Liao Qing-jiang
2003
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Journal
Chinese Journal of Medicinal Chemistry
Abstract
Aim To synthesize 6-methoxy-2-(4-methoxyphenyl)benzothiophene which is an important intermediate for synthesis of raloxifene hydrochloride.Method The target compound was synthesized through bromination and thioetherification from 4-methoxyacetophenone as a starting material.Then polyphosphoric acid(PPA) was used as a catalyst for the cyclization-rearrangement reaction.Results and Conclusion Three isomers accompanied by the target compound were isolated from the mother liquor and their chemical structures were confirmed by IR, 1H-NMR and HRMS.After using methanesulfonic acid as a catalyst instead of PPA,the yield of the target compound was increased in this improved synthesis.