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A simple and high-yield synthesis of (S)-BZM, (R)-BZM AND (S)-IBZM for the preparation of (S)-123I-IBZM

✍ Scribed by M. Bobeldijk; N. P. L. G. Verhoeff; J. A. J. M. Vekemans; H. M. Buck; P. A. P. M. Van Doremalen; J. J. Van Hoof; A. G. M. Janssen

Publisher
John Wiley and Sons
Year
1990
Tongue
French
Weight
358 KB
Volume
28
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

(S)‐2‐Hydroxy‐6‐methoxy‐N‐[(1‐ethyl‐2‐pyrrolidinyl)methyl]benzamide ((S)‐BZM; (S)‐5a), the precursor of (S)‐2‐hydroxy‐3‐^123^I‐iodo‐6‐methoxy‐N‐[(1‐ethyl‐2‐pyrrolidinyl)methyl]benzamide ((S)‐^123^I‐IBZM) was synthesized via a simple method and in high yield starting from 2,6‐dimethoxybenzoic acid (1a). N‐Hydroxysuccinimide/dicyclohexyl‐carbodiimide (DCC) was used as activating system in the reaction of 1a with (S)‐2‐aminomethyl‐1‐ethylpyrrolidine (3a).

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