目的研究坎地沙坦酯的合成新方法,并对其工艺路线进行优化。方法以3-硝基邻苯二甲酸为原料,经过酯化、氯化、Curtius重排、脱Boc保护、还原、环合、水解、酯化、烃化、脱保护10步反应得到坎地沙坦酯。结果与结论该路线反应条件温和,原料廉价易得,同时避免了剧毒化合物烷基锡的使用,成本较低,总收率12.3%,适合工业化生产。 Aim To study a new method for the synthesis of candesartan cilexetil and to optimize its process route. Methods 3-nitrophthalic acid was used as starting material to obtain candesartan 10-step reaction after esterification, chlorination, Curtius rearrangement, deprotection, reduction, cyclization, hydrolysis, esterification, alkylation and deprotection. Tantalum. RESULTS AND CONCLUSION The reaction route of this route was mild and the raw materials were cheap and easily available. At the same time, the use of alkyltin, a highly toxic compound, was avoided. The cost was lower and the total yield was 12.3%. It was suitable for industrial production.