Process of preparation of peptides and N-carbamoyl protected peptides

摘要

Prepn. of peptides of formula NH2-CHR1-CONH-CHR2-COR3 (I) comprises treating an N-carbamoyl peptide of formula R4NHCO-NH-CHR1-CONH-CHR2-COR3 (III) with a carbamoylase, opt. in the presence of solvent; or by removing the carbamoyl protecting gp. chemically, opt. in the presence of solvent and/or acid. In the formulae, R1 and R2 = H; 1-6C alkyl (opt. interrupted or substd. by the heteroatoms N,O or S, where the heteroatoms are opt. substd. by H, 1-4C alkyl or benzyl or are opt. linked to carbon by double bonds); phenyl or benzyl (both opt. substd. by halo or OH); or heteroaralkyl (such as 3-indolylmethyl or 2-, 3- or 4-pyridylmethyl); R3 = 1-4C alkoxy, NH2, OH, NR1R2, benzoyloxy (opt. substd. by 1 of more of halo, NO2, NH2, 1-4C alkyl, or 1-4C alkoxy) or one or more units of type NH-CHR2-COR3; and R4 = H, 1-4C alkyl, phenyl (opt. substd. by 1 or more of halo, 1-4C alkyl, 1-4C alkoxy, NO2, CN, CF3, 1-6C alkoxycarbonyl, COOH or NR1R2), aralkyl (such as benzyl) (opt. substd. by halo, 1-4C alkyl or 1-4C alkoxy), naphthyl or heteroaralkyl (such as (sic) 2-, 3- or 4-thienyl or -pyridyl or 2-quinolyl).