𝔖 Bobbio Scriptorium
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A chemical probe for the estrogen receptor: Synthesis of the 3H-isotopomer of raloxifene

✍ Scribed by Jeffrey A. Dodge; Mark G. Stocksdale; C. David Jones

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
360 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

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 catalyzed halogen‐tritium exchange provided the target compound with a specific activity of 30.1 Ci/mmol.

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