Synthesis of (+)-ambrisentan / 中国药科大学学报

ABSTRACT

A five-step synthetic method of ambrisentan starting from benzophenone was developed.The reaction methods of resolution and substitution were optimized.A stable,facilitating method of detection and efficient resolution reagent,L-phenylglycinamide,was used and helped to obtain highly optical pure intermediates.In the substitution reaction,NaOH was chosen as the base,which is safe and suitable for the industry.This method was mild,easily operated with a total yield up to 31.0％,and may have a good application prospect.