Month: March 2022

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1062580-52-2,(3R,4R)-1-Benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride,as a common compound, the synthetic route is as follows.

Add SMA 11.0kg, SMB 12.8kg, DIPEA 19.5kg, DMSO to a 200L reactor50.0 kg, 15.0 kg of purified water, and the temperature was raised to 107C. After the reaction is complete, add 24.0kg absolute ethanol to room temperature and addWater 30.0kg, stirring and decrystallization 2h, suction filtration, drying at 60±5C, 17.2kg of white solid. Yield 93.0%, SMB residue0.3%, HPLC purity 98.9%.

1062580-52-2, The synthetic route of 1062580-52-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Yangzijiang Pharmaceutical Group Co., Ltd.; Xiao Can; Xu Jingren; Cai Wei; Zhu Xiaohe; Zhang Haibo; Lv Huimin; Hu Tao; Wu Jianhua; Gu Cheng; Xu Chenjun; (12 pag.)CN107793418; (2018); 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.71985-80-3,1-Methylpiperidine-4-carboxylic acid hydrochloride,as a common compound, the synthetic route is as follows.,71985-80-3

(iv) Methyl [3-({[3-(6-amino-2-butoxy-8-oxo-7,8-dihydro-9H-purin-9- yl)propyl][(l-methylpiperidin-4-yl)carbonyl]amino}methyl)phenyl]acetate; 5 The product from step (iii) (O.lg), diisopropyl ethylamine (0.1ml) and l-methylpiperidine-4- carboxylic acid hydrochloride (45mg) were dissolved in NMP (3ml) then etaATU (130mg) added to the mixture. The mixture was stirred at rt for 5h then purified by SCX and RPetaPLC, which afforded the title compound. Yield 70mg.1H NMR delta (DMSO- d6) 7.23 (IH, t), 7.12 (IH, d), 7.03 (IH, s), 7.02 (IH, d), 6.15 (2H, brs), o 4.50 (2H, s), 4.16 (2H, t), 3.65 (2H, t), 3.61 (2H, s), 3.60 (3H, s), 3.25 (2H, t), 2.68 (2H, m),2.10 (3H, s), 1.86- 1.96 (2H, m), 1.63 (5H, m), 1.42 (4H, m), 0.91 (3H, t).MS: APCI (+ve): 568 (M+l).

71985-80-3 1-Methylpiperidine-4-carboxylic acid hydrochloride 2760043, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; ASTRAZENECA AB; DAINIPPON SUMITOMO PHARMA CO., LTD; WO2008/4948; (2008); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

19099-93-5, 1-Cbz-Piperidin-4-one is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

19099-93-5, Benzyl 4-oxopiperidine-1-carboxylate (5g, 21 mmol) in THF (50 ml) was cooled to 0C. Sodium hydride (1.1 g, 43 mrnol), then iodomethane (3.0 ml, 47 mrnol) was added slowly. Mixture was stirred at 0C for 2 hours, then slowly warm up to room temperature and stirred overnight. Saturated aq. NH4C1 solution was added and the product was extracted with EtOAc. The extract was washed with brine, dried over anhydrous sodium sulfate, and concentrated. The crude product thus obtained was purified by column chromatography on a 100 grain-size silica gel column, eluting with gradient EtOAc/hexane to afford the titled product as colorless oil.

As the paragraph descriping shows that 19099-93-5 is playing an increasingly important role.

Reference：
Patent; MERCK SHARP & DOHME CORP.; ALI, Amjad; LO, Michael Man-Chu; LIM, Yeon-Hee; STAMFORD, Andrew; KUANG, Rongze; TEMPEST, Paul; YU, Younong; HUANG, Xianhai; HENDERSON, Timothy, J.; KIM, Jae-Hun; BOYCE, Christopher; TING, Pauline; ZHENG, Junying; METZGER, Edward; ZORN, Nicolas; XIAO, Dong; GALLO, Gioconda, V.; WON, Walter; WU, Heping; WO2014/105666; (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.236406-22-7,1-Boc-4-(Aminomethyl)-4-methylpiperidine,as a common compound, the synthetic route is as follows.

General procedure: General Procedure 2: To a stirred solution of 3-isopropylimidazopyridine carboxylic acid 11 (1.0 mmol) in DCM (6.0 mL) at r.t.,diisopropylethylamine (2.0 mmols) and Boc-protected amines 22 (1.05 mmols) were added. After 5 minutes, TBTU (500.0 mg, 1.05mmols) was added in portions over a period of 5 minutes. The reaction mixturewas stirred for 4 h before it was diluted with ice cold water and DCM. The twolayers were separated. The organic layer was washed with brine solution, driedover anhydrous Na2SO4 and the solvent was removed under reduced pressure. Thecrude compound was purified by silica gel column chromatography to obtaincompounds 23, 236406-22-7

As the paragraph descriping shows that 236406-22-7 is playing an increasingly important role.

Reference：
Article; Nirogi, Ramakrishna; Mohammed, Abdul Rasheed; Shinde, Anil K.; Bogaraju, Narsimha; Gagginapalli, Shankar Reddy; Ravella, Srinivasa Rao; Kota, Laxman; Bhyrapuneni, Gopinadh; Muddana, Nageswara Rao; Benade, Vijay; Palacharla, Raghava Chowdary; Jayarajan, Pradeep; Subramanian, Ramkumar; Goyal, Vinod Kumar; European Journal of Medicinal Chemistry; vol. 103; (2015); p. 289 – 301;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.768-66-1,2,2,6,6-Tetramethylpiperidine,as a common compound, the synthetic route is as follows.

20 g of 2,2,6,6-tetramethylpiperidine are mixed with 40.7 g, 1.1 eq, of 15% sodium hydroxide solution and cooled to 5 to 10C. Over a period of 1.5 hours, 10.8 g, 1.1 eq. of chlorine gas are introduced, then nitrogen gas is used to drive out the excess chlorine and the mixture is warmed to room temperature (RT). After separating the phases, washing the aqueous phase with 25 ml of dichloromethane, drying the combined organic phases with magnesium sulphate and distilling off the dichloromethane in vacuo, 24.2 g, 99%), of l-chloro-2,2,6,6-tetramethylpiperidine are obtained., 768-66-1

768-66-1 2,2,6,6-Tetramethylpiperidine 13035, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; BAYER INTELLECTUAL PROPERTY GMBH; FORD, Mark James; WO2013/120874; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

912368-73-1, (S)-tert-Butyl 3-(methylamino)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred solution of (S)-tert-butyl 3-(methylamino)piperidine- 1 -carboxylate (5 g, 25 mmol) in toluene (150 ml) was added triethylamine (5.42 ml, 37.5 mmol) followed by 3,4- dimethylfuran-2,5-dione (3.15 g, 2Smmol) at RT and the resulting reaction mixture was heated at reflux temperature for 16 h. The reaction mixture was cooled to RT and dilutedwith EtOAc and washed with water. The organic layer was dried and evaporated. The crude product was purified by flash chromatography to obtain 6.0 g of the product.?H NMR (300 MHz, CDC13) oe ppm 1.45 (s, 9H), 1.65- 1.83 (m, 2H), 1.95 (s, 6H), 2.05 – 2.29 (m, 2H), 2.60 – 2.75 (m, 1H), 3.22-3.35 (m, 1H), 3.92 – 4.10 (m, 3H)., 912368-73-1

Big data shows that 912368-73-1 is playing an increasingly important role.

Reference：
Patent; ORION CORPORATION; HAIKARAINEN, Anssi; KUMPULAINEN, Esa; POHJAKALLIO, Antti; PYSTYNEN, Jarmo; WANG, Shouming; (191 pag.)WO2018/2437; (2018); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

56839-43-1, 1-(4-Ethylphenyl)-2-methyl-3-(piperidin-1-yl)propan-1-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,56839-43-1

A mixture of 3.06 g (10.4 mmol) of racemic eperisone hydrochloride in ?0 mL of ethyl acetate was washed with two 50-mL portions of 4% aqueous sodium bicarbonate and one 50-mL portion of water. The ethyl acetate solution was dried over magnesium sulfate, filtered, and concentrated in vacuo to give 2.13 g (79% yield) of the free base as a colorless oil

As the paragraph descriping shows that 56839-43-1 is playing an increasingly important role.

Reference：
Patent; BIONEVIA PHARMACEUTICALS, INC.; KALOFONOS, Isabel; STAHLY, G., Patrick; MARTIN-DOYLE, William; KALOFONOS, Dimitris; STULTS, Jeffrey, S.; HANKO, Jason, A.; WO2010/81070; (2010); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

4801-58-5, Piperidin-1-ol is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a 25-mL flask equipped with a magnetic stirrer, in which the air was replaced by N2, was added CuBr (0.05 mmol), toluene (1.0 mL), aldehyde (1.0 mmol), alkyne (1.5 mmol), and hydroxylamine (1.5 mmol). The mixture was stirred at 70C. After the completion of the reaction (monitored by TLC), the reaction solution was submitted to flash chromatographic separation on silica gel using petroleum ether/ethyl acetate as an eluent to give the corresponding product., 4801-58-5

As the paragraph descriping shows that 4801-58-5 is playing an increasingly important role.

Reference：
Article; Guo, Na; Ji, Jian-Xin; Tetrahedron Letters; vol. 53; 36; (2012); p. 4797 – 4801;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.85908-96-9,N-Boc-2-Piperidone,as a common compound, the synthetic route is as follows.

85908-96-9, General procedure: To a solution of compounds 15, 16, 17 (2 mmol) and diphenyl phosphoryl chloride (0.62 mL, 3 mmol) in anhydrous THF (30 mL) cooled at -78 C and under nitrogen atmosphere, was added dropwise with stirring a solution of KHMDS (6 mL, 0.5 M in toluene, 3 mmol). After 30 min at -78 C, water (20 mL) was added and the resulting mixture was extracted with Et2O (2 × 50 mL) and dried over MgSO4. Evaporation of the solvent under vacuum yielded the vinyl phosphates as yellow oils, which were used directly in the next coupling step.

85908-96-9 N-Boc-2-Piperidone 7577838, apiperidines compound, is more and more widely used in various fields.

Reference：
Article; Sallio, Romain; Lebrun, Stephane; Agbossou-Niedercorn, Francine; Michon, Christophe; Deniau, Eric; Tetrahedron Asymmetry; vol. 23; 13; (2012); p. 998 – 1004;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

122860-33-7, Benzyl 4-(hydroxymethyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step A: benzyl 4-(iodomethyl)piperidine-1-carboxylate (1165) A solution of I2 (9.77 g, 38.50 mmol) in THF (5 mL) was added in dropwise to a stirred solution of benzyl 4-(hydroxymethyl)piperidine-1-carboxylate (8.00 g, 32.10 mmol), 1H-imidazole (2.62 g, 38.50 mmol) and triphenylphosphine (10.10 g, 38.50 mmol) in THF (15 mL) at ambient temperature in a period of 4 hr. The reaction mixture was then quenched with water (30 mL), diluted with water (40 mL) and extracted with EtOAc (3×40 mL). The combined organic layers were washed with water (20 mL) and brine (20 mL), dried over anhydrous Na2SO4 and concentrated under reduced pressure. The residue was purified by silica gel, eluted with EtOAc/PE (1/10) to afford the title compound: LCMS (ESI) calc’d for C14H18INO2 [M+H]+: 360. found 360.

122860-33-7, 122860-33-7 Benzyl 4-(hydroxymethyl)piperidine-1-carboxylate 736490, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; Merck Sharp & Dohme Corp.; Mandal, Mihir; Tang, Haifeng; Xiao, Li; Su, Jing; Li, Guoqing; Yang, Shu-Wei; Pan, Weidong; Tang, Haiqun; DeJesus, Reynalda; Hicks, Jacqueline; Lombardo, Matthew; Chu, Hong; Hagmann, William; Pasternak, Alex; Gu, Xin; Jiang, Jinlong; Dong, Shuzhi; Ding, Fa-Xiang; London, Clare; Biswas, Dipshikha; Young, Katherine; Hunter, David N.; Zhao, Zhiqiang; Yang, Dexi; (405 pag.)US2016/333021; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem