Peptide prodn - in the presence of 1-hydroxybenzotriazole

摘要

Peptides are prepd. at greatly accelerated reaction rates by reacting a protected amino acid or peptide of formula (I): (where X is an amino-protecting gp or pyroglutamyl, Y is lower alkyl opt. substd. by opt. protected OH, SH, NH2, COOH, CONH2, guanidino, aryl, imidazolyl or indolyl, or -NH-CHY- can also be pyrrotidinyl, R is halogen or NO2, n = 1-5 and m = 0-10) with an opt. protected amino acid or peptide of formula (II): H2N-CHY-CO(NH-CHY-CO)-m2 W (where m2 = 0-500, W is OH, alkoxy, aralkoxy or amino opt. substd. by alkyl, aralkyl or aryl), in the presence of =0.1 equiv. of 1-hydroxybenzotriazole, and opt. partly or entirely removing protecting gps. from the product of formula: X(NH-CHY-CO)m1 NH-CHY-CO-NH-CHY-CO(NH-CHY-CO)m2 W