New synthetic method of bazedoxifene

A synthetic method and chemical formula technology, applied in the field of drug synthesis, can solve the problems of increasing the difficulty of purification of final products, increasing the cost of synthesis, and increasing the amount of starting materials, so as to improve the overall conversion rate, shorten the reaction steps, and mild reaction conditions Effect
CN102690225BActive Publication Date: 2014-12-24南京正济医药销售有限公司
12 Cites 2 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
南京正济医药销售有限公司
Publication Date
2014-12-24

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention discloses a new synthetic method of bazedoxifene. Bazedoxifene is prepared by the steps of bromination, substitution, reductive amination, substitution, cyclization, deprotection, and the like of azepane which is selected as a raw material. The synthetic method of the invention has the advantages of mild reaction conditions, simple and convenient operating process, easily obtained reagent, and low cost.
Need to check novelty before this filing date? Find Prior Art

Description

(1) Technical field

[0001] The invention belongs to the technical field of medicine synthesis, in particular, the invention relates to a synthesis method of bazedoxifene, a medicine for treating postmenopausal women's osteoporosis. (2) Technical background

[0002] Bazedoxifene, English name Bazedoxifene, is an indole derivative, its chemical name is 1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4 -hydroxyphenyl)-3-methyl-1H-indole-5-ol. Its chemical structural formula is as follows:

[0003]

[0004] Bazedoxifene, originally developed by Wyeth, is a third-generation selective estrogen receptor modulator. Launched in Italy and Spain in April 2009, the trade name is Conbriza, which is used to treat osteoporosis in postmenopausal women.

[0005] There are mainly two synthetic methods of bazedoxifene reported in the literature at present.

[0006] 1. EP0802183, JP1998036346, and US5998402 use p-hydroxybenzyl alcohol as the starting material to be replaced by ethyl bromoacetate,...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More