Heterocyclic Building Blocks-piperidine

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3970-68-1,4-Methylpiperidin-4-ol,as a common compound, the synthetic route is as follows.

To a solution of 0.04 g (0.1 mmol) of 4-[(S)-4-(3-chloro-phenylcarbamoyl)-3-methyl-2-oxo- piperazin-l-yl]-butyric acid (intermediate 19) and 0.04 ml of triethylamine (0.3 mmol) in 0.8 ml DMF was added 0.05 g (0.12 mmol) of HATU. The mixture was shaken for 10 minutes before being added to the appropriate amine (0.12 mmol) and the mixture shaken overnight. The mixture was then directly purified by preparative HPLC.

3970-68-1, As the paragraph descriping shows that 3970-68-1 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; AEBI, Johannes; BINGGELI, Alfred; GREEN, Luke; HARTMANN, Guido; MAERKI, Hans P.; MATTEI, Patrizio; WO2011/48032; (2011); A1;,
Piperidine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.22540-50-7,6-Oxopiperidine-3-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of intermediate 5b (100 mg, 0.248 mmol) in DCM (5 mL) was added 6-oxopiperidine-3-carboxylic acid (38 mg, 0.265 mmol), EDC (51 mg, 0.266 mmol) and DMAP (2.5 mg) and the solution was stirred at room temperature for 5 h. A second addition of 6-oxopiperidine-3-carboxylic acid (38 mg), EDC (51 mg), and DMAP (2.5 mg) was performed and it was stirred over night. A third addition of 6-oxopiperidine-3-carboxylic acid (38 mg) and EDC (51 mg) was performed and it was stirred over night. The reaction mixture was diluted with DCM (50 mL) and extracted twice with water, saturated sodium bicarbonate solution and with brine. The organic layer was dried over sodium sulfate and the solvent was removed under reduced pressure

22540-50-7, The synthetic route of 22540-50-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Santhera Pharmaceuticals (Schweiz) AG; EP2439197; (2012); A1;,
Piperidine – Wikipedia
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25504-47-6, Methyl 2-oxopiperidine-4-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Add Lawesson’s reagent (9.2 g, 22.7 mmol) to a solution of methyl2-oxopiperidine-4-carboxylate (6.5 g, 41.4 mmol) in toluene (83 mL) and heat to reflux for 2 hours. Cool the solution and concentrate to dryness under reduced pressure. Purify the residue by flash chromatography on silica gel, eluting with ethyl acetate :dichloromethane (gradient 5-15percent) to afford the title compound (6.95 g). lH NMR (CDCI3) delta 1.97 (m, 1H), 2.17 (m, 1H), 2.78 (m, 1H), 3.03 (m, 1H), 3.24 (m, 1H), 3.39 (m, 1H), 3.49 (m, 1H), 3.72 (s, 3H), 8.48 (bs, 1H)., 25504-47-6

The synthetic route of 25504-47-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ELI LILLY AND COMPANY; PRIETO, Lourdes; TABOADA MARTINEZ, Lorena; WO2011/82010; (2011); A1;,
Piperidine – Wikipedia
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.163271-08-7,tert-Butyl (4-methylpiperidin-4-yl)carbamate,as a common compound, the synthetic route is as follows.

To a solution of 3-(benzyloxy)-5-bromo-2-(2,3-dichlorophenyl)pyrazine (90.0 mg, 220 muetaiotaomicron, 1 equiv) in toluene (1 mL) was added ter/-butyl(4-methylpiperidin-4-yl)carbamate (70.5 mg, 329 muiotaetaomicron, 1.5 equiv), NaOt-Bu (42.2 mg, 439 muiotaetaomicron, 2 equiv), [l-(2- diphenylphosphanyl-l-naphthyl)-2-naphthyl]-diphenyl-phosphane (137 mg, 219 muiotaetaomicron, 1 equiv) and Pd2(dba)3 (10.0 mg, 11.0 mumol, 0.05 equiv). The reaction mixture was then warmed to 90 C and stirred for 1 hour. The reaction mixture was then filtered and concentrated under reduced pressure. The residue was purified by silica gel chromatography to give fer/-butyl(l-(6- (benzyloxy)-5-(2,3-dichlorophenyl)pyrazin-2-yl)-4-methylpiperidin-4-yl)carbamate (100 mg, 184 mupiiotaomicron, 83.8% yield) as a white solid.

163271-08-7, 163271-08-7 tert-Butyl (4-methylpiperidin-4-yl)carbamate 19691370, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; REVOLUTION MEDICINES, INC.; JOGALEKAR, Ash; WON, Walter; KOLTUN, Elena S.; GILL, Adrian; MELLEM, Kevin; AAY, Naing; BUCKL, Andreas; SEMKO, Christopher; KISS, Gert; (496 pag.)WO2018/13597; (2018); A1;,
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Piperidine | C5H11N – PubChem

167414-75-7, Benzyl 4-(3-ethoxy-3-oxopropanoyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

167414-75-7, Intermediate 5, 3.8 g (20 mmol), intermediate 3 7.99 g (24 mmol) was added to a 50 mL round bottom flask. Add 20 mL of acetic acid to dissolve, and react at 130 ¡ãC overnight. After the reaction is completed, the acetic acid is removed by rotary evaporation. 1M NaOH was added dropwise to precipitate a large amount of off-white solid, which was filtered. Washing with a small amount of MeOH gave a white solid M086. Yield 75.0percent.

The synthetic route of 167414-75-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Kunming Xianghao Technology Co., Ltd.; Luo Huairong; Hong Xuechuan; Zhu Xi; Zhu Jinmei; Wu Guisheng; Deng Zixin; Zhu Yingmin; Lu Yungang; Deng Ke; Qu Chunrong; (25 pag.)CN103694242; (2016); B;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1029413-55-5,tert-Butyl 4-(4-amino-1H-pyrazol-1-yl)piperidine-1-carboxylate,as a common compound, the synthetic route is as follows.

Compound 48-b (250 mg, 0.68 mmol) and compound 32-c (181 mg, 0.68 mmol) were dissolved in N,N-dimethylformamide (3 mL), and potassium carbonate (281 mg, 2.37 mmol), 2-dicyclohexylphosphino-2?,6?-diisopropoxy-1,1?-biphenyl (58 mg, 0.13 mmol) and tris(dibenzylideneacetone)dipalladium (136 mg, 0.24 mmol) were added. The reaction solution was heated to 110 C. and stirred for 16 hours under nitrogen gas atmosphere. After cooling to room temperature, the reaction mixture was partitioned between ethyl acetate (100 mL) and water (100 mL). The organic phase was dried over anhydrous sodium sulfate, filtered and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel TLC preparative plate (petroleum ether: ethyl acetate=1:1) to give 48-a as a pale yellow solid (75 mg, yield 18%). LC-MS (ESI): m/z=599[M+H]+.

1029413-55-5, As the paragraph descriping shows that 1029413-55-5 is playing an increasingly important role.

Reference£º
Patent; GUANGZHOU MAXINOVEL PHARMACEUTICALS CO., LTD.; XU, Zusheng; ZHANG, Nong; WANG, Tinghan; SUN, Qingrui; WANG, Yuguang; (90 pag.)US2018/208604; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

496807-97-7,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.496807-97-7,3,3-Difluoropiperidine hydrochloride,as a common compound, the synthetic route is as follows.

To a dichloroethane (10 mL) solution of methyl (lS)-3- oxocyclopentanecarboxylate (0.28 mL, 2.2 mmol, step A), 3,3-difluoropiperidine hydrochloride (420 mg, 2.7 mmol, 1.2 equiv.), and triethylamine (0.43 mL, 3.1 mmol, 1.4 equiv.) were added sodium triacetoxyborohydride (940 mg, 4.4 mmol, 2.0 equiv.) and acetic acid (0.25 mL, 4.4 mmol, 2.0 equiv.). The reaction mixture was stirred at room temperature for 12 hours and quenched with IN aqueous sodium hydroxide. It was extracted with dichloroethane, dried (sodium sulfate), and concentrated in vacuo to afford a crude product. Chromatography over silica gel, eluting with hexanes/ethyl acetate, afforded the title compound as a diastereomeric mixture. LC/MS = 248 [M+l].

As the paragraph descriping shows that 496807-97-7 is playing an increasingly important role.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; ALI, Amjad; GALLO, Gioconda V.; HENDERSON, Timothy J.; KUANG, Rongze; LIM, Yeon-Hee; LO, Michael Man-Chu; METZGER, Edward; RUIZ, Manuel de Lera; STAMFORD, Andrew; TEMPEST, Paul; WHITEHEAD, Brent; WU, Heping; WO2015/27431; (2015); A1;; ; Patent; MERCK SHARP & DOHME CORP.; ALI, Amjad; GALLO, Gioconda, V.; HENDERSON, Timothy, J.; KUANG, Rongze; LIM, Yeon-Hee; LO, Michael Man-Chu; METZGER, Edward; RUIZ, Manuel de Lera; STAMFORD, Andrew; TEMPEST, Paul; WHITEHEAD, Brent; WU, Heping; WO2015/31221; (2015); 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.21987-29-1,4,4-Difluoropiperidine,as a common compound, the synthetic route is as follows.

A mixture of Intermediate B (879 mg, 3.30 mmol), 4,4-difluoropiperidine (400 mg, 3.30 mmol), Pd2(dba)3 (302 mg, 0.330 mmol), xantphos (382 mg, 0.660 mmol) and KO’Bu (748 mg, 6.60 mmol) in toluene (10 ml) was bubbled with argon for 10 min. The mixture was then heated at 100¡ãC for overnight. The reaction was quenched with 60percent NaHC03 aqueous solution. The aqueous phase was extracted with DCM/IPA (20 ml x3, V/V = 3/1 ). The combined organic phase was dried over anhydrous MgS04. Filtered and concentrated. The residue was purified by silica gel chromatography (eluted with 2percent MeOH in DCM) to give the title compound as yellow solid (270 mg, 31 percent yield). LCMS (method B): [M+H]+ = 265, tR = 1.79 min.

21987-29-1, 21987-29-1 4,4-Difluoropiperidine 2758352, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; NOVARTIS AG; CHEN, Chao; DENG, Haibing; GUO, Haibing; HE, Feng; JIANG, Lei; LIANG, Fang; MI, Yuan; WAN, Huixin; XU, Yao-Chang; YU, Hongping; ZHANG, Ji Yue (Jeff); WO2013/38362; (2013); 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.24211-55-0,(S)-Piperidin-3-ol,as a common compound, the synthetic route is as follows.

4-Chloro-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine (43 mg, 0.10 mmol) prepared in step 4 of Example 1 was dissolved in 5 mL of tetrahydrofuran, and (S)-3-hydroxypiperidine (12 mg, 0.12 mmol) and sodium carbonate (16 mg, 0.15 mmol) were added. The mixture was heated under reflux for 16 h. The resultant solution was filtered, and the filtrate was purified by column chromatography to give the title compound. 1H NMR (500MHz, DMSO-d6): delta 10.70 (br, 1H), 8.55-8.66 (m, 3H), 8.26-8.33 (m, 1H), 8.08-8.11 (m, 1H), 7.85 -7.96 (m, 1H), 4.97-4.98 (m, 1H), 4.16-4.49 (m, 2H), 3.26-3.60 (m, 3H), 1.83-1.92 (m, 2H), 1.51-1.54 (m, 2H).ES: m/z 486.1 [M+H]+., 24211-55-0

24211-55-0 (S)-Piperidin-3-ol 6950221, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; Nanjing Sanhome Pharmaceutical Co., Ltd.; WANG, Yong; ZHAO, Liwen; LIU, Xiaorong; ZHANG, Yan; HUANG, Dandan; JIANG, Chunhuan; SHI, Xinsheng; GU, Hongfeng; PANG, Silin; HAI, Wei; GE, Bingyang; (71 pag.)EP3489230; (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.1095010-47-1,1-tert-Butyl 3-methyl 5-hydroxypiperidine-1,3-dicarboxylate,as a common compound, the synthetic route is as follows.

To a dichloromethane solution (25 mL) of 1-tert-butyl 3-methyl 5-hydroxypiperidine-1,3-dicarboxylate (1.30 g), Dess-Martin reagent (2.33 g) was added. After stirring for 3 hours at room temperature, Dess-Martin reagent (1.31 g) was further added to the reaction solution, and the mixture was stirred for further 2.5 hours. Then, saturated aqueous solution of sodium hydrogen carbonate (50 mL) and a 10% sodium thiosulfate aqueous solution (50 mL) were added sequentially to the mixture, and the organic layer was separated. The product was further extracted from the aqueous layer with dichloromethane (10 mL) four times. The obtained organic layer was dried with anhydrous sodium sulfate, filtered. The filtrate was concentrated under reduced pressure, the residue was purified with silica gel column chromatography (chloroform/methanol=100/0 to 98/2) to give 1-tert-butyl 3-methyl 5-oxopiperidine-1,3-dicarboxylate (1.14 g) as an oil. 1H NMR (300 MHz, CDCl3) delta 1.46 (s, 9H), 2.58-2.79 (m, 2H), 3.03-3.11 (m, 1H), 3.73 (s, 3H), 3.77-3.93 (m, 2H), 4.02 (s, 2H)

1095010-47-1, 1095010-47-1 1-tert-Butyl 3-methyl 5-hydroxypiperidine-1,3-dicarboxylate 45790959, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; SUMITOMO CHEMICAL COMPANY, LIMITED; SUMITOMO DAINIPPON PHARMA CO., LTD.; FUSANO, Akira; KOBAYASHI, Tomonori; SAITO, Yasuhiro; KANAI, Toshio; (55 pag.)US2016/221948; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem