發(fā)布時間：2018-04-04 01:01

  本文選題：雷迪帕韋　切入點：丙型肝炎治療藥物　出處：《上海醫(yī)藥》2016年09期

【摘要】：乙醛酸甲酯與R(+)-α-甲基芐胺縮合、與環(huán)戊二烯通過aza-Diels Alder反應(yīng),產(chǎn)物經(jīng)氫化、上Boc保護、水解、縮合得到苯并咪唑衍生物,繼續(xù)與聯(lián)硼酸頻哪醇酯反應(yīng)得到雷迪帕韋關(guān)鍵中間體:(1R,3S,4S)-3-[6-(4,4,5,5-四甲基-1,3,2-二氧雜環(huán)戊硼烷-2-基)-1H-苯并咪唑-2-基]-2-氮雜雙環(huán)[2.2.1]庚烷-2-羧酸叔丁酯,總收率40.6%(以乙醛酸甲酯計),關(guān)鍵中間體經(jīng)過三步反應(yīng)得到雷迪帕韋丙酮合物,純度99.7%,ee值達100%。
[Abstract]:Benzimidazole derivatives were synthesized by condensation of methyl glyoxylate with R (T- 偽 -methylbenzylamine) and reaction with cyclopentadiene via aza-Diels Alder. The product was hydrogenated, protected by Boc, hydrolyzed and condensed.緇х畫涓庤仈紜奸吀棰戝摢閱囬叝鍙嶅簲寰楀埌闆瘋開甯曢煢鍏抽敭涓棿浣，

本文編號：1707683