Affiliation:
1. School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing 211816, P.R. China
Abstract
The lymphocyte function-associated antigen-1 (LFA-1) antagonist of ‘Compound 4’ was synthesised by a convenient route using cheap, commercially available starting materials and catalysts under mild reaction conditions and by easily handled reactions. The total yield in the preparation of ‘Compound 4’ was more than 38% via Sonogashira coupling of an iodide and an alkyne, reduction of the alkyne catalysed by Raney nickel and later steps involving hydrolysis of an ester, condensation of an acid and an amine and a final hydrolysis of an ester.