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目的:优化合成路线并合成小分子CCR5拮抗剂TAK-779。方法:该优化后的合成路线以溴苯为起始原料,经傅克酰基化、还原、环合等反应得到目标化合物TAK-779。结果与结论:目标化合物和中间体的结构经1H-NMR和FAB-MS确证。该路线优化了合成工艺,合成TAK-779总收率为17.3%。该路线收率高,原料易得,成本低廉,操作简单。
OBJECTIVE: To optimize the synthetic route and synthesize the small molecule CCR5 antagonist TAK-779. Methods: The optimized synthesis route used bromobenzene as the starting material, and the target compound TAK-779 was obtained by Friedel-Crafts acylation, reduction and cyclization. RESULTS AND CONCLUSION: The structures of target compounds and intermediates were confirmed by 1H-NMR and FAB-MS. The route optimizes the synthesis process and the total yield of synthetic TAK-779 is 17.3%. The route yield high, raw materials easily available, low cost, easy to operate.