Metal salts induced improved α-hydroxylation of ketones for the preparation of the key chiral intermediate of azole antifungals

Article abstract of DOI:10.1016/S0957-4166(97)00403-5

The first example demonstrating the influence of metal salts for an improved synthesis of 2',4'-difluoro-(R)-2-hydroxypropiophenone, (2), a key intermediate for the preparation of azole antifungals such as Sch 42427 (1) in excellent enantiomeric excess and high chemical yield via the use of camphorsulfonyloxaziridines is described.