Methods and compositions for preparation of H-ARG-X-Z-Y-TYR-R

Claim 1

The protected tetrapeptide of formula alpha-T-X-omega-U-Z-Y-TYR-R', wherein: R' is OU or NH 2 ; X is epsilon-T"-LYS and Y is VAL or X and Y are both SAR; Z is ASP or GLU; and T and T" are each a member selected from the group consisting of: (a) ##STR19## wherein R 1 is phenyl; tolyl; xylyl; adamantyl; allyl; beta-cyanoethyl; fluorenylmethyl; benzyl, benzyl wherein the phenyl ring is substituted with from one to three members selected from halo, nitro, loweralkyl, and loweralkoxy, diisopropylmethyl; diphenylmethyl; cyclohexyl; cyclopentyl; vinyl; t-butyl; t-amyl; dimethyltrifluoromethylmethyl; or dimethylbiphenylmethyl; (b) ##STR20## wherein R 2 is loweralkyl of two to four carbons or loweralkyl of one to four carbons substituted with from one to five halo groups; (c) ##STR21## wherein V is S or O and R 3 and R 1 are each benzyl or loweralkyl; (d) ##STR22## wherein R 5 and R 6 taken individually are each loweralkyl or R 5 and R 6 taken together is ##STR23## where R 7 and R 8 are each hydrogen or loweralkyl; (e) ##STR24## wherein R 9 is hydrogen or nitro; and (f) ##STR25## wherein R 10 is hydrogen, methyl, halo, or nitro provided that T is monodentate when X is SAR; and U is benzyl or benzyl in which the phenyl group is substituted with from one to three members each selected from halo, nitro, C 1 -C 3 loweralkyl, and C 1 -C 3 loweralkoxy.