A process for preparing (R) -3- (2-deoxy-erythro-pen d-to-furanosyl) -3,6,7,8-tetrahydroimidazol-diazepin-4.5 to 1.3-8-ol.

摘要

2-Amino-1-(5-amino-1H-imidazol-4-yl)ethanone, 6,7dihytroimidazo¢4,5-d!¢1,3!diazepin-8(3H)-one and acid-addition salts thereof are disclosed. 2-Amino-1-(5-amino-1H-imidazol-4-yl)ethanone and its acid-addition salts are prepared by catalytically reducing an acid-addition salt of 2-amino-1-¢5-amino-1-(protected)-1H-imidazol-4-yl!ethanone. 6,7-Dihydro-imidazo¢4,5-d!¢1,3!diazepin-8(3H)-one and its acid-addition salts are prepared by reacting an acid-addition salt of 2amino-1-(5-amino-1H-imidazol-4-yl)ethanone with a compound able to contribute a formyl group. The later product may subsequently be converted into (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo¢4,5-d!¢1,3!diazepin-8-ol. Furanose derivatives of 6,7-dihydroimidazo¢4,5-d!¢1,3!-diazepine are also disclosed and their methods of preparation Lastly, a method for resolvlng an isomer mixture of 3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo- ¢4,5-d!¢1,3!diazepin-8-ol compounds is related.