An improved industrial synthesis of florfenicol plus an enantioselective total synthesis of thiamphenicaol and florfenicol

摘要

Both thiamphenicol (1) and its 3'-fluoro derivative, florfenicol (2) are broad spectrum antibiotics possessing activity against many Gra negative and Gram positive microorganisms. The current industrial synthesis of florfenicol is based upon the established thiamphenicol process which starts with the condensation of p-(meth- ylsulfonyl)benzaldehyde (14) and glycine.