Prepn. of substd. glycinamide derivs. - by reacting substd. acetonitrile with 3,3-penta:methylene oxaziridine in the presence of an auxiliary base

摘要

The prepn. of substd. glycinamide derivs. of formula (I) and their salts and derivs., esp. their N-cyclohexylidene derivs. of formula (II) comprises reacting substd. ethanonitrile derivs. of formula (III) with 3,3-pentamethylene oxaziridine formula (IV) in the presence of an auxiliary base. In the formula, R1 and R2 = each alkyl, cycloalkyl, aralkyl, aryl, hetaryl, each opt. substd. H, NH2, or CONR3R4; R3 and R4 = each H, aryl, alkyl or together form a ring system. USE/ADVANTAGE - (I) and (II) are amino acid derivs. which can be used in the construction or modification of cpds. with biological activity. Eg amino malonic acid diamides. The many variations of substituents R1 and R2 enable various properties e.g. hydrophilia to be built into the end prod. The starting materials IV is simple, relatively cheap and is not dangerous to work with.