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

Abstract

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 ).