4-Aminotetrahydropyran hydrochloride → 10-bromo-N3-(tetrahydro-2H-pyran-4-yl)-6,7-dihydro-5H-5,7-methanobenzo[c]imidazo[1,2-a]azepine-2,3-dicarboxamide

関与物質

反応手順

10-bromo-2-carbamoyl-6,7-dihydro-5H-5,7-methanobenzo[c]imidazo[1,2-a]azepine-3-carboxylic acid (0.1 g) was reacted with tetrahydro-2H-pyran-4-amine hydrochloride similarly to the conditions described in Example 2 to produce 10-bromo-N3-(tetrahydro-2H-pyran-4-yl)-6,7-dihydro-5H-5,7-methanobenzo[c]imidazo[1,2-a]azepine-2,3-dicarboxamide. This intermediate was then reacted with (2R)-2-(5-methylisoxazol-3-yl)but-3-yn-2-ol via General Procedure E to afford 5.7 mg (10%) of 10-[(3R)-3-hydroxy-3-(5-methylisoxazol-3-yl)but-1-ynyl]-N3-tetrahydropyran-4-yl-5,6,7,12-tetrahydro-5,7-methanobenzo[c]imidazo[1,2-a]azepine-2,3-dicarboxamide. M+1=516.

情報源と証拠