反応 #162708

反応方程式

4-{[(1S,2R)-2-aminocyclohexyl]amino}-N-(2-methoxyethyl)-6-methylquinazolin-2-carboxamide

ethylacetoimidate hydrochloride

triethylamine

→

desired compound

収率 77.9%

4-{[(1S,2R)-2-(ethanimidoylamino)cyclohexyl]amino}-N-(2-methoxyethyl)-6-methylquinazolin-2-carboxamide

収率 77.9%

溶媒

ethanol

反応条件

後処理

1. 1
   濃縮After the reaction solution was concentrated
2. 2
   その他the residue was purified by silica gel column chromatography (chloroform:methanol=20:1)

実験手順

To a solution of 450 mg of 4-{[(1S,2R)-2-aminocyclohexyl]amino}-N-(2-methoxyethyl)-6-methylquinazolin-2-carboxamide and 467 mg of ethylacetoimidate hydrochloride in 10 ml of ethanol, 764 mg of triethylamine was added, and the mixture was stirred at 80° C. for 8 hours. After the reaction solution was concentrated, the residue was purified by silica gel column chromatography (chloroform:methanol=20:1), whereby 391 mg of a desired compound was obtained as a pale yellow powder.

出典