Category: 50534-49-1

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, category: piperidines, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 50534-49-1, Name is N,N-Dimethylpiperidin-3-amine, molecular formula is C7H16N2. In a Patent, authors is £¬once mentioned of 50534-49-1

Pharmaceutical compositions and methods of inhibiting gastric acid secretion

Pharmaceutical compositions and methods of inhibiting gastric acid secretion by administering 1-(9-xanthenyl) amino-substituted-piperidines and pyrrolidines and new 1-(9-xanthenyl) amino-piperidine compounds.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 50534-49-1, help many people in the next few years.category: piperidines

Reference£º
Piperidine – Wikipedia,
Piperidine | C5H3692N – PubChem

 

50534-49-1, N,N-Dimethylpiperidin-3-amine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

50534-49-1, General procedure: Compound 265a was prepared from 3-carbamoyl-l-(2-((2-((3-chloro-2-fluorobenzyl)amino)- 2-oxoethyl)(cyclopropyl)amino)-2-oxoethyl)-lH-indazole-5-carbonyl azide (235a) (400 mg, 0.38 mmol) and N,N-dimethylpiperidin-3 -amine (97 mg, 0.76 mmol) using TEA (0.21 mL, 1.52 mmol) as base according to the procedure reported in step-4 of Scheme 129. This gave after workup, purification by flash column chromatography [silica gel (12 g), eluting with DMA80 in DCM 0 to 40%] followed by preparative HPLC [Cis column, eluting with CH3CN in water (containing 0.1% TFA) 0-100%] l-(2-((2-((3-chloro-2-fluorobenzyl)amino)-2- oxoethyl)(cyclopropyl)amino)-2-oxoethyl)-5-(3-(dimethylamino)piperidine-l-carboxamido)- lH-indazole-3-carboxamide (265a) (32 mg, 0.051 mmol, 13 % yield) white solid as a TFA salt; NMR (300 MHz, DMSO-d) delta 9.60 – 9.46 (m, 1H), 8.77 (s, 1H), 8.50 (t, J= 5.8 Hz, 1H), 8.25 – 8.18 (m, 1H), 7.66 (s, 1H), 7.56 – 7.50 (m, 2H), 7.50 – 7.42 (m, 1H), 7.32 (s, 1H), 7.27 – 7.19 (m, 1H), 7.19 – 7.08 (m, 1H), 5.61 (s, 2H), 4.33 (d, J= 5.7 Hz, 2H), 4.24 (d, J = 13.0 Hz, 2H), 3.98 (s, 2H), 3.94 – 3.88 (m, 1H), 3.33 – 3.22 (m, 1H), 3.10 – 2.97 (m, 2H), 2.86 and 2.85 and 2.82 and 2.81 (4s, 6H), 2.13 – 2.03 (m, 1H), 1.86 – 1.65 (m, 2H), 1.61 – 1.39 (m, 1H), 1.03 – 0.95 (m, 2H), 0.95 – 0.85 (m, 2H);19F NMR (282 MHz, DMSO-i) delta – 73.92 (TFA peak), -121.58; MS (ES+): 627.5 (M+1). Scheme 266 A suspension of 3-acetyl-l-(2-((2-((3-chloro-2-fluorobenzyl)amino)-2- oxoethyl)(isopropyl)amino)-2-oxoethyl)-lH-indole-5-carbonyl azide (129d) (75 mg, 0.14 mmol) in THF/Tol (24 mL, Ratio: 1 :2) was heated at reflux for 4h, cooled to room temperature and concentrated in vacuum to dryness. The residue obtained was dissolved in THF (20 mL) and ACN (10 mL) followed by the addition of cyclopropanamine (16.25 mg, 0.29 mmol) and triethylamine (0.060 mu^, 0.427 mmol). The reaction mixture was stirred at room temperature overnight, diluted with EtOAc (100 mL), washed with water (3x), dried, filtered and concentrated in vacuum. The residue was purified by column chromatography [silica (12 g), eluting with CMA80 in CHCb 0 to 40%] followed by preparative HPLC with water/ ACN to give 2-(3-acetyl-5-(3-cyclopropylureido)-lH-indol-l-yl)-N-(2-((3-chloro-2- fluorobenzyl)amino)-2-oxoethyl)-N-isopropylacetamide (129e) (6 mg, 10.79 mupiiotaomicron, 6% yield) as a white solid after lyophilization; NMR (300 MHz, DMSO-de) (a mixture of two rotamers) delta 8.84 – 8.13 (m, 4H), 7.60 – 6.90 (m, 5H), 6.27 (d, J = 2.3 Hz, 1H), 5.29 and 5.11 (2s, 2H), 4.66 – 4.50 and 4.28-4.20 (2m, 1H), 4.47 (d, J = 5.4 Hz) and 4.34 (d, J = 5.8 Hz) (2d, 2H), 4.17 and 3.84 (2s, 2H), 2.40 and 2.39 (2s, 3H), 1.24 (d, J = 6.3 Hz) and 1.00 (d, J = 6.8 Hz) (2d, 6H), 0.71 – 0.55 (m, 2H), 0.50 – 0.31 (m, 2H); 19F NMR (282 MHz, DMSO-d) delta -73.45 (TFA peak), -121.20, -121.82; MS (ES+); 578.5 (M+Na); MS (ES”): 554.5 (M-l).

50534-49-1 N,N-Dimethylpiperidin-3-amine 14459854, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; BIOCRYST PHARMACEUTICALS, INC.; KOTIAN, Pravin, L.; BABU, Yarlagadda, S.; ZHANG, Weihe; VOGETI, Lakshminarayana; WU, Minwan; CHINTAREDDY, Venkat, R.; RAMAN, Krishnan; (479 pag.)WO2017/136395; (2017); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

50534-49-1, N,N-Dimethylpiperidin-3-amine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

50534-49-1, General procedure: Compound 265a was prepared from 3-carbamoyl-l-(2-((2-((3-chloro-2-fluorobenzyl)amino)- 2-oxoethyl)(cyclopropyl)amino)-2-oxoethyl)-lH-indazole-5-carbonyl azide (235a) (400 mg, 0.38 mmol) and N,N-dimethylpiperidin-3 -amine (97 mg, 0.76 mmol) using TEA (0.21 mL, 1.52 mmol) as base according to the procedure reported in step-4 of Scheme 129. This gave after workup, purification by flash column chromatography [silica gel (12 g), eluting with DMA80 in DCM 0 to 40%] followed by preparative HPLC [Cis column, eluting with CH3CN in water (containing 0.1% TFA) 0-100%] l-(2-((2-((3-chloro-2-fluorobenzyl)amino)-2- oxoethyl)(cyclopropyl)amino)-2-oxoethyl)-5-(3-(dimethylamino)piperidine-l-carboxamido)- lH-indazole-3-carboxamide (265a) (32 mg, 0.051 mmol, 13 % yield) white solid as a TFA salt; NMR (300 MHz, DMSO-d) delta 9.60 – 9.46 (m, 1H), 8.77 (s, 1H), 8.50 (t, J= 5.8 Hz, 1H), 8.25 – 8.18 (m, 1H), 7.66 (s, 1H), 7.56 – 7.50 (m, 2H), 7.50 – 7.42 (m, 1H), 7.32 (s, 1H), 7.27 – 7.19 (m, 1H), 7.19 – 7.08 (m, 1H), 5.61 (s, 2H), 4.33 (d, J= 5.7 Hz, 2H), 4.24 (d, J = 13.0 Hz, 2H), 3.98 (s, 2H), 3.94 – 3.88 (m, 1H), 3.33 – 3.22 (m, 1H), 3.10 – 2.97 (m, 2H), 2.86 and 2.85 and 2.82 and 2.81 (4s, 6H), 2.13 – 2.03 (m, 1H), 1.86 – 1.65 (m, 2H), 1.61 – 1.39 (m, 1H), 1.03 – 0.95 (m, 2H), 0.95 – 0.85 (m, 2H);19F NMR (282 MHz, DMSO-i) delta – 73.92 (TFA peak), -121.58; MS (ES+): 627.5 (M+1). Scheme 266 A suspension of 3-acetyl-l-(2-((2-((3-chloro-2-fluorobenzyl)amino)-2- oxoethyl)(isopropyl)amino)-2-oxoethyl)-lH-indole-5-carbonyl azide (129d) (75 mg, 0.14 mmol) in THF/Tol (24 mL, Ratio: 1 :2) was heated at reflux for 4h, cooled to room temperature and concentrated in vacuum to dryness. The residue obtained was dissolved in THF (20 mL) and ACN (10 mL) followed by the addition of cyclopropanamine (16.25 mg, 0.29 mmol) and triethylamine (0.060 mu^, 0.427 mmol). The reaction mixture was stirred at room temperature overnight, diluted with EtOAc (100 mL), washed with water (3x), dried, filtered and concentrated in vacuum. The residue was purified by column chromatography [silica (12 g), eluting with CMA80 in CHCb 0 to 40%] followed by preparative HPLC with water/ ACN to give 2-(3-acetyl-5-(3-cyclopropylureido)-lH-indol-l-yl)-N-(2-((3-chloro-2- fluorobenzyl)amino)-2-oxoethyl)-N-isopropylacetamide (129e) (6 mg, 10.79 mupiiotaomicron, 6% yield) as a white solid after lyophilization; NMR (300 MHz, DMSO-de) (a mixture of two rotamers) delta 8.84 – 8.13 (m, 4H), 7.60 – 6.90 (m, 5H), 6.27 (d, J = 2.3 Hz, 1H), 5.29 and 5.11 (2s, 2H), 4.66 – 4.50 and 4.28-4.20 (2m, 1H), 4.47 (d, J = 5.4 Hz) and 4.34 (d, J = 5.8 Hz) (2d, 2H), 4.17 and 3.84 (2s, 2H), 2.40 and 2.39 (2s, 3H), 1.24 (d, J = 6.3 Hz) and 1.00 (d, J = 6.8 Hz) (2d, 6H), 0.71 – 0.55 (m, 2H), 0.50 – 0.31 (m, 2H); 19F NMR (282 MHz, DMSO-d) delta -73.45 (TFA peak), -121.20, -121.82; MS (ES+); 578.5 (M+Na); MS (ES”): 554.5 (M-l).

50534-49-1 N,N-Dimethylpiperidin-3-amine 14459854, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; BIOCRYST PHARMACEUTICALS, INC.; KOTIAN, Pravin, L.; BABU, Yarlagadda, S.; ZHANG, Weihe; VOGETI, Lakshminarayana; WU, Minwan; CHINTAREDDY, Venkat, R.; RAMAN, Krishnan; (479 pag.)WO2017/136395; (2017); 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.50534-49-1,N,N-Dimethylpiperidin-3-amine,as a common compound, the synthetic route is as follows.

EXAMPLE DDD86292 2,6-Dichloro-4-[2-(3-dimethylamino-pyrrolidin-1-yl)-pyridin-4-yl]-N-(1,3,5-trimethyl-1 H-pyrazol-4-yl)-benzenesulfonamide Prepared by heating the chloropyridine of intermediate 12 (250 mg, 0.58 mmol) with 3-dimethylaminopiperidine (200 mul) in EtOH (1.5 ml) at 155 C. for 1 h according to the method of DDD86213 to give the title compound as a white powder (150 mg, 0.29 mmol, 49%). deltaH (CDCl3, 300K) 8.48 (1H, d J 5.1 Hz), 7.49 (2H, s), 7.39 (1H, d J 4.7 Hz), 7.32 (1H, s), 3.76-3.46 (6H, s br), 3.63 (3H, s), 3.46-3.39 (1H, m), 2.75 (2H, s br), 2.28 (2H, s br), 2.05 (3H, s), 1.85 (3H, s), 1.56 (2H, s br). m/z (ES+, 70V) 523.2 (MH+)., 50534-49-1

As the paragraph descriping shows that 50534-49-1 is playing an increasingly important role.

Reference£º
Patent; Brand, Stephen; Wyatt, Paul; Thompson, Stephen; Smith, Victoria; Bayliss, Tracy; Harrison, Justin; Norcross, Neil; Cleghorn, Laura; Gilbert, Ian; Brenk, Ruth; US2011/312921; (2011); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem