| 摘要 |
Preparation of 1-(3,4-dimethoxy-phenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine (I) involves reacting 3-[2-(3,4-dimethoxy-benzoyl)-4,5-dimethoxy-phenyl]-pentan-2-one-ketal with hydrazine, its hydrate or salt formed with an inorganic or organic acid. Preparation (M1) of 1-(3,4-dimethoxy-phenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine (I) involves reacting 3-[2-(3,4-dimethoxy-benzoyl)-4,5-dimethoxy-phenyl]-pentan-2-one-ketal of formula (II) with hydrazine, its hydrate or salt formed with an inorganic or organic acid. [Image] R 1and R 21-4C alkyl (preferably methyl or ethyl); and R 1+R 22-6C alkylene (preferably ethylene). Independent claims are also included for: (1) preparation: (a) (M2) of 3-[2-(3,4-dimethoxy-benzoyl)-4,5-dimethoxy-phenyl]-pentan-2-one (IV); (b) (M3) of compounds (VIII); (c) (M4) of compounds (II); and (2) compounds of formula (II) and (VIII). [Image]. |
