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缩胆囊素是肽类激素 ,在消化道和神经传导方面起重要作用。许多非肽类物质与缩胆囊素受体也有很强的亲合力 ,成为人们感兴趣的研究课题。该文用四氢嘧啶酮环系替代吡咯环 ,设计合成了非肽缩胆囊素拮抗剂 (+)RP6 6 80 3的类似物。合成反应以天冬酰胺叔丁酯为起始原料 ,先与苯甲醛形成亚胺 ,再与甘氨酸酰氯发生环化缩合 ,生成中间体 3-苯基 - 4-氨甲基羰基 - 5 -叔丁氧羰基四氢嘧啶酮 ,最后与间甲苯异氰酸酯反应 ,即得目标产物。以天冬酰胺叔丁酯计总收率为 42 %。
Cholecystokinin is a peptide hormone that plays an important role in the digestive tract and nerve conduction. Many non-peptide substances and cholecystokinin receptor also has a strong affinity, has become an interesting research topic. In this paper, the pyrrole ring was replaced by tetrahydropyrimidone ring system, and the analog of non-peptide cholecystokinin antagonist (+) RP6 6 803 was designed and synthesized. Synthesis of asparagine tert-butyl ester as the starting material, first with benzaldehyde to form imine, and glycine acid chloride cyclization condensation, resulting in the intermediate 3-phenyl - 4 - aminomethylcarbonyl - 5 - tert-butyl Oxycarbonyl tetrahydropyrimidone, and finally with m-toluene isocyanate reaction, the desired product. The total yield of asparagine t-butyl ester was 42%.