ANALOGS OF CARBOXY-TERMINAL OCTAPEPTIDE (B-23-B-30) OF A HUMAN INSULIN CHAIN WITH A MODIFICATION IN POSITIONS B-24 AND B-25

摘要

The synthetic analogues of the carboxyterminal sequence of the B-chain of human insulin with a variation of amino acids in position B-24 and/or in position B-25 of the general formula:Gly-X-Y-Tyr-Thr-Pro-Lys-Thr23 24 25 26 27 28 29 30whereX is D-Phe Y is D-Phe (substance I)X is L-Phe Y is L-p-MePhe (substance II)X is L-Phe Y is D-p-MePhe (substance III)X is L-Phe Y is L-p-EtPhe (substance IV)X is L-Phe Y is D-p-EtPhe (substance V)X is L-p-MePhe is L- Phe (substance VI)X is D-p-MePhe Y is L- Phe (substance VII)X is L-p-EtPhe Y is L- Phe (substance VIII)X is D-p-EtPhe Y is L- Phe (substance IX)The substances are prepared by synthesis on a solid phase using the Boc/Biz protective strategy from the hydroxylbenztriazolic esters of individual amino acids whose possible side hydroxyls are protected, the hydroxyl of tyrosine by the 2.5-dichlorobenzyloxycarbonyl group, and the hydroxyl of threonine by the benzyl group.