摘要 |
<p>Compounds of the formula <FORM:1071349/C2/1> in which the abbreviations represent the amino-acids in their L-configuration, R is H, methyl, isopropyl, 1-methylpropyl, 2-methylpropyl, methoxymethyl or benzyloxymethyl and X is -Tyr- or -Tyr-Pro-, are prepared by condensing a decapeptide of the formula <FORM:1071349/C2/2> with a trideca- or a tetradeca-peptide of the formula <FORM:1071349/C2/3> in which BOC is a tertiary butoxycarbonyl group, B is a tertiary butyl group and A represents an anion, and subsequently removing the protecting groups. BOC - Gly - Tyr - Ser - Met - Glu(OBu) - His-Phe-Arg-Try-Gly-OH is prepared by condensing BOC-Gly-OH and H-Tyr-Ser-OCH3 to form BOC-Gly-Tyr-Ser-OCH3, then forming BOC-Gly-Tyr-Ser-MetOCH3 and the hydriazide before converting this to the azide and condensing it with the appropriate hexapeptide. BOC-Ser(OB3)-Tyr-Ser-OCA3 is similarly prepared. Pharmaceutical compositions having ACTH activity comprise the tricosa- and tetracosapeptides of the invention together with a suitable carrier.</p> |