Bazedoxifene

CAT#: H120203

CAS#: 198481-32-2

Description: Bazedoxifene is a third generation selective estrogen receptor modulator (SERM), developed by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. In late 2013, Pfizer received approval for bazedoxifene as part of the combination drug DUAVEE in the prevention (not treatment) of postmenopausal osteoporosis. Bazedoxifene is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).

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Synthetic Routes

Bazedoxifene - Synthetic Route 1

Bazedoxifene route01

Synthetic reference

Mylavarapu, Ravikumar; Kondaiah, G. C. M.; Reddy, L. Amaranth; Dubey, Manoj Kumar; Jasmine; Mukkanti, Kagga; Bandichhor, Rakeshwar. An improved synthesis of Bazedoxifene acetate. Chemistry & Biology Interface. Volume 5. Issue 2. Pages 137-150. Journal; Online Computer File. (2015).

Bazedoxifene - Synthetic Route 2

Bazedoxifene route02

Synthetic reference

Shang, Yaping; Jonnada, Krishna; Yedage, Subhash Laxman; Tu, Hua; Zhang, Xiaofeng; Lou, Xin; Huang, Shijun; Su, Weiping. Rhodium(III)-catalyzed indole synthesis at room temperature using the transient oxidizing directing group strategy. Chemical Communications (Cambridge, United Kingdom). Volume 55. Issue 64. Pages 9547-9550. Journal; Online Computer File. (2019).

Bazedoxifene - Synthetic Route 3

Bazedoxifene route03

Synthetic reference

Hwang, Seong Gwan; Park, Jang Ha; Seo, Rak Seok; Choi, Seon Hui; Kim, Gyeong Deok; Kim, Dong Hwa. Method for preparation of bazedoxifene. Assignee MFC Co., Ltd., S. Korea. KR 2019110400. (2019).

Bazedoxifene - Synthetic Route 4

Bazedoxifene route04

Synthetic reference

Wu, Jianhua; Xu, Jingren; Cai, Wei; Zhu, Xiaohe; Zhang, Haibo; Lv, Huimin; Hu, Tao; Xiao, Can; Gu, Cheng; Xu, Chenjun. Process for preparation of bazedoxifene acetate. Assignee Yangtze River Pharmaceutical Group Co., Ltd., Peop. Rep. China. CN 107793344. (2018).

Bazedoxifene - Synthetic Route 5

Bazedoxifene route05

Synthetic reference

Luthra, Parven Kumar; Bhuta, Sachin; Nair, Raji; Salunke, Sanjukumar; Venkataraman, Deepak. Process for preparing novel mesylate intermediate for the synthesis of Bazedoxifene acetate. Assignee Sandoz AG, Switz. IN 2011KO00877. (2016).

Bazedoxifene - Synthetic Route 6

Bazedoxifene route06

Synthetic reference

Joshi, Shreerang; Bhuta, Sachin; Talukdar, Sanjay; Sawant, Sudhir; Venkatraman, Deepak. Process for the preparation of bazedoxifene acetate from cyanomethoxybenzyl halides. Assignee Sandoz AG, Switz. WO 2010118997. (2010).