Raloxifene derivative and preparation method thereof

Abstract

The invention discloses a raloxifene derivative. A molecular structural formula is shown in the description. According to the raloxifene derivative prepared by the invention, raw materials are simpleand reaction conditions are easy to realize; the yield is relatively high; no harmful substances are generated in a reaction process; the raloxifene derivative is simple in raw materials and reactionconditions.

Description

technical field [0001] The invention relates to the field of organic chemistry, in particular to a raloxifene derivative and a preparation method thereof. Background technique [0002] Raloxifene, as a selective estrogen receptor modulator and anti-tubulin agent, is mainly used to treat postmenopausal osteoporosis in women. Its derivative DRL527 was found to be a mutation-selective antagonist of ERa (E353A) and ERb (E305A). Other relevant information has also been reported, raloxifene derivatives as polymerization inhibitors and as inhibitors of acetyl-CoA carboxylase. [0003] Given their importance in medicinal chemistry, it is of great interest to chemists to develop efficient methods for the synthesis of raloxifene derivatives. The classical approach to the synthesis of raloxifene relies on intermolecular Friedel-Crafts acylation 6 , but generally suffer from several limitations in the formation of environmentally harmful HCl, poor regioselectivity and functional grou...

AI Technical Summary

Problems solved by technology

The classical approach to the synthesis of raloxifene relies on intermolecular Friedel-Crafts acylation 6 , but generally suffer from several limitations in the formation of environmentally harmful HCl, poor regioselectivity and functional group tolerance

Therefore, the synthesis of raloxifene derivatives often requires complex reaction raw materials

Images