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目的 合成三尖杉碱吲哚类似物。方法 以色胺为原料经缩合、环合、水解与脱羧反应得吲哚哌啶酮化合物 ,经Bischler Napieralski反应得烯胺。通过烯胺的溴化与氧化 重排反应得到吲哚氮杂化合物。用溴苄与吲哚氮杂反应在吲哚环上引入苄基保护基 ,经还原、环合反应合成了三尖杉碱吲哚类似物。结果 经 10步反应合成了三尖杉碱吲哚类似物。总收率 14.3%。结论 合成得三尖杉碱吲哚类似物 ,并对反应作了改进 ,使收率提高 ,副产物减少。
OBJECTIVE: To synthesize the homocapral indole analogues. Methods The tryptamine was used as the starting material to synthesize indole piperidone via condensation, cyclization, hydrolysis and decarboxylation, and enamine was obtained by Bischler Napieralski reaction. Indole azepine compounds are obtained by the bromination and oxidative rearrangement of enamines. The benzyl protecting group was introduced into the indole ring by the reaction of benzyl bromide and indole azepine. The homologue of the homocapral indole was synthesized by reduction and cyclization reaction. Results Cephaloin indole analogs were synthesized in 10 steps. The total yield of 14.3%. Conclusion The indole analogs of ciphalosaccin were synthesized and the reaction was improved, the yield was increased and the by-products were reduced.