依普利酮的合成路线及参考文献? 依普利酮是一种高血压药物,属于高选择性醛酮受体拮抗剂。它通过竞争性抑制醛固酮与盐皮质激素受体结合,从而降低血压。 合成路线1 参考文献: Ng JS, Wang PT, et al. 2001. Processes for preparation of 9,11-epoxy steroids and intermediates useful therein. US 6180780 参考文献: Ng JS, Wang PT, et al. 2001. Processes for preparation of 9,11-epoxy steroids and intermediates useful therein. US 6180780 合成路线2 参考文献: Ng JS, Wang PT, et al. 2001. Processes for preparation of 9,11-epoxy steroids and intermediates useful therein. US 6180780 合成路线3 参考文献: Wuts PGML 2004. Processes for preparing 7-carboxy substituted steroids. US 2004087562 合成路线4 参考文献: Wuts PGM 2004. Processes for preparing 7-carboxy substituted steroids. US 2004087562 合成路线5 依普利酮合成的主要难点在于引入carbomethoxy取代基。下面是由Pharmacia&Upjohn制药厂开发的合成路线,通过furylation引入carbomethoxy取代基。 参考文献: Wuts PGM 2004. Processes for preparing C-7 substituted steroids. US 2004097475 合成路线6 参考文献 Pearloan BA, Padilla AG, et al. 2006. A new approach to the furan degradation problem involving oconoly-sis of the trans enediope and its use in cost-effective synthesis of eplerenone Org Lett, 8: 2111~2113 其他有关依普利酮合成的文献: Ng JS, Liu C, et al. 1998. Processes for preparation of 9,11-epoxy steroids and their intermediates. WO 9825948 Ng JS, Wang PT, et al. 1997. Preparation of 7-carboxyl-9,11-epoxy steroids and intermediates useful therein and a general process for the epoxidation of olefinic double bonds. WO 9721720 Wang S, Li J, et al. 2006. Synthesis of eplerenone from 11β-hydroxycanrenone. 发明专利申请公开说明书, CN 1749266 Wiecrorek JJ, Maisto KD, et al. 2005. An improved process for the preparation of 9,11-epoxy steroids. WO 2005092913 Ye W, Lu C, et al. 2006. Preparation of methyl 9α,11α-epoxy-17β-hydroxy 3-oxo-pregn-4-ene-7,21-di-carboxylate electone (eplerenone). 发明专利中请公开说明书, CN 1724557 来源:博普智库 查看更多