Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.53617-36-0,1-Methyl-4-(piperidin-4-yl)piperazine,as a common compound, the synthetic route is as follows.,53617-36-0

1k) tert.-butyl 7-methyl-5-{(R)-3-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-3-oxo-2-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carbonyloxy]-propyl}-indazol-1-carboxylate A solution of 440 mg tert.-butyl 5-{(R)-2-carboxy-2-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carbonyloxy]-ethyl}-7-methyl-indazol-1-carboxylate, 256 mg (0.8 mmol) TBTU, 146 muL (1.0 mmol) triethylamine and 147 mg (0.8 mmol) 1-methyl-4-piperidin-4-yl-piperazine in 8 mL DMF was stirred for 2 h at RT. The reaction solution was filtered through an injection filter and purified directly by HPLC without any further working up. The fractions containing the product were combined, evaporated down i.vac., made alkaline with 15percent K2CO3 solution, extracted three times with 30 mL DCM, the combined organic phases were dried over Na2SO4 and the solvent was eliminated i. vac. Yield: 160 mg (28percent of theory) ESI-MS: (M+H)+=757 retention time (HPLC): 6.6 min (method A)

53617-36-0 1-Methyl-4-(piperidin-4-yl)piperazine 795707, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Boehringer Ingelheim International GmbH; US2005/256099; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

10338-57-5, 4-(Piperidin-1-yl)benzaldehyde is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A flame-dried sealed tube equipped with exo-cyclic enol ether (0.3mmol) and 18-crown-6 (23.8mg, 0.09mmol) was pumped to vacuum and exchanged with nitrogen for three times. Aldehyde (0.45mmol), solution of t-BuOK in THF (60muL) and DMF (1mL) were then added successively under nitrogen atmosphere. The mixture was stirred at 110C and the reaction was monitored by TLC. After completion of the reaction, the mixture was cooled and concentrated aqueous solution of NH4Cl was added to quench the reaction. The resulting mixture was extracted with CH2Cl2 and the organic phase was washed with concentrated brine and dried over Na2SO4. The solvent was evaporated under reduced pressure, and the residue was passed through column chromatography on silica gel to afford the desired product C.

10338-57-5, As the paragraph descriping shows that 10338-57-5 is playing an increasingly important role.

Reference：
Article; Shang, Xue Song; Li, Deng Yuan; Li, Nian Tai; Liu, Pei Nian; Dyes and Pigments; vol. 114; C; (2015); p. 8 – 17;,
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Piperidine | C5H11N – PubChem

85908-96-9,85908-96-9, N-Boc-2-Piperidone is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Substrate (0.5 mmol) was added to a reaction vial with CH2Cl2 (5 mL) and Cu(OTf)2 (9 mg, 0.025 mmol, 5 mol %). The reaction was allowed to stand at room temperature for 18 h before being quenched with H2O and extracted into CH2Cl2 (3×20 mL). The organic extracts were dried over MgSO4 and concentrated in vacuo.This yielded the pure product without need for further purification procedures: if pure product was not obtained the reaction was undertaken at 50C or 80C in a sealed J-Young tube.

The synthetic route of 85908-96-9 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Evans, Vikki; Mahon, Mary F.; Webster, Ruth L.; Tetrahedron; vol. 70; 41; (2014); p. 7593 – 7597;,
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Piperidine | C5H11N – PubChem

768-66-1, 2,2,6,6-Tetramethylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

768-66-1, To a stirred, cooled (0 C) solution of 2,2,6,6-tetramethylpiperidine(0.50 mL, 3.0 mmol) in THF (5 mL) was added BuLi(about 1.6 M hexanes solution, 3.0 mmol). After 15 min at 0 C,ZnCl2TMEDA (0.25 g, 1.0 mmol) was added, and the mixture wasstirred for 15 min at this temperature before introduction of thesubstrate (2.0 mmol). After 2 h at room temperature, a solutionof I2 (0.74 g, 3.0 mmol) in THF (5 mL) was added. The mixturewas stirred overnight before addition of an aqueous saturated solutionof Na2S2O3 (10 mL) and extraction with CH2Cl2 (3 20 mL).The combined organic layers were dried over Na2SO4 and concentratedunder reduced pressure before purification by flash chromatographyon silica gel.

The synthetic route of 768-66-1 has been constantly updated, and we look forward to future research findings.

Reference：
Article; Nagaradja, Elisabeth; Bentabed-Ababsa, Ghenia; Scalabrini, Mathieu; Chevallier, Floris; Philippot, Stephanie; Fontanay, Stephane; Duval, Raphael E.; Halauko, Yury S.; Ivashkevich, Oleg A.; Matulis, Vadim E.; Roisnel, Thierry; Mongin, Florence; Bioorganic and Medicinal Chemistry; vol. 23; 19; (2015); p. 6355 – 6363;,
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Piperidine | C5H11N – PubChem

53617-36-0, 1-Methyl-4-(piperidin-4-yl)piperazine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

53617-36-0, (Example 20) N-(3-Fluoro-4-{[2-({[2-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl}amino)pyridin-4-yl]oxy}phenyl)-N’-(4-fluorophenyl)clopropane-1,1-dicarboxamide To a solution of [4-(2-fluoro-4-{[1-(4-fluorophenylcarbamoyl)cyclopropanecarbonyl]amino}phenoxy)pyridin-2-yl]-N-(phenoxycarbonyl)carbamic acid phenyl ester (66 mg) in N,N-dimethylformamide (1.0 ml) was added 1-methyl-4-(piperidin-4-yl)piperazine (73.3 mg) at room temperature, followed by stirring overnight. The reaction mixture was partitioned between ethyl acetate and water. The organic layer was washed with a saturated aqueous solution of ammonium chloride and brine in this order, and dried over anhydrous sodium sulfate. The solvent was concentrated under reduced pressure. The resultant residue was purified by silica gel column chromatography (Fuji Silysia NH, eluent; ethyl acetate, then ethyl acetate:methanol = 95:5). Fractions containing the target compound were concentrated under reduced pressure. A solid was precipitated by addition of diethyl ether:heptane = 1:3 to the resultant residue. The solvent was removed under reduced pressure. The solid residue was dried under reduced pressure to provide the titled compound as white powder (60.1 mg, 95 percent). 1H-NMR Spectrum (CDCl3) delta (ppm): 1.40-2.00 (9H, m), 2.29 (3H, s), 2.35-2.70 (8H, m), 2.88 (2H, m), 4.00-4.10 (2H, m), 6.56 (1H, dd, J = 2.4, 5.6 Hz), 7.00-7.30 (5H, m), 7.40-7.50 (2H, m), 7.56 (1H, d, J = 2.4 Hz), 7.68 (1H, dd, J = 2.4, 12.0 Hz), 8.05 (1H, d, J = 5.6 Hz), 8.63 (1H, brs), 9.54 (1H, brs). ESI-MS (m/z): 656 [M+Na]+.

53617-36-0 1-Methyl-4-(piperidin-4-yl)piperazine 795707, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Eisai R&D Management Co., Ltd.; EP1889836; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.138377-80-7,3-Aminopiperidin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

To a solution of 3-aminopiperidin-2-one hydrochloride (1.50 g) in methanol (10 mL) was added AMBERLYST (registered trademark) A21 (750 mg) at room temperature. The reaction mixture was stirred at room temperature overnight, theinsoluble material was removed by filtration, and the filtrate was concentrated under reduced pressure. To a solution of the residue in ethanol (20 mL) was added 4-thioxothiazolidin-2-one (1.330 g) at room temperature. The reaction mixture wasstirred at room temperature overnight, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (NH, methanol/ethyl acetate) . To a solution of the residue and l-[2,4- bis (trifluoromethyl) benzyl] piperidine-4-carbaldehyde (1018 mg) in 2-propanol (10 mL) was added piperidinium acetate (436 mg) at room temperature. The reaction mixture was stirred at 60°C overnight, and the solvent was evaporated under reducedpressure. The residue was purified by silica gel columnchromatography (NH, methanol/ethyl acetate) and recrystallized from ethyl acetate/diisopropyl ether to give the titlecompound (530 mg) .? NMR (300 MHz, DMSO-d6) delta 1.38-1.59 (2H, m) , 1.68-1.91 (5H, m) , 2.01-2.27 (4H, m) , 2.69-2.84 (2H, m) , 3.17 (2H, brs) , 3.71 (2H, s), 4.43-4.55 (1H, m) , 6.89 (1H, d, J = 8.8 Hz), 7.83 (1H, brs), 7.98 (1H, s) , 8.02-8.12 (2H, m) , 9.34 (1H, brs).MS (ESI+) : [M+H]+ 535.1.

138377-80-7, 138377-80-7 3-Aminopiperidin-2-one hydrochloride 19795138, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; MATSUMOTO, Shigemitsu; ONO, Koji; TOMINARI, Yusuke; KATOH, Taisuke; MIWA, Kazuhiro; HASUOKA, Atsushi; IMAMURA, Shinichi; WO2013/18929; (2013); A1;,
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Piperidine | C5H11N – PubChem

89895-06-7, 1-(Piperidin-4-yl)ethanone hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,89895-06-7

0224] 1-(Piperidin-4-yl)ethanone hydrochloride(6.07 g, 21.85 mmol) obtained in Preparation Example 6-4 was dissolvedin acetonitrile (75 mL). Potassium carbonate (K2CO3) (5.83 g, 34.96 mmol) and iodoethane (CH3CH2I) (2.77 mL,28.41 mmol) were added dropwise to the resulting solution and the solution was stirred for 18 hrs. The solution wasevaporated under reduced pressure to concentrate, diluted with EtOAc, and washed with water. The washed organicsolvent was dried over anhydrous magnesium sulfate (MgSO4) to concentrate. The resulting residue was isolated andpurified by silica gel column chromatography (dimethylchloride/methanol = 10/1) to give the white title compound (5.18g, 76 %).1H NMR (400 MHz, CDCl3) delta 2.81 (m, 2H), 2.24 (s, 3H), 2.16 (m, 1H), 2.09 (m, 2H), 1.94 (m, 2H), 1.80 (m, 2H), 1.60(m, 2H), 1.48 (m, 3H).

89895-06-7 1-(Piperidin-4-yl)ethanone hydrochloride 44151897, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Beyondbio Inc.; MIN, Changhee; OH, Byungkyu; KIM, Yongeun; PARK, Changmin; (98 pag.)EP3255042; (2017); A2;,
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Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4629-78-1,3-Methylpiperidin-4-one hydrochloride,as a common compound, the synthetic route is as follows.

Preparation of acyl-chloride: A solution of 200 mg (0.571 mmol) of the compound from Example 52A in 4 mL of dichloromethane was initially treated at RT with 249 mu (2.86 mmol) of oxalyl chloride and then with a small drop of DMF.After the reaction mixture had been stirred at RT for 2.5 h, it was concentrated to dryness on a rotary evaporator.The remaining residue was dried under high vacuum and then reacted further in the next substep. Preparation of the amide: The acid chloride obtained above was dissolved in 1 ml of dichloromethane and added to a solution of 171 mg (1.14 mmol) of 3-methylpiperidine-4-one hydrochloride and 398 mu (2.28 mmol) N, N-diisopropylethylamine in 5 ml of dichloromethane dropped.The reaction mixture was stirred at RT for 2 h.After the mixture was concentrated on a rotary evaporator to dryness, the crude product (method 6) was purified by preparative HPLC.After combining the product fractions, evaporation and drying under high vacuum, 236 mg (88% d. Th., 95% purity) of the title compound.

4629-78-1, 4629-78-1 3-Methylpiperidin-4-one hydrochloride 22728864, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; HAERTER, MICHAEL; DELBECK, MARTINA; KALTHOF, BERND; LUSTIG, KLEMENS; LINDNER, NIELS; KAST, RAIMUND; WASNAIRE, PIERRE; SUESSMEIER, FRANK; (372 pag.)TW2016/7950; (2016); A;,
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Piperidine | C5H11N – PubChem

3518-83-0, N-Ethyl-4-hydroxypiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 4-hydroxy-N-ethylpiperidine (267mg, 2.0 mmol) inTHF (5.0 mE) at RT was added NaH(60%w/w, 91 mg, 2.3 mmol) with stirring. The reaction mixturewas stirred at RT under nitrogen for 45 minutes. To the reac-tion mixture was then added 3-(4-chloro-6-methyl-2-pyrim-idinyl)-i-(3,4-dichlorophenyl)guanidine (4) (166 mg, 0.5mmol). The reaction mixture was stirred at RT for 5 hours and then heated to 90 C. for 18 hrs. The reaction mixture was cooled, poured into ice-water mixture and extracted with CH2C12 (2×25 mE). The CH2C12 layerwas washedwith waterand dried (Na2504), filtered and concentrated in vacuo toyield crude compound (200 mg, 94.8%). The crude com-pound was purified by column chromatography several times(silica, eluent, mixture ofCH2C12:MeOH:NH4OH in the ratio400: 50:2 respectively) to obtain the title compound (25) (20mg, 9%) as a solid. HPEC (254 nm): Method 3, Rt 2.89 miMS (ESI) mlz 425.3 [M+H].

3518-83-0, 3518-83-0 N-Ethyl-4-hydroxypiperidine 77056, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Curtana Pharmaceuticals, Inc.; BEATON, Graham; TUCCI, Fabio; RAVULA, Satheesh B.; WANG, Hua-Yu; (104 pag.)US2016/237069; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.138377-80-7,3-Aminopiperidin-2-one hydrochloride,as a common compound, the synthetic route is as follows.

Example 10 ; 3-[({4-[(3-chloro-2-fluorophenyl) amino]-7-methoxyquinazolin-6- yl} methyl) amino] piperidin-2-one; (Process (a)); 4- [ (3-Chloro-2-fluorophenyl) amino]-7-methoxyquinazoline-6-carbaldehyde was coupled with 3-amino-piperidin-2-one (prepared by converting 3-amino-piperidin-2-one hydrochloride to the free-base form) using an analogous method to that described for the equivalent step in Example 1 to give the title compound ; 1H NMR spectrum : (DMSO d6) 1. 5= (m, 1H), 1.68 (m, 1H), 1.84 (m, 1H), 2.16 (m, 1H), 2.73 (brs, 1H), 3.05 (dd, 1H), 3.13 (m, 2H), 3.84 (d, 1H), 3.93 (d, 1H), 3.98 (s, 3H), 7.21 (s, 1H), 7.28 (t, 1H), 7.48 (t, 1H), 7.53 (m, 2H), 8.35 (s, 1H), 8.44 (s, 1H), 9.80 (s, 1H); Mass Spectrum : (M+H) +430., 138377-80-7

The synthetic route of 138377-80-7 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/75439; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem