Category: 220394-97-8

220394-97-8, 1-Boc-4-(Cbz-amino)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of r/-butyl 4-(benzyloxycarbonylamino)piperidine-l -carboxylate (2.13 g, 6.38 mmol) in methanol (20 mL) was added 4 N hydrogen chloride in dioxane (8.0 mL, 31.8 mmol) in a dropwise manner at room temperature, then heated to 40 C for 1 hour. The mixture was concentrated and dried to give benzyl piperidin-4-ylcarbamate hydrochloride as a white solid, which was used without further purification. MS (EI) for C |3H,8N202: 235.0 (MH+).

220394-97-8, The synthetic route of 220394-97-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; EXELIXIS, INC.; RICE, Kenneth, D.; FOSTER, Paul; WO2014/160177; (2014); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

220394-97-8, 1-Boc-4-(Cbz-amino)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Piperidin-4-yl-carbamic acid benzyl ester[00457] HCl (10ml, 4M solution in dioxane) was added in one portstirred solution of 4-benzyloxycarbonylamino-piperidine-1 -carboxylic acid te/f-butyl ester (1 .2g, 3.6mmol) in dioxane (5ml) and the suspension was stirred at room temperature under a nitrogen atmosphere for 3 hours. After this time the reaction was concentrated under vacuum and the resulting solid was collected by filtration, washed with TBME (3 x 100ml) and dried under vacuum to give the title compound (0.74g, 88% yield) as a white solid.

220394-97-8, The synthetic route of 220394-97-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CHDI, INC.; DOMINGUEZ, Celia; WITYAK, John; PRIME, Michael; COURTNEY, Stephen; YARNOLD, Christoper; BROOKFIELD, Frederick; MARSTON, Richard; MACDONALD, Douglas; WO2011/60321; (2011); 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.220394-97-8,1-Boc-4-(Cbz-amino)piperidine,as a common compound, the synthetic route is as follows.

tert -Butyl 4-(((benzyloxy)carbonyl)amino)piperidine-l-carboxylate (49.0 g, 0.147 mol) in a solution of HC1 in MeOH (4N, 400 mL) was stirred at 23 C for 2 h. The reaction mixture was concentrated to give benzyl piperidin-4-ylcarbamate hydrochloride as a yellow solid. ‘H NMR (400 MHz, CD3OD): delta 7.37- 7.31 (m, 5H), 5.10 (s, 2H), 3.74 -3.71 (m, 1H), 3.43-3.39 (m, 2H), 3.10- 3.07 (m, 2H), 2.15- 2.10 (m, 2H), 1.75 (dd, J = 10.4, 22 Hz, 2H).

220394-97-8, 220394-97-8 1-Boc-4-(Cbz-amino)piperidine 1514305, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; MERCK SHARP & DOHME CORP.; CROWLEY, Brendan; FRALEY, Mark; POTTEIGER, Craig; GILFILLAN, Robert; PATEL, Mehul; ARRINGTON, Ken; MITCHELL, Helen; SCHIRRIPA, Kathy; MCWHERTER, Melody; BIFTU, Tesfaye; NAIR, Anilkumar; WANG, Cheng; YANG, De-Yi; ZHU, Cheng; KAR, Nam Fung; HUANG, Xianhai; CHEN, Lei; ZHOU, Wei; LIU, Qingsheng; CAI, Jiaqiang; WO2015/161011; (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.220394-97-8,1-Boc-4-(Cbz-amino)piperidine,as a common compound, the synthetic route is as follows.

Step 2To a solution of 68 (13 g, 38.9 mmol) in DCM (5 mL) was added HCl/EA (20 mL). The mixturewas stirred at rt for 2 h. The mixture was filtered and filter cake was concentrated under vacuum to afford 69 (7.59 g, 83% yield).

220394-97-8, As the paragraph descriping shows that 220394-97-8 is playing an increasingly important role.

Reference：
Patent; SYROS PHARMACEUTICALS, INC.; PARAZA PHARMA, INC.; CIBLAT, Stephane; DEROY, Patrick; LEBLANC, Melissa; MARINEAU, Jason, J.; MOORE, Joel; ROY, Stephanie; SIDDIQUI, M., Arshad; SPROTT, Kevin; WINTER, Dana, K.; KABRO, Anzheliika; LEGER, Serge; MILLER, Tom; SCHMIDT, Darby; BRADLEY, Michael; WO2015/58163; (2015); A2;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

220394-97-8, 1-Boc-4-(Cbz-amino)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The tert-butyl 4- (benzyloxycarbonylamino) piperidine-1-carboxylate (6.38 g) obtained in Step 1 was dissolved in 1,4-dioxane (27 mL). Hydrogen chloride / 1,4-dioxane solution (55 mL, 4 M) was added thereto at room temperature, and the mixture was stirred at room temperature for 5 hours. Thereafter, the obtained solution was concentrated under reduced pressure. The obtained residue was washed with tert-butyl methyl ether (150 mL) to give the title compound (4.76 g, yield 92%).

220394-97-8, 220394-97-8 1-Boc-4-(Cbz-amino)piperidine 1514305, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; NIPPON SODA COMPANY LIMITED; IHORI, YOICHI; INOUE, SHUJI; SHIBAYAMA, KOTARO; KANG, CHANG-KYUNG; SHIINOKI, YASUYUKI; NISHIMURA, SATOSHI; (65 pag.)JP2016/222654; (2016); 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.220394-97-8,1-Boc-4-(Cbz-amino)piperidine,as a common compound, the synthetic route is as follows.

(Example 1b) Benzyl N-(piperidin-4-yl)carbamate A mixture of tert-butyl 4-{[(benzyloxy)carbonyl]amino}piperidine-1-carboxylate obtained in Example 1a (13.1 g, 39.2 mmol), a 5 N aqueous hydrochloric acid solution (40 ml, 200 mmol) and methanol (40 ml) was stirred at room temperature for 23 hours. A 5 N aqueous sodium hydroxide solution (40 ml) was added to the reaction mixture under ice-cooling. Water and the solvent were distilled off from the reaction mixture while the mixture was azeotropically distilled with ethanol. Ethanol was added to the residue, the insoluble matter was removed by filtration, and the filtrate was concentrated to give the title compound (9.10 g, yield 99.1%). 1H-NMR (400 MHz, CDCl3) delta ppm; 1.31-1.42 (2H, m), 1.92-2.04 (2H, br), 2.70 (2H, d, J=12 Hz), 3.10 (2H, d, J=12 Hz), 3.56-3.68 (1H, br), 4.72-4.81 (1H, br), 5.09 (2H, s), 7.26-7.40 (5H, m).

220394-97-8, As the paragraph descriping shows that 220394-97-8 is playing an increasingly important role.

Reference：
Patent; Eisai R&D Management Co., Ltd.; YOSHIDA Ichiro; OKABE Tadashi; MATSUMOTO Yasunobu; WATANABE Nobuhisa; OHASHI Yoshiaki; ONIZAWA Yuji; HARADA Hitoshi; EP2757103; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

220394-97-8, 1-Boc-4-(Cbz-amino)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of tert-butyl 4-{[(benzyloxy)carbonyl]amino}piperidine-1-carboxylate obtained in Example 1a (13.1 g, 39.2 mmol), a 5 N aqueous hydrochloric acid solution (40 ml, 200 mmol) and methanol (40 ml) was stirred at mom temperature for 23 hours. A 5 N aqueous sodium hydroxide solution (40 ml) was added to the reaction mixture under ice-cooling. Water and the solvent were distilled off from the reaction mixture while the mixture was azeotropically distilled with ethanol. Ethanol was added to the residue, the insoluble matter was removed by filtration, and the filtrate was concentrated to give the title compound (9.10 g, yield 99.1%). 1H-NMR (400 MHz, CDCl3) delta ppm; 1.31-1.42 (2H, m), 1.92-2.04 (2H, br), 2.70 (2H, d, J=12 Hz), 3.10 (2H, d, J=12 Hz), 3.56-3.68 (1H, br), 4.72-4.81 (1H, br), 5.09 (2H, s), 7.26-7.40 (5H, m)., 220394-97-8

220394-97-8 1-Boc-4-(Cbz-amino)piperidine 1514305, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; EISAI R&D MANAGEMENT CO., LTD.; YOSHIDA, Ichiro; OKABE, Tadashi; MATSUMOTO, Yasunobu; WATANABE, Nobuhisa; ONIZAWA, Yuji; OHASHI, Yoshiaki; HARADA, Hitoshi; US2013/65925; (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.220394-97-8,1-Boc-4-(Cbz-amino)piperidine,as a common compound, the synthetic route is as follows.

Benzyloxycarboxamide-tert-butyl piperidine-1-carboxylate (0.334 g, 1 mmol),Was dissolved in 5 mL of chloroform, TFA (3.42 g, 30 mmol) was dropped at room temperature,The reaction was stirred for 1h, the excess TFA was distilled off under reduced pressure,Add DIEA (0.258g, 2mmol), cyclopentanone 1mL, sodium triacetoxyborohydride (0.636g, 3mmol), the reaction at room temperature for 1h, add a small amount of water quenched reaction, saturated sodium bicarbonate to adjust pH = 6 ~ 7, The mixture was extracted with dichloromethane and dried over anhydrous sodium sulfate. After concentration, the residue was subjected to column chromatography to obtain 0.314 g of a white solid in a yield of 104%., 220394-97-8

The synthetic route of 220394-97-8 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; Chinese Academy Of Medical Sciences Pharmaceutical Institute; Xu Boling; Chen Xiaoguang; Jin Jing; Zhu Lina; Zhang Chongjing; (85 pag.)CN102250075; (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.220394-97-8,1-Boc-4-(Cbz-amino)piperidine,as a common compound, the synthetic route is as follows.

(Example 1b) Benzyl N-(piperidin-4-yl)carbamate A mixture of tert-butyl 4-{[(benzyloxy)carbonyl]amino}piperidine-1-carboxylate obtained in Example 1a (13.1 g, 39.2 mmol), a 5 N aqueous hydrochloric acid solution (40 ml, 200 mmol) and methanol (40 ml) was stirred at room temperature for 23 hours. A 5 N aqueous sodium hydroxide solution (40 ml) was added to the reaction mixture under ice-cooling. Water and the solvent were distilled off from the reaction mixture while the mixture was azeotropically distilled with ethanol. Ethanol was added to the residue, the insoluble matter was removed by filtration, and the filtrate was concentrated to give the title compound (9.10 g, yield 99.1%). 1H-NMR (400 MHz, CDCl3) delta ppm; 1.31-1.42 (2H, m), 1.92-2.04 (2H, br), 2.70 (2H, d, J=12 Hz), 3.10 (2H, d, J=12 Hz), 3.56-3.68 (1H, br), 4.72-4.81 (1H, br), 5.09 (2H, s), 7.26-7.40 (5H, m).

220394-97-8, As the paragraph descriping shows that 220394-97-8 is playing an increasingly important role.

Reference：
Patent; Eisai R&D Management Co., Ltd.; YOSHIDA Ichiro; OKABE Tadashi; MATSUMOTO Yasunobu; WATANABE Nobuhisa; OHASHI Yoshiaki; ONIZAWA Yuji; HARADA Hitoshi; EP2757103; (2014); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

220394-97-8, 1-Boc-4-(Cbz-amino)piperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of tert-butyl 4-{[(benzyloxy)carbonyl]amino}piperidine-1-carboxylate obtained in Example 1a (13.1 g, 39.2 mmol), a 5 N aqueous hydrochloric acid solution (40 ml, 200 mmol) and methanol (40 ml) was stirred at mom temperature for 23 hours. A 5 N aqueous sodium hydroxide solution (40 ml) was added to the reaction mixture under ice-cooling. Water and the solvent were distilled off from the reaction mixture while the mixture was azeotropically distilled with ethanol. Ethanol was added to the residue, the insoluble matter was removed by filtration, and the filtrate was concentrated to give the title compound (9.10 g, yield 99.1%). 1H-NMR (400 MHz, CDCl3) delta ppm; 1.31-1.42 (2H, m), 1.92-2.04 (2H, br), 2.70 (2H, d, J=12 Hz), 3.10 (2H, d, J=12 Hz), 3.56-3.68 (1H, br), 4.72-4.81 (1H, br), 5.09 (2H, s), 7.26-7.40 (5H, m).

220394-97-8, 220394-97-8 1-Boc-4-(Cbz-amino)piperidine 1514305, apiperidines compound, is more and more widely used in various fields.

Reference：
Patent; EISAI R&D MANAGEMENT CO., LTD.; YOSHIDA, Ichiro; OKABE, Tadashi; MATSUMOTO, Yasunobu; WATANABE, Nobuhisa; ONIZAWA, Yuji; OHASHI, Yoshiaki; HARADA, Hitoshi; US2013/65925; (2013); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem