf. preceding abstract. The 3-oxypyridyl betaines and bis(3-oxypyridyl) betaines described in the preceding abstract hydrogenated over Rh-C yield the corresponding N-substituted-3-hydroxypiperidines and N,N’-bis(3-hydroxypiperidines), resp. These compounds, their ethers, and quaternary salts were examined for pharmacol. activity. N-(p-Chlorobenzyl)-3-oxypyridyl betaine-HCl (38.4 g.) in 250 cc. MeOH hydrogenated, 4 hrs. at 20° and 50 lb. initial pressure over 2 g. Rh-C, filtered, diluted with 300 cc. Et₂O, and the precipitate filtered off, the filtrate concentrated to 125 cc. and diluted with 260 cc. Et₂O, the precipitate filtered off, and the combined product (32.5 g.) recrystallized from MeOH-EtOAc yielded N-(p-chlorobenzyl)-3-hydroxypiperidine-HCl, m. 210-12°. Similarly were prepared the following compounds (m.p., % yield, and reduction time in hrs. given): 1-ethyl-3-hydroxypiperidine-HBr, 144-6° (EtOAc-Et₂O), 81, 1.75 [picrate, m. 81-3° (EtOAc-Et₂O)]; 1-benzyl-3-hydroxypiperidine-HCl, 167-70° (EtOH-EtOAc), 53, 4.5; 1-(2-dimethylaminoethyl)-3-hydroxypiperidine-2HCl, 267 8° (MeOH), 60, 1.5; 1-(3-dimethylaminopropyl)-3-hydroxypiperidine-2HCl (I), 222-6° (MeOH-EtOAc), 48. N-(5-Cyanopentyl)-3-oxypyridylbetaine-HCl (10.9 g.) in 200 cc. MeOH hydrogenated 9 hrs. over 2 g. Rh-C and filtered, the residue washed with 150 cc. H₂O, the MeOH removed from the combined filtrates, the aqueous residue basified with 6N NaOH, and the product isolated with CHCl₃ yielded 24% N-(6-aminohexyl)-3-hydroxypiperidine, b_0.08 110-12°, and 12% bis-[6-(3-hydroxypiperidino)hexyl]amine, b_0.2220-30°. 1-Phenacyl-3-oxypyridylbetaine-HCl(II)(40.8 g.) in 250 cc. MeOH hydrogenated over 2 g. Rh-C and worked up in the usual manner gave 5.0 g. distillate, b_0.09 90-5°, which deposited 0.4 g. 1-(2-phenethyl)-3-hydroxy-piperidine, m. 66-8° (hexane), and 22 g. 1-(2-hydroxy-2-phenylethyl)-3-hydroxypiperidine, b_0.05 140-50°. The p-Br derivative of II hydrogenated in the usual manner 16 hrs. yielded 8% 1-[2-(p-bromophenyl)-2-hydroxyethyl]-3-hydroxypiperidine (III), b_0.2 125-40°. The p-Cl derivative of II yielded similarly 6% p-Cl analog of III, m. 104-6° (heptane), and the p-Ph derivative of II gave 18% p-Ph (IIIa) analog of III, b_0.05 196-206°. The appropriate betaine hydrohalide (0.1 mole) in 250 cc. MeOH hydrogenated over 2 g. Rh-C gave the corresponding bis(3-hydroxypiperidino)alkane (m.p. or b.p./mm., % yield, and hydrogenation time in hrs. given): 1,3-bis(3-hydroxypiperidino)propane (IV), 146-51°/0.07, 50, 4, [dimethiodide m. 245-7° (EtOH)]; 1,4-butane analog (V) of IV, 108-10° (heptane), 60, 1, [V.2HCl, m. 263-5° (MeOH-EtOAc), 56%; V.2HBr, m. 261-5° (MeOH-EtOAc), 40%; V.2MeI, m. 235-7° (MeOH-EtOAc), 48%]; 1,5-pentane analog (VI) of IV, 176-80°/0.3, -, 6, (VI.2HBr, m. 173-5° (EtOH-EtOAc), 61%; VI.2MeI, m. 257-8° (EtOH), 73%); 1,6-hexane analog (VII) of IV, 91-3° (hexane), -, 5, [VII.2HBr, m. 219-21° (MeOH-EtOAc), 82%; VII.2MeI, m. 182-4° (EtOH), 71]; 1,4(1,4-dimethylbutane) analog, 162-8°/0.05, 59, 1.5; 1,10decane analog (VIII) of IV, 79-81° (pentane), -, 2, [VIII.-2HBr, 189-93° (MeOH-EtOAc), 33%; VIII.2MeI, m. 16575°]; p-CH₂C₆H₄CH₂ analog (IX) of IV, 140-3° (heptane), -, 7, [IX.2HCl, 309-10° (aqueous EtOH), 35%]. IV (3.9 g.) in 20 cc. C₅H₅N treated dropwise with stirring with 7.4 g. iso-PrCOCl during 0.5 hr., kept 20 hrs., and filtered, the residue dissolved in 15 cc. H₂O and 60 cc. Et₂O, the mixture adjusted to pH 8 with N NaOH and shaken, the aqueous phase extracted with 50 cc. Et₂O, and the combined Et₂O solutions worked up yielded 3.06 g. 1,3-bis(3-isobutyroxypiperidino)propane (X), b_0.03 156-8°. X (1.2 g.) in 8 cc. MeCN treated with 5 cc. p-MeC₆H₄SO₃Me, kept 10 days, and filtered yielded 0.2 g. X.2p-MeC₆H₄SO₃Me, m. 216-18° (MeOH). IV (10.5 g.) in 90 cc. PhMe treated at 50° with 2.54 g. NaH, refluxed 2 hrs. with stirring, the free base from 20.9 g. Me₂N-(CH₂)₂Cl.HCl in PhMe added, the mixture refluxed 20 hrs., cooled, and centrifuged, the supernatant decanted and evaporated, and the residue distilled yielded 7.86 g. 1,3-bis[3-(2-dimethylaminoethoxy)piperidino] propane, b_0.155 160-5°. VI.HBr (4.7 g.) in 49 cc. Ac₂O kept 6 days at 20°, the excess Ac₂O removed, the residue dissolved in 30 cc. Et₂O, the solution diluted with 15 cc. H₂O, adjusted with shaking with N NaOH to pH 8, the aqueous layer extracted with 25 cc. Et₂O, and the combined Et₂O solutions worked up yielded 1,5-bis(3-acetoxypiperidino)pentane (XI), b_0.05 158-64°. XI (177 mg.) in 5 cc. hexane treated with 1 cc. of a solution of 1.2 g. MeI in 10 cc. hexane, kept 4 days in the dark, and centrifuged, and the precipitate triturated with hexane gave XI.2MeI, hygroscopic, m. 108-13°. VIII (7.6 g.) in 100 cc. PhMe treated at 50° with 1.2 g. NaH, refluxed 2 hrs. with stirring, cooled, treated with 7.2 g. EtI, refluxed 3 hrs. with stirring, filtered, and distilled yielded 44% 1,10-bis(3-ethoxypiperidino)decane (XII), b_0.2 180-8°. N,N’-Tetramethylenebis(3oxypyridyl) betaine-2HCl (15.85 g.) in 250 cc. EtOH hydrogenated 9 hrs. over 0.5 g. PtO₂ and worked up in the usual manner yielded 4.5 g. 1,4-bis(piperidino)butane, b_0.05 114-20°, m. 107-10°; dipicrate, m. 189-90° (H₂O). N,N'(1,4-Buta-2-enylene)bis(3-oxypyridyl)betaine-2HBr hydrogenated 27 hrs. in the usual manner over PtO₂ and worked up gave 27 g. V, m. 108-12° (heptane). By the general procedures were prepared the following compounds XIII (R, Y, m.p./or b.p./mm., and % yield given): Ac, (CH₂)₃, 138-40°/0.05, 45; EtCO, (CH₂)₃ (XIV), 146-51°/0.03, 48; PrCO, (CH₂)₃, 156-62°/0.05, 57; Et, (CH₂)₃, 124°/0.02, 23; Ac, (CH₂)₄, 150-2°/0.02, 49; EtCO, (CH₂)₄ di-HCl salt, 270-5° (EtOH-hexane), 37; PrCO, (CH₂)₄, 170-4°/0.02, 58; iso-PrCO, (CH₂)₄, 156-62°/0.02, 34; Et, (CH₂)₄ (XV), 139-46°/0.1, 35; Me₂N(CH₂)₂, (CH₂)₄ (XVI), 148-65°/0.03, 21 [XVI.4MeI, m. 158-60° (EtOAc), 42%]; EtCO, (CH₂)₅ (XVII), 168-72°/0.04, 60; PrCO, (CH₂)₅ (XVIII), 177-84°/0.03, 550 iso-PrCO, (CH₂)₅, 178-88°/0.04, 50; Et, (CH₂)₅ (XIX), 140-50°/0.01, 34; Me₂N(CH₂)₂, (CH₂)₅, 168-75°/0.1, 34 [tetramethiodide, m. 250-4° (aqueous EtOH), 34%]; Ac, (CH₂)₆, 67-9° (aqueous Me₂CO), 8; EtCO, (CH₂)₆, 176-82°/0.03, 53; PrCO, 188-90°/0.03, 56; iso-PrCO, 180-5°/0.02, 88; p-O₂NC₆H₄CO, (CH₂)₆ dipicrate, 224-5° (BuOH), -; Et, (CH₂)₆ (XX), 150-8°/0.08, 29; Me₂NCH₂CH₂, (CH₂)₆ (XXI), 186-90°/0.16, 16 [XII.4MeI, m. 258-61° (MeOH-EtOAc), 20%]; Ac, CHMe(CH₂)₂CHMe (XXII), 158-62°/0.03, 81; Ac, (CH₂)₁₀, 76-8° (aqueous MeOH), 24; EtCO, (CH₂)₁₀ (XXIII), 196-204°/0.03, 64; PrCO, (CH₂)₁₀ (XXIV), 208-10°/0.08, 28 [XXIV.2p-MeC₆H₄SO₃Me, m. 125-7° (BuOH), 6%]; iso-PrCO, (CH₂)₁₀ (XXV), 198-208°/0.02, 34. Potentiated adrenaline activity was shown by I, IIIa, XIV, V.2HCl, XV, VI.2HBr, VI.2MeI, VII.2MeI, VIII.2HBr, moderate ganglionic blocking action by XVIII, partial block by IIIa, V.HCl, and XVI, adrenergic blocking effect by XXI and VIII.2HBr, and slight, lasting hypotensive effect by IIIa, V.HCl, XVI, and XIX. IIIa, LD_min. 750 mg./kg. subcutaneously, at 20 mg./kg. reduced the motor activity of rats 43%. XXI.4MeI showed depression of motor activity. Antiinflammatory activity of 17 units/g. was obtained with XII; XX, XXII, VI.2HBr, IV.2MeI, XV, XI, XVII, XIX showed lesser effectiveness. Curare-like effects (about 10% of the activity of decamethonium) were noted with XXI, XXIII, XXIV, XXV, and XII.

Journal of the American Chemical Society published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C25H23NO4, Formula: C7H15NO.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Lei, Hanqi published the artcileCRISPR screening identifies CDK12 as a conservative vulnerability of prostate cancer, HPLC of Formula: 1702809-17-3, the publication is Cell Death & Disease (2021), 12(8), 740, database is CAplus and MEDLINE.

Androgen receptor (AR) signaling inhibitors provide limited survival benefits to patients with prostate cancer (PCa), and worse, few feasible genomic lesions restrict targeted treatment to PCa. Thus, a better understanding of the critical dependencies of PCa may enable more feasible therapeutic approaches to the dilemma. We performed a kinome-scale CRISPR/Cas9 screen and identified cyclin-dependent kinase 12 (CDK12) as being conservatively required for PCa cell survival. Suppression of CDK12 by the covalent inhibitor THZ531 led to an obvious anti-PCa effect. Mechanistically, THZ531 downregulated AR signaling and preferentially repressed a distinct class of CDK12 inhibition-sensitive transcripts (CDK12-ISTs), including prostate lineage-specific genes, and contributed to cellular survival processes. Integration of the super-enhancer (SE) landscape and CDK12-ISTs indicated a group of potential PCa oncogenes, further conferring the sensitivity of PCa cells to CDK12 inhibition. Importantly, THZ531 strikingly synergized with multiple AR antagonists. The synergistic effect may be driven by attenuated H3K27ac signaling on AR targets and an intensive SE-associated apoptosis pathway. In conclusion, we highlight the validity of CDK12 as a druggable target in PCa. The synergy of THZ531 and AR antagonists suggests a potential combination therapy for PCa.

Cell Death & Disease published new progress about 1702809-17-3. 1702809-17-3 belongs to piperidines, auxiliary class Cell Cycle,CDK, name is (R,E)-N-(4-(3-((5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide, and the molecular formula is C30H32ClN7O2, HPLC of Formula: 1702809-17-3.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Yi, Hailing published the artcileUltrasonic treatment enhances the formation of oxygen vacancies and trivalent manganese on α-MnO₂ surfaces: Mechanism and application, Synthetic Route of 826-36-8, the publication is Journal of Colloid and Interface Science (2022), 629-638, database is CAplus and MEDLINE.

Catalytic activity is the main obstacle limiting the application of peroxymonosulfate (PMS) activation on transition metal oxide catalysts in organic pollutant removal. Herein, ultrasonic treatment was applied to α-MnO₂ to fabricate a new u-α-MnO₂ catalyst for PMS activation. Di-Me phthalate (DMP, 10 mg/L) was almost completely degraded within 90 min, and the pseudofirst-order rate constant for DMP degradation in the u-α-MnO₂/PMS system was âˆ? times that in the initial α-MnO₂/PMS system. The ultrasonic treatment altered the crystalline and pore structures of α-MnO₂ and produced defects on the u-α-MnO₂ catalyst. According to the XPS, TG, and EPR results, higher contents of trivalent Mn and oxygen vacancies (OVs) were produced on the catalyst surfaces. The OVs induced the decomposition of PMS to produce ¹O₂, which was identified as the main reactive oxygen species (ROS) responsible for DMP degradation The u-α-MnO₂ catalyst presented great reusability, especially by ultrasonic regeneration of OVs toward the used catalyst. This study provides new insights into regulating OVs generation and strengthening catalyst activity in the PMS activation process for its application in water purification

Journal of Colloid and Interface Science published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C6H12N2O, Synthetic Route of 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Dong, Yuxiang published the artcileStructure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439), Quality Control of 39546-32-2, the publication is Journal of Medicinal Chemistry (2017), 60(7), 2654-2668, database is CAplus and MEDLINE.

Building on insights gained from the discovery of the antimalarial ozonide arterolane (OZ277), we now describe the structure-activity relationship (SAR) of the antimalarial ozonide artefenomel (OZ439). Primary and secondary amino ozonides had higher metabolic stabilities than tertiary amino ozonides, consistent with their higher pK_a and lower log D_7.4 values. For primary amino ozonides, addition of polar functional groups decreased in vivo antimalarial efficacy. For secondary amino ozonides, addnl. functional groups had variable effects on metabolic stability and efficacy, but the most effective members of this series also had the highest log D_7.4 values. For tertiary amino ozonides, addition of polar functional groups with H-bond donors increased metabolic stability but decreased in vivo antimalarial efficacy. Primary and tertiary amino ozonides with cycloalkyl and heterocycle substructures were superior to their acyclic counterparts. The high curative efficacy of these ozonides was most often associated with high and prolonged plasma exposure, but exposure on its own did not explain the presence or absence of either curative efficacy or in vivo toxicity.

Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Quality Control of 39546-32-2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Huang, Zhiyan published the artcileCoagulation treatment of swine wastewater by the method of in-situ forming layered double hydroxides and sludge recycling for preparation of biochar composite catalyst, COA of Formula: C9H17NO, the publication is Chemical Engineering Journal (Amsterdam, Netherlands) (2019), 784-792, database is CAplus.

In order to achieve enhanced treatment of swine wastewater as well as resource recycle, in this work, we applied coagulation treatment on swine wastewater by adding Fe and Mg ions, MgFe layered double hydroxides (LDHs) was yielded during coagulation process and the coagulation sludge was recycled to prepare biochar composite catalyst. The removal rates of total phosphorus (TP) and COD (COD) by Mg-Fe coagulation could achieve 82.55% and 98.51%, which is higher than that by coagulation with individual Mg²⁺ or individual Fe³⁺. Finely dispersed MgFe-LDHs flocculation was formed during the coagulation process and was embedded within zoogloea, suspended particles, organic matters, etc. The obtained coagulation sludge was recycled to prepare biochar composite catalyst by oxygen-limited pyrolysis. Redox reaction of iron compounds and electron shuttles capacity of biochar in the catalyst could activate potassium peroxymonosulfate (PMS) to generate ·OH, ·OOH and ¹O₂, which was responsible for catalysis potential. The as-prepared biochar composite catalyst showed satisfactory catalytic degradation capacity on tylosin and rhodamine B (pH value varied from 3 to 10), and the maximum degradation rate achieved 92.2% for tylosin and 81.9% for rhodamine B (RhB). Coagulation treatment of swine wastewater and in-situ formed layered double hydroxides recycling was suitable in wastewater treatment and resource recycling, of which the degradation rates of RhB were above 83% after five cycling experiments In general, the combined process exhibits great potential for the deep treatment of swine wastewater and resource recycling for sludge.

Chemical Engineering Journal (Amsterdam, Netherlands) published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, COA of Formula: C9H17NO.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Wu, Chun-Feng published the artcileSynthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer, HPLC of Formula: 39546-32-2, the publication is European Journal of Medicinal Chemistry (2022), 114055, database is CAplus and MEDLINE.

The development of inhibitors targeting the PI3K-Akt-mTOR signaling pathway has been greatly hindered by the on-target AEs, such as hyperglycemia and hepatotoxicities. In this study, a series of diaryl urea derivatives has been designed and synthesized based on clin. candidate gedatolisib, and most of the newly synthesized derivatives showed kinase inhibitory and antiproliferative activities within nanomolar and submicromolar level, resp. The terminal L-proline amide substituted derivative I showed 8.6-fold more potent PI3Kα inhibitory activity (0.7 nM) and 4.6-fold more potent antiproliferative effect against HCT116 cell lines (0.11μM) compared with control gedatolisib. The potential antitumor mechanism and efficacy of I in HCT116 xenograft models have also been evaluated, and found I showed comparable in vivo antitumor activity with gedatolisib. The safety investigations revealed that compound I exhibited more safer profiles in the selectivity of liver cells (selectivity index: >6.6 vs 1.85) and blood glucose regulation than gedatolisib. In addition, the in vitro stability assays also indicated that developed compound I possessed good metabolic stabilities.

European Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C9H9BO2, HPLC of Formula: 39546-32-2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Long, Jiao published the artcileNickel/Bronsted Acid-Catalyzed Chemo- and Enantioselective Intermolecular Hydroamination of Conjugated Dienes, Safety of Piperidine-4-carboxamide, the publication is iScience (2019), 369-379, database is CAplus and MEDLINE.

A novel nickel/Bronsted acid-catalyzed asym. hydroamination of acyclic 1,3-dienes was established. A wide array of primary and secondary amines were transformed into allylic amines with high yields and high enantioselectivities under very mild conditions. Moreover, this method was compatible with various functional groups and heterocycles, allowing for late-stage functionalization of biol. active complex mols. Remarkably, this protocol exhibited good chemoselectivity with respect to amines bearing two different nucleophilic sites. Mechanistic studies revealed that the enantioselective carbon-nitrogen bond-forming step was reversible.

iScience published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Safety of Piperidine-4-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem