Somatostatin, derivatives thereof, and process therefor

Details Somatostatin, derivatives thereof, and process therefor Somatostatin, derivatives thereof, and process therefor

C - Chemistry, Metallurgy

07

C

530/7.26

C07C 103/52 (1980.01)

Patent

CA 1047028

SOMATOSTATIN DERIVATIVE OF SOMATOSTATIN AND PROCESS THEREFOR Abstract of the Disclosure Compounds of the formula 1 or 1a Image (1) Image (1a) in which R1 is hydrogen or amino and R2 is hydrogen or carboxyl are disclosed. The compound of formula 1 and 1a in which R1 is NH2 and R2 is COOH is the hormone "somatostatin" and its linear form, respectively; derivatives thereof in which the Lys group (i.e.,L-Lys group) is replaced with a D-Lys group are disclosed as well. The compounds of formulae 1 and 1a are obtained by a process comprising the preparation of a first heptapeptide derivative of formula Image in which R3 is hydrogen or Boc-NH- and .alpha. is Acm or Trt,and the preparation of a second heptapeptide derivative of formula Image Image in which R2 is as defined herein, .beta. is Acm or Trt, and .gamma., .gamma.1 and .gamma.2 are either all hydrogen or all Bu+. Said first and second heptapeptide derivatives are obtained from smaller peptides by a series of condensations involving the reaction of an appropriately protected peptide unit having an activated carboxylic ester with an appropriately protected peptide having a free amino group. Subsequently the first and second heptapeptide derivatives are condensed according to the azide method to obtain the linear tetradecapeptide derivative of formula - 1 - Image in which R2,R3,.alpha.,.beta.,.gamma.,.gamma.1, and .gamma.2 are as defined herein; there- after the linear tetradecapeptide derivative is transformed into the desired tetradecapeptide of formula 1 by oxidizing and deprotecting processes. The linear, reduced form of the tetra- decapeptides of this invention (i.e. the compounds of formula 1a) are obtained by deprotection of the aforementioned linear tetra- decapeptide derivative or by reduction of the tetradecapeptide derivatives of formula 1. The compounds of formulae 1 and 1a are useful for management of juvenile diabetes and the treatment of acromegaly and methods for their use are disclosed. - 2 -

301445

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