Method for preparing Derivatives of Pentapeptide of Tyr ala Gly I - NH2 or Lev - NH2 (ET) - NH2 or CYS or Cys (p-methoxybenzyl)

摘要

Compounds of the formula IMAGE +TR IMAGE and pharmaceutically acceptable non-toxic acid addition salts thereof, in which L and D, when applicable, define the chirality; R1 is hydrogen, C1-C3 primary alkyl, or allyl; R2 is hydrogen or C1-C3 primary alkyl, subject to the limitation that when R1 is allyl, R2 is hydrogen; R3 is hydrogen or C1-C3 primary alkyl; R4 is C1-C4 primary or secondary alkyl; R5 is hydrogen or C1-C4 primary or secondary alkyl; R6 is hydrogen or C1-C3 primary alkyl; R7 is hydrogen or C1-C3 primary alkyl; Y is hydrogen or acetyl; Z is hydrogen of IMAGE in which R8 is C1-C3 alkyl or hydrogen; and W is isopropyl, -VR9, or -CH2-X-CH3, in which V is O or S, R9 is C1-C4 alkyl or aralkyl, and X is O, S, or -CH2-, subject to the limitation that, when W is isopropyl, R7 is C1-C3 primary alkyl; are useful analgesic agents.