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Syntheses of carbon-14 labelled AJ-9677, a specific β3-adrenoceptor agonist

✍ Scribed by Takeshi Ochi; Hiroshi Toda; Akira Minamida; Yoshiaki Terauchi; Toshihiko Fujii

Publisher: John Wiley and Sons
Year: 2004
Tongue: French
Weight: 123 KB
Volume: 47
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.821

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✦ Synopsis

Abstract

Two ^14^C‐labelled versions of AJ‐9677, a novel anti‐diabetic drug candidate, have been synthesized. The first, [acetic acid‐2‐^14^C]AJ‐9677, was synthesized via a four‐step process starting from 2‐chloro‐N,N‐diethyl[2‐^14^C]acetamide (3), and the second, [hydroxymethine‐^14^C]AJ‐9677, by a two step process from (R)‐3‐chloro[7‐^14^C]styrene oxide (8). When stored in the solid state both compounds undergo radiolytic decomposition in a similar manner, despite the labelled position being different, to give the dechlorinated derivative (12a, 12b). Purification of the required product was achieved after derivatization to the methyl esters. Copyright © 2004 John Wiley & Sons, Ltd.

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