84541-38-8Relevant articles and documents
Preparation method of raloxifene hydrochloride and intermediate thereof
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, (2020/06/02)
The preparation method comprises the following steps: preparing a raloxifene hydrochloride precursor (intermediate 2) from 1-{4-[2-(piperidine-1-yl)ethyoxyl]phenyl}-2-(2-sulfydryl-4-methoxyphenyl)ethanone (intermediate 1) and 4-methoxybenzoyl halide, performing demethylation protection, and preparing raloxifene hydrochloride from the demethylated raloxifene hydrochloride precursor and hydrochloricacid. Herein, the intermediate 1 is generated by removing benzyl protection from an intermediate 3 (1-{4-[2-(piperidine-1-yl)ethoxy]phenyl}-2-(2-benzylthio-4-methoxyphenyl)ethanone) in trifluoroacetic acid through a reaction; (3-methoxyphenyl) benzyl sulfide is oxidized to generate a sulfoxide compound, and then the sulfoxide compound reacts with 1-[2-(4-ethynylphenoxy)ethyl]piperidine to generate an intermediate 3. The method has the advantages of mild reaction conditions, few side reactions, high yield, cheap reagent raw materials, easy recovery and easy preparation, and is suitable for industrial large-scale production.
A pizotifen derivative and its preparation method (by machine translation)
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Paragraph 0048-0050; 0058; 0060; 0070-0073; 0078-0079, (2019/02/25)
The invention discloses a pizotifen derivatives, its molecular formula is The preparation of the pizotifen derivatives raw materials used is simple, its reaction condition is easy to reach, and has a higher yield, in the reaction process also will not produce harmful substances, is a raw material and the reaction conditions are simple pizotifen derivatives. (by machine translation)
Direct synthesis of 3-acylbenzothiophenes: Via the radical cyclization of 2-alkynylthioanisoles with α-oxocarboxylic acids
Liu, Wei,Hu, Yao-Qian,Hong, Xiao-Yi,Li, Guo-Xing,Huang, Xiao-Bo,Gao, Wen-Xia,Liu, Miao-Chang,Xia, Yuanzhi,Zhou, Yun-Bing,Wu, Hua-Yue
, p. 14148 - 14151 (2019/01/03)
A radical cascade cyclization of 2-alkynylthioanisoles with α-oxocarboxylic acids with AgNO3 has been described. This reaction provides a novel route to directly access 3-acylbenzothiophenes from simple chemical feedstocks. In particular, the utility of the approach was demonstrated by its application to the synthesis of a polymerization inhibitor and a raloxifene precursor.