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N-苄氧羰基-D-脯氨酸(2)经酰氯化反应制得N-苄氧羰基-D-脯氨酰氯(3),在三氯化铝催化下与5-溴吲哚经傅-克酰化反应制得(R)-3-(N-苄氧羰基吡咯烷-2-基甲酰基)-5-溴-1H-吲哚(5),再经二氢-双(2-甲氧基乙氧基)铝酸钠(SDMA)还原,得依立曲坦中间体(R)-5-溴-3-(N-甲基吡咯烷-2-基甲基)-1H-吲哚,总收率约41.5%(以2计)。
N-benzyloxycarbonyl-D-proline (2) N-benzyloxycarbonyl-D-prolyl chloride (3) is obtained by the acid chlorination reaction and reacted with 5-bromoindole under the catalysis of aluminum trichloride (5) by carboylation to give (R) -3- (N-benzyloxycarbonylpyrrolidine-2-carbonyl) -5-bromo- Methoxyethoxy) sodium aluminate (SDMA) to afford ertattran intermediate (R) -5-bromo-3- (N-methylpyrrolidin-2- ylmethyl) The overall yield is about 41.5% (in 2).