| 摘要 |
The invention comprises 12-methylmercaptodeserpidine of m.pt 220-222 DEG C., and a process for its preparation wherein the methyl ester of 2 - b - carbomethoxy - 3 - a - methoxy - 4 - b - acetoxy - 6 - b - formyl - cyclohexylacetic acid is condensed with 7-methylmercapto-tryptamine, the Schiff's base formed is reduced with sodium borohydride in methanol giving simultaneous cyclization of the lactum ring and deacetylation; the thus formed methyl ester of 2,3-seco-3-oxo-12-methylmercapto deserpidic acid is esterified with 3,4,5-trimethoxybenzoyl chloride in pyridine (giving 2,3-seco-3-oxo-12-methylmercapto deserpidine) and cyclized by heating with phosphorus oxychloride; the 3,4-dehydro - 12 - methylmercapto deserpidine obtained is then converted to a quaternary salt such as the perchlorate and reduced with zinc in the presence of a strong acid. |
