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目的改进G蛋白偶联受体119(GPR119)激动剂MBX-2982的合成工艺。方法以4-氰基哌啶-1-甲酸叔丁酯为起始原料,经过硫代、缩合、醚化、脱Boc保护以及取代反应制得MBX-2982。结果与结论经5步反应合成目标化合物MBX-2982,其结构经1H-NMR及MS谱确证。对多步反应条件进行了工艺考察及优化,总收率为42.8%(以4-氰基哌啶-1-甲酸叔丁酯计),高于文献收率(30.8%)。
Objective To improve the synthesis of G protein - coupled receptor 119 (GPR119) agonist MBX - 2982. Methods Starting from tert-butyl 4-cyanopiperidine-1-carboxylate, MBX-2982 was prepared by thio, condensation, etherification, deprotection and substitution reaction. Results and Conclusion The target compound MBX-2982 was synthesized via 5 steps and its structure was confirmed by 1H-NMR and MS spectra. The process conditions were optimized and investigated. The overall yield was 42.8% (based on tert-butyl 4-cyanopiperidine-1-carboxylate), higher than the literature yield (30.8%).