Nitrogen substituents introduction - in methyl and methylene gps using phosgene immonium chloride

摘要

Nitrogen-substits. are introduced into methyl or methylene gps. by reaction of 1 mole cpds. contg. keto- or carboxyl gp. activated -CH2- gps. in the molecule with 2 moles phosgene immonium chloride of formula:- (where R1 = 1-18C alkyl, pref. 1-4C alkyl). Reaction is carried out in an anhydrous medium at 0-100 degrees C, pref. 40-80 degrees C. Initially an amide chloride is obtd. which is converted by hydrolysis, alcoholysis, thiolysis or aminolysis.