Category: 138377-80-7

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.

[Preparation Example 116] Preparation of 3-[(benzylsulfonyl)(methyl)amino]-N-((1S,2S,4R)-2-{[tert- butyl(dimethyl)silyl]oxy}-1-isobutyl-4-methyl-5-oxo-5-{[(3R or 3S)-2- OXOPIPERIDINYL] AMMO} PENTVBENZAMIDE 91 mg (0. 15 mmol) of the compound obtained in Preparation Example 58 was dissolved in 5 ml of N, N-DIMETHYLFORMAMIDE and cooled to 0°C, then 34 mg (0.225 mmol) obtained in Preparation Example 115 and 86 mg (0.225 mmol) of HATU were added thereto. 0.5 ml (excess amount) of N, N-diisopropylethylamine was then added thereto and heated to room temperature, followed by stirring for 3 hours. After removing solvent by distillation under reduced pressure, the residue was dissolved in ethyl acetate and washed with water, 0.5 N hydrochloride solution, saturated sodium bicarbonate solution and sodium chloride solution. After removing solvent by distillation under reduced pressure, the product was purified by column chromatography using a 5: 95 mixture of methanol and dichloromethane to obtain 21 mg of the title compound at 20percent yield. 1H NMR (400 MHz, CDC) ; 7.82 (1H, s), 7.59 (1H, d), 7.45-7. 33 (7H, m), 6.79 (1H, d), 6.27 (1H, d), 5.48 (1H, s), 4.50-4. 20 (4H, m), 3.80 (1H, m), 3.23 (3H, s), 3.22-3. 12 (2H, m), 2.54 (1H, m), 2.28 (1H, m), 1.97 (1H, m), 1.92-1. 48 (6H, m), 1.39 (1H, m), 1.17 (3H, d), 0.98 (3H, d), 0.97 (3H, d), 0.91 (9H, s), 0.12 (3H, s), 0.11 (3H, s), 138377-80-7

As the paragraph descriping shows that 138377-80-7 is playing an increasingly important role.

Reference：
Patent; LG Life Sciences Ltd.; ProMediTech, Inc.; WO2005/30709; (2005); 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;,
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

138377-80-7, 3-Aminopiperidin-2-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Phenyl {3-[(2-aminopyrimidin-5-yl) ethynyl] phenyl} carbamate (Example 23) (50 mg), 3- amino-piperidin-2-one hydrochloride (46 mg) and triethylamine (0.06 mL) in THF (2 mL) were heated at 80°C for 24 hours. The reaction mixture was concentrated in vacuo and the solid triturated with water then diethyl ether, dried under vacuum at 60°C to give the title compound as a beige solid (41 mg, 77percent) ; ‘H NMR (DMSO-d6) 1.49-1. 62 (m, 1H), 1.71-1. 82 (m, 2H), 2.16-2. 28 (m, 1H), 3.10-3. 18 (m, 2H), 3.95-4. 04 (m, 1H), 6.42-6. 48 (d, 2H), 6.98-7. 04 (m, 1H), 7.09 (s, 2H), 7.20-7. 31 (m, 2H), 7.65 (s, 2H), 8.41 (s, 2H), 8.85 (s, 1H) ; MS m/e MH 351., 138377-80-7

As the paragraph descriping shows that 138377-80-7 is playing an increasingly important role.

Reference：
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/60970; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

138377-80-7, 3-Aminopiperidin-2-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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

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 60C 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

As the paragraph descriping shows that 138377-80-7 is playing an increasingly important role.

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

138377-80-7, 3-Aminopiperidin-2-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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 60C 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;,
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.

Reference Example 1 : 3-(4,-MethylbenzenesuIfonylamino)tetrahydropyridin-2- one:; 3-aminotetrahydropyridin-2-one hydrochloride (10 mmol), K2C03 (30 mmol) and 4- methylbenzenesulfonyl chloride (10 mmol) were reacted according to the above procedure to give the product (1.64 g, 69percent):Vmax/cm”1 3224, 1658 (secondary CONH, lactam), 1598, 1494 (aromatic ring), 1324, 1161 (S02-N), 814, 802 (pam-disubstituted benzene). NMR: deltaEta (400MHz, CDC13) 7.77 (2H, d, J 8.5, ortho-U), 7.29 (2H, d, J 8.0, meta- H), 5.79 (1H, br d, J 1.0, C7H7-S02NH), 5.56 (1Eta, br s, CONH-CH2), 3.49-3.42 (1H, m, CH-CO), 3.31-3.24 (2H, m, CH2NH), 2.53-2.45 (1H, m, lactam CH2), 2.40 (3H, s, CH3), 1.97-1.88 (1H, m, lactam CH2), 1.88-1.68 (2H, m, lactam CH2). 13C NMR: 6C (100MHz, CDC13) 172.2 (lactam C=0), 142.2 (ipso-C), 136.2 (para-C), 129.7 (aromatic CH), 127.3 (aromatic CH), 53.3 (CH-CO), 42.0 (C3/4-NH), 29.6 (lactam CH2), 28.6 (lactam CH2), 27.9 (lactam CH2), 21.5 (CH3).HRMS (+ESI) C,2H16N203S + Na+: calcd 291.0774; found 291.0777.

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

Reference：
Patent; CAMBRIDGE ENTERPRISE LIMITED; FUNXIONAL THERAPEUTICS LIMITED; GRAINGER, David, John; FOX, David, John; WO2011/154695; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

138377-80-7, 3-Aminopiperidin-2-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,138377-80-7

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

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

138377-80-7, 3-Aminopiperidin-2-one hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Reference Example 11 : 3-(Pyridin-3′-carbonylamino)tetrahydropyridin-2- one:; Oxalyl chloride (20 mmol) was added to a solution of nicotinic acid (10 mmol) in DCM (40 mL), along with one drop of catalytic DMF. The reaction mixture was stirred for 16 h and then the solvent was removed under high vacuum. The resulting crystals were dissolved in DCM (10 mL). In a separate flask, 3- aminotetrahydropyridin-2-one hydrochloride (10 mmol) and 2C03 (30 mmol) were added to water (30 mL) and stirred, giving a solution to which the acid chloride solution was added. The reaction was worked-up as above to give the product (0.10 g, 5percent):Vmax cm”‘ 3257 (N-H, amide), 1642, 1541 (secondary CONH, lactam, NH), 1591 , 1479 (aromatic pyridine ring). NMR: deltaEta (400MHz, CDC13) 9.03 (I H, d, J 2.0, 2′-aryl CH), 8.71 (I H, dd, J 5.0, 1.5, 6′-aryl CH), 8.12 (I H, dt, J 8.0, 2.0, 4′-aryl CH), 7.36 (IH, dd, J 8.0, 5.0, 5’-aryl CH), 7.27 (I H, br d, J2.0, C5H4N-CONH), 5.91 (IH, br s, CONH-CH2), 4.45 (IH, dt, J 1 1.0, 5.5, CH-CO), 3.44-3.32 (2H, m, CH2NH), 2.72 (IH, dt, J 14.5, 4.5, NHCH- C 2), 2.06-1.93 (2H, m, lactam CH2), 1.70-1.54 (I H, m, lactam CH2).13C NMR: 6c (100MHz, CDC13) 171.8 (lactam C=0), 166.0 (aryl C=0), 152.5 (aryl N- CH), 148.6 (aryl N-CH), 135.3 (ortho-C(-C )), 133.4 (ipso-C), 123.6 (meta-C), 51.2 (CH-CO), 42.0 (CH2-NH), 27.3 (lactam CH2), 21.3 (lactam CH2). HRMS (+ESI) C, ,H 13N302 + H+: calcd 220.1081 ; found 220.1085., 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; CAMBRIDGE ENTERPRISE LIMITED; FUNXIONAL THERAPEUTICS LIMITED; GRAINGER, David, John; FOX, David John; WO2011/154696; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem