论文部分内容阅读
改进并建立了以4-二甲氨基吡啶(DMAP)-对甲苯磺酸盐为催化剂,二环己基碳酰亚胺(DCC)为缩合剂直接用13-cis-维A酸与醇、酚或胺合成13-cis-维A酰衍生物的方法。合成了8种新目标化合物,收率80%～95%,核磁共振氢谱和碳谱研究表明,13-cis-维A酰部分的构型均保持不变。合成方法彻底抑制了反应中N-异维A酰基脲的副反应,而且反应条件温和,对于极易异构化的13c-is-维A酸的酯化和酰胺化反应十分有利。
In this paper, we improved and established a new method for the synthesis of 4-dimethylaminopyridine (DMAP) -p-toluenesulfonate with dicyclohexylcarbodiimide (DCC) as condensing agent and 13-cis- Amine Synthesis of 13-cis-retinoic acid derivatives. Eight novel target compounds were synthesized in 80% ~ 95% yield. The results of 1H-NMR and C-NMR showed that the configuration of 13-cis-retinyl acyl moiety remained unchanged. The synthesis method completely inhibits the side reaction of the N-iso-A acylurea in the reaction, and the reaction conditions are mild, and is very favorable for the esterification and amidation reaction of the easily isomerized 13c-is-retinoic acid.