PREPARATION OF FLUORINATED METHYL AMINOALKANOIC ACIDS AND NOVEL PROCESS INTERMEDIATES

摘要

Fluorinated alkenylamines of the Formula V:- and fluorinated methyl ketimine magnesium halides of the formula IV:- wherein n represents 0, 1, 2 or 3; R1 represents hydrogen or C1-C10 alkyl and Y represents (a), when n represents 0, CH2F, (b), when n represents 1, CH2F or CHF2, or (c) when n represents 2 or 3, CH2F, CHF2 or CF3 and X is chlorine, bromine or iodine, are novel process intermediates. The former are obtained by hydrolysis aid subsequent reduction of the latter compounds which result from reaction of the corresponding alkenyl magnesium halides with the corresponding fluorinated acetonitriles. The fluorinated alkenylamines of Formula V are oxidized whilst the amino group is protected to provide, after removal of the amine protecting group, the corresponding fluorinated methyl aminoalkanoic acids which are useful pharmalogical or anti-bacterial agents.