A chemical probe for the estrogen receptor: Synthesis of the 3H??isotopomer of raloxifene

JA Dodge, MG Stocksdale…

Index: Dodge; Stocksdale; Jones Journal of Labelled Compounds and Radiopharmaceuticals, 1995 , vol. 36, # 1 p. 43 - 49

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Citation Number: 4

Abstract

Abstract Radiolabelled raloxifene (LY156758) has been prepared by tritium gas hydrogenolysis of a 3-aroyl-bis-brominated precursor. The requisite halogenated intermediate was accessed by regioselective aroylation of benzothiophene 6 with the acid chloride of 3, 5-dibromo-4-[2-(1-piperdinyl) ethoxy] benzoic acid (5). Selective deprotection of the aryl methyl ethers in the presence of the ethoxy side-chain followed by palladium ...