Tetrahedron letters

Effective lithiation of 3-bromopyridine: synthesis of 3-pyridine boronic acid and variously 3-substituted pyridines

D Cai, RD Larsen, PJ Reider

Index: Cai, Dongwei; Larsen, Robert D; Reider, Paul J Tetrahedron Letters, 2002 , vol. 43, # 23 p. 4285 - 4287

Full Text: HTML

Citation Number: 62

Abstract

Substituted pyridines are important components of drug candidates. Recently, we required 3-pyridine boronic acid (1) as an intermediate in a Suzuki cross-coupling. Although the compound is commercially available, it is expensive (>$100/g) and often only small quantities can be obtained. Herein, we describe an improved process for the lithiation of 3-bromopyridine and the preparation of 3-pyridine boronic acid, which is capable of producing kilogram ...