1236156-65-2Relevant academic research and scientific papers
Preparation method of candesartan cilexetil and intermediate of candesartan cilexetil
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Paragraph 0025; 0027; 0029; 0031, (2019/08/01)
The invention relates to a preparation method of candesartan cilexetil and an intermediate of the candesartan cilexetil. The intermediate is hydrogenated to remove benzyloxycarbonyl and triphenylmethyl protecting groups in the presence of Pd/C, and nitro is reduced to amino, so that the 'one-pot multi-step' operation is realized, no acid is needed during deprotection, side-chain cyclohexyl carbonate degradation is avoided, the product purity is high, and the candesartan cilexetil is prepared by cyclization. According to the preparation method of candesartan cilexetil and the intermediate of the candesartan cilexetil disclosed by the invention, the problems in the prior art that side chains are degraded when common t-butyloxycarboryl protecting groups on amino are removed under strong acidconditions and triphenylmethyl protecting groups on tetrazole are transferred to amino are solved.
Novel and practical synthesis of candesartan cilexetil
Mao, Yongjun,Xiong, Ruisheng,Liu, Zheng,Li, Haihong,Shen, Jingkang,Shen, Jingshan
experimental part, p. 1503 - 1508 (2010/12/24)
A novel and convergent synthetic route of candesartan cilexetil (API of Atacand), an effective angiotensin II receptor blocker, is described. Cleavage of the N-Boc and N-trityl protective group are implemented simultaneously and formation of the benzimidazole ring is conducted at the last step of this route, which gives candesartan cilexetil in 55% yield over six steps with 99.1% purity (HPLC).
