C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
530/7.26
C07C 103/52 (1980.01)
Patent
CA 1040623
DERIVATIVES OF RETRO-ENANTIO-SOMATOSTATlN. INTERMEDIATES THEREFOR,AND PROCESS THEREFOR Abstract of the Disclosure Compounds of the formula I or Ia Image (I.) Image (Ia.) in which R is hydrogen or CONHCH2CONHCH2CH3 are disclosed. The compounds are obtained by a process which comprises the following step: preparing peptide fragments II, III, V and VII see below, by a series of condensations involving the reaction of an appropriately protected peptide having an activated ester group with an appropriately protected peptide having a free amino group; condensing Image (II) by means of the azide method with Image (III) followed by hydrogenolysis of the reaction product to obtain Image (IV), condensing the latter by means of the azide method with Image (V) followed by treating the resulting compound with hydrazine hydrate to obtain Image (VI), condensing the latter by means of the azide method with -1- HNH?HCH2STrt (VII) in which R is hydrogen or CONHCH2CONHCH2CH3 to obtain the linear protected peptide Image (VIII) in which R is as defined herein; thereafter said linear peptide is transformed into the desired cyclic peptide of formula I by deprotecting and oxidizing processes. In addition, the linear, reduced form of the peptide of formula Ia is obtained by deprotection of the aforementioned linear peptide or by reduction of the cyclic peptide. The peptides of formulae I and Ia are useful for the management of diabetes and the treatment of acromegaly. Methods for their use are also disclosed. -2-
234424
Abraham Nedumparambil A.
Immer Hans U.
Nelson Verner R.
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