| 摘要 |
The process for making N-(2-propinyl), N-(2-butinyl) and N-(2,3-butadienyl) derivs. of 2-amino methyl (1-methyl indole) as free bases or salts, for use as monoanivric oxidase inhibitors, consists of (a) conversion of 1-methyl indole 2-carboxylic acids to the acid chlorides pref. by reaction with PCl5; (b) reaction with ammonia or amines to give the amides; (c) redn. with lithium hydride and aluminium, pref. in THF under reflux, to the corresp. 2-amino methyl- (1-methyl indoles); and (d) reaction with 2-propinyl, 2-butinyl or 2,3-butadienyl bromide in presence of tert. butylamine.
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