反应 #1797555

反应方程式

ammonia

7-[2-(6-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)-ethyl]-4,5,6,7-tetrahydro-3H-azepin-2-ylamine

7-[2-(6-Phenyl-3H-imidazo[4,5-b]pyridin-2-yl)-ethyl]-4,5,6,7-tetrahydro-3H-azepin-2-ylamine

compound 1

7-[2-(6-Phenyl-3H-imidazo[4,5-b]pyridin-2-yl)-ethyl]-4,5,6,7-tetrahydro-3H-azepin-2-ylamine

N-methyl-N-(tetrahydro-furan-2-ylmethyl)-4-{2-[2-(7-thioxo-azepan-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridin-6-yl}-benzenesulfonamide

→

title compound

4-{2-[2-(7-Amino-3,4,5,6-tetrahydro-2H-azepin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridin-6-yl}-N-methyl-N-(tetrahydro-furan-2-ylmethyl)-benzenesulfonamide

溶剂

methanol

反应条件

后处理

1. 1
   其他The title compound is synthesized
2. 2
   其他Purification by flash chromatography on RP-C8 resin (eluent: acetonitrile/water 2:1 parts by volume) and lyophilization from 1.0 ml of water and 3.0 ml of dioxane

实验过程

The title compound is synthesized as described for 7-[2-(6-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)-ethyl]-4,5,6,7-tetrahydro-3H-azepin-2-ylamine (compound 1) from 114 mg of N-methyl-N-(tetrahydro-furan-2-ylmethyl)-4-{2-[2-(7-thioxo-azepan-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridin-6-yl}-benzenesulfonamide (compound A10) and 5.0 ml of methanol containing ammonia (strength: 7.0 M) at 50° C. for 64 hours. Purification by flash chromatography on RP-C8 resin (eluent: acetonitrile/water 2:1 parts by volume) and lyophilization from 1.0 ml of water and 3.0 ml of dioxane afford 14 mg of the title compound as an amorphous, colorless solid of m.p. 260° C. ESI-MS: 511.4 (MH+). TLC: Rf=0.17 (HPTLC RP-C18, acetonitrile/water 2:1 parts by volume).

来源