Tag: M.W:200-300

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.159635-22-0,tert-Butyl 3-hydroxy-4-methylenepiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Method DStep 1: (S)-3-hydroxy-4-methylene-piperidine-1-carboxylic Acid tert-butyl ester; 3-Hydroxy-4-methylene-piperidine-1-carboxylic acid tert-butyl ester (4.50 g; 21.10 mmol) was dissolved in TBME (63 ml) and vinyl butyrate (22.5 ml). The solution was heated to 50 C. and the reaction started by the addition of Lipase TL IM (1.08 g (carrier-fixed); Novozymes, Denmark). The solution was stirred at 50 C. for 20 h until the enantiomeric excess of the retained alcohol was >99%. The enzyme was filtered off, the filter cake washed with TBME and the filtrate concentrated in vacuo. The residual oil was chromatographed on silicagel (100 g; 0.040-0.063 mm; CH2Cl2?CH2Cl2/acetone 9:1) to separate the formed optically enriched (R)-butyrate from the retained (S)-alcohol (1.83 g white crystals; 41%). Analytics: >99 GC; >99% ee (GC on BGB-176; 30 m¡Á0.25 mm; H2; 1.2 bar; 80 C. to 210 C. with 3 C./min; inj. 200 C.; Det. 210 C.; retention times: (R)-alcohol 29.60 min, (S)-alcohol 29.81 min). [alpha]D=-17.70 (c=1.00, CHCl3)., 159635-22-0

159635-22-0 tert-Butyl 3-hydroxy-4-methylenepiperidine-1-carboxylate 10584700, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Adam, Jean-Michel; Aebi, Johannes; Binggeli, Alfred; Green, Luke; Hartmann, Guido; Maerki, Hans P.; Mattei, Patrizio; Ricklin, Fabienne; Roche, Olivier; US2010/22518; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

91419-52-2, 1-Boc-4-Cyanopiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

91419-52-2, 4-Cyanopiperidine-1-formic acid tert-butyl ester (3.00 g, 14.27 mmol) was dissolved in tetrahydrofuran (30.00 mL), slowly added dropwise with lithium hexamethyldisilazide (1M, 28.54 mL) at -78 C and under nitrogen protection, stirred for 1 hour, slowly added dropwise with ethyl chloroformate (3.10 g, 28.54 mmol), and then stirred under nitrogen protection at -78 C for 1 hour. TLC showed that the reaction was complete. The reaction solution was quenched with a saturated solution of sodium bicarbonate (15 mL), and extracted with ethyl acetate (20 mL x 2), and the combined organic phases were washed with a saturated solution of ammonium chloride (50 mL), dried over anhydrous sodium sulfate (10 g), filtered and concentrated to give 1E. 1H NMR (400MHz, DMSO-d6) delta= 4.23 (q, J = 7.1 Hz, 2H), 4.00 – 3.92 (m, 2H), 2.95 (br, 2H), 2.07 (br d, J = 13.3 Hz, 2H), 1.89 – 1.76 (m, 2H), 1.40 (s, 9H), 1.24 (t, J = 7.1 Hz, 3H).

91419-52-2 1-Boc-4-Cyanopiperidine 1514443, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Medshine Discovery Inc.; LIU, Xile; DING, Charles Z.; CHEN, Shuhui; WU, Lingyun; HU, Lihong; WAN, Haiwen; (118 pag.)EP3567030; (2019); 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.268550-48-7,tert-Butyl 1-oxo-2,8-diazaspiro[4.5]decane-8-carboxylate,as a common compound, the synthetic route is as follows.

5-Bromo-3,4-dichloro-2-(2,5-dimethyl-1H-pyrrol-1-yl)pyridine (225 mg, 0.70 mmol) and 8- boc-2,8-diaza-spiro-[4.5]decan-1-one (197 mg, 0.77 mmol) were loaded in a microwave vial. The capped vial was evacuated using high vacuum and purged with nitrogen (each three times). Triethylamine (0.27 mL, 2.11 mmol) and NMP (2.3 mL) were added and the mixture was degassed by using the high vacuum and purged with nitrogen three times. The reaction mixture was heated in the microwave at 220 C for 1 h before it was cooled and dropped in vigorously stirred water (8 mL). The resulting precipitate was filtered off and the residue was purified by chromatography on silica gel (dichloromethane/ethanol) to give the title compound as a light brown solid (153 mg, 50%). 1H-NMR (500 MHz, CDCl3) ppm = 8.47 (s, 1H), 6.53 (bs, 1 H), 5.90 (s, 2H), 3.52 – 3.32 (m, 6H), 2.25 – 2.10 (m, 4H), 2.01 (s, 6H), 1.58 (d, J=13.0, 2H). HRMS m/z (ESI+) [M+H]+ C19H22BrClN4O, calc 437.0738, found 437.0733, Rt = 3.05 min (HPLC method B).

268550-48-7, The synthetic route of 268550-48-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK PATENT GMBH; CANCER RESEARCH TECHNOLOGY LIMITED; SCHIEMANN, kai; STIEBER, Frank; BLAGG, Julian; MALLINGER, Aurelie; WAALBOER, Dennis; RINK, Christian; CRUMPLER, Simon Ross; WO2014/63778; (2014); 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.255051-14-0,4-(2-(Trifluoromethyl)phenyl)piperidine hydrochloride,as a common compound, the synthetic route is as follows.

2-Amino 4,6-dichloro pyrimidine (0.164 g, 1 mmol), 4-(2-trifluoromethyl-phenyl)-piperidine hydrochloride (0.266 g, 1 mmol), and cesium carbonate (0.684 g, 2.1 mmol) were dissolved in a mixture of 1,4-dioxane (5 ml) and H2O (5 ml) in a 20 ml microwave vial. The mixture was stirred at 210 C. for 20 minutes in a microwave reactor. Solvent was removed and the residue was dissolved in 5% methanol in CH2Cl2 (20 ml), dried over Na2SO4 and concentrated to get the crude intermediate, 4-chloro-6-[4-(2-trifluoromethyl-phenyl)-piperidin-1-yl]-pyrimidin-2-ylamine (0.42 g) which was directly used in the following step. The crude intermediate (0.42 g), L-p-borono-phenylalanine (0.209 g, 1 mmol), sodium carbonate (0.210 g, 2 mmol), and dichlorobis(triphenylphosphine)-palladium(II) (35 mg, 0.05 mmol) were dissolved in a mixture of MeCN (2.5 ml) and H2O (2.5 ml) in a 10 ml microwave vial. The vial was sealed and stirred in a microwave reactor at 150 C. for 6 minutes. The mixture was filtered, and the filtrate was concentrated. The residue was dissolved in MeOH and H2O (1:1) and purified by preparative HPLC using MeOH/H2O/TFA as the solvent system to afford 2-amino-3-(4-{4-(2-trifluoromethyl-phenyl)-piperidine-1-yl]-pyrimidin-4-yl}-phenyl)-propionic acid as a TFA salt. HPLC: Method A, Retention time=3.203 min. LCMS M+1 486. 1H NMR (400 MHz, CD3OD) delta 1.80-2.20 (m, 5H), 3.0-3.16 (m, 2H), 3.22-3.42 (m, 2H), 4.22 (t, 1H), 4.42-4.54 (m, 1H), 5.22-5.34 (m, 1H), 6.80 (s, 1H), 7.40 (t, 1H), 7.50-7.60 (m, 4H), 7.68 (d, 1H), 7.82 (d, 2H)., 255051-14-0

The synthetic route of 255051-14-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Devasagayaraj, Arokiasamy; Jin, Haihong; Liu, Qingyun; Marinelli, Brett; Samala, Lakshama; Shi, Zhi-Cai; Tunoori, Ashok; Wang, Ying; Wu, Wenxue; Zhang, Chengmin; Zhang, Haiming; US2007/191370; (2007); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

620611-27-0, tert-Butyl 4-(aminomethyl)-4-fluoropiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

620611-27-0, fe/Y-butyl 4-((3 ,5-dichlorobenzamido)methyl)-4-fluoropiperidine- 1 -carboxylate (4-5); 1-Hydroxybenzotriazole (6.27 g, 46.4 mmol) and 3,5-dichlorobenzoic acid (8.13 g, 42.6 mmol) were suspended in 210 mL dry CH2Cl2. Diisopropylethylamine (13.5 mL, 77.4 mmol) was added and all compounds went into solution. Amine 4-4 (10.4 g crude, 38.7 mmol) was added in 210 mL dry CH2CI2. PS-carbodiimide resin (59.5 g, 77.4 mmol) was then added and the mixture was stirred for 14 h. MP-carbonate resin (41.8 g, 120 mmol) was added and stirring was resumed for 3 h. The reaction was then filtered to remove resin and concentrated in vacuo, yielding 22.2 g of crude 4-5 as a viscous yellow oil. The crude amide 4-5 was carried forward. 1HNMR (CDCl3, 300 MHz): 7.94 (d, J= 1.8 Hz, IH),7.66 (d, J= 1.8 Hz, 2H), 6.44 (br t, IH)5 3.93 (br, 2H), 3.65 (br, 2H), 3.12 (br t, 2H), 1.83 (br t, 2H), 1.67 (m, 2H), 1.46 (s, 9H); MS (Electrospray): m/z 427.1 (M+Na), 349.1 (M-t-Bu+H).

As the paragraph descriping shows that 620611-27-0 is playing an increasingly important role.

Reference£º
Patent; MERCK & CO., INC.; WO2007/2884; (2007); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.24228-40-8,Ethyl N-benzylpiperidine-4-carboxylate,as a common compound, the synthetic route is as follows.,24228-40-8

Step 1. 1-Benzylpiperidine-4-carboxylic acid Ethyl 1-benzylpiperidine-4-carboxylate (13.73 g) in methanol (100 ml) was treated with 40% aqueous sodium hydroxide (8.3 ml) at room temperature 16 h. The solvent was removed in vacuo and the residue re-dissolved in water (100 ml), acidified with dilute hydrochloric acid to pH 4 and concentrated. The residue was extracted with hot ethanol (200 ml), filtered and concentrated again. Addition of dichloromethane resulted in crystallization giving the title compound as a colourless crystaline solid, (3.24 g, 27%). Removal of solvent from the filtrate and trituration with ether gave a second batch as an amorphous white solid, (9.24 g, 73%); numax (CH2 Cl2) 2496 (vbr), 1720 and 1604 (br) cm-1.

The synthetic route of 24228-40-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Hinks; Jeremy David; Takle; Andrew Kenneth; Hunt; Eric; US6020368; (2000); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1155-56-2,1-Benzyl-N-phenylpiperidin-4-amine,as a common compound, the synthetic route is as follows.

Reference Example 2 N-(1-Benzyl-4-piperidinyl)-N-phenylacetamide (1-Benzyl-4-piperidinyl)-phenylamine obtained in Step1 of Reference Example 1 was heated in acetic anhydride at 70C to obtain the oily title compound.

1155-56-2, 1155-56-2 1-Benzyl-N-phenylpiperidin-4-amine 70865, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Takeda Pharmaceutical Company Limited; EP1559428; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

79421-45-7,79421-45-7, 1-(4-Nitrophenyl)piperidin-4-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 6 Synthesis of Compound 13 [Show Image] Compound 12 (1.50 g, 6.75 mmol) was dissolved in methanol (25 ml), 10% palladium-carbon (150 mg) was added, and the interior of the system was replaced with a hydrogen gas. After stirred at room temperature for 2 hours, the reaction solution was filtered using Celite, and washed with methanol. The filtrate, and the washing solution were combined, and the solvent was distilled off under reduced pressure to obtain Compound 13 (1.28 g, yield 99%). 1H-NMR (CDCl3 / TMS) deltappm: 1.70-1.80 (m, 2H), 2.07 (br, 2H), 2.84 (br, 2H), 3.37 (br, 3H), 3.85 (br, 1H), 6.65 (d, J = 8.4Hz, 2H), 6.91 (br, 2H).

As the paragraph descriping shows that 79421-45-7 is playing an increasingly important role.

Reference£º
Patent; SHIONOGI & CO., LTD.; EP1988077; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

1209780-71-1, tert-Butyl 3,3-difluoro-4-hydroxypiperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Tert-butyl 3,3-difluoro-4-hydroxypiperidine-1-carboxylate (8-1) (100 mg, 0.42 mmol) and tetrahydrofuran (5 mL) were added to a 25 mL flask, and cooled to 0 C under protection of nitrogen, sodium hydride (20 mg, 0.5 mmol) was added thereto, and the reaction was performed for 30 minutes. Iodomethane (120 mg, 0.84 mmol) was then added thereto, and the reaction was performed for 16 hours. The reaction solution was slowly poured into water, and a crude product of the title compound 100 mg was obtained after work-up, and was used directly for the next reaction without purification. ESI-MS (m/z): 252.2 [M+H]+,, 1209780-71-1

1209780-71-1 tert-Butyl 3,3-difluoro-4-hydroxypiperidine-1-carboxylate 56932106, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.; SONG, Shuai; CAI, Jiaqiang; TIAN, Qiang; ZENG, Hong; SONG, Hongmei; DENG, Hanwen; TANG, Zujian; DUAN, Xiaofan; LONG, Rongrong; LIU, Yao; WANG, Lichun; WANG, Jingyi; (80 pag.)EP3508483; (2019); 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.138163-07-2,1-Benzyl 4-methyl piperidine-1,4-dicarboxylate,as a common compound, the synthetic route is as follows.

General procedure: A 0.2 M solution of the corresponding methyl ester in aq NH4OH (28-30%) was stirred at r.t. for 16 h. The solvent was evaporated to affordthe amide, which was, in some cases, purified by silica gel chromatography. The known amides 3, 33 5a,34 5b, 6c 5h,35 11a,36 11b,37 11c,3611e,38 11h,4 11i,39 11j,39 13,40 14,41 20,42 and 2343 were synthesized following the general procedure described above. Compound 5e was synthesized following the literature.44, 138163-07-2

The synthetic route of 138163-07-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Keita, Massaba; Vandamme, Mathilde; Paquin, Jean-Francois; Synthesis; vol. 47; 23; (2015); p. 3758 – 3766;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem