Procedure for the preparation of a new a decapeptide, its protected derivatives and its salts. (Machine-translation by Google Translate, not legally binding)

摘要

Procedure for the preparation of a new undecapeptide, its protected derivatives and its salts, especially the new undecapeptide L-pyroglutamyl-L-alanyl-L-aspartyl-L-prolyl-L-asparaginyl-L-lysyl-L-xylanil-L -tyrosyl-glycyl-L-leucyl-L-methioninamide, its protected derivatives and its non-toxic and pharmaceutically acceptable organic or inorganic acid addition salts, characterized by condensation of the pentapeptide L-phenylalanyl-L-tyrosyl-glycyl L-leucyl-L-methioninamide with the hexapeptide of L-pyroglutamyl-L-alanyl-L-aspartyl-L-prolyl-L-asparaginyl-I-lysine, in which the imino group of the pyroglutamyl radical and the group ε-amino of the lysyl radical are blocked by a protective group taken from the group consisting of trityl, tocil, phthalyl, carbobenzoxy, tertiary carbo-butoxy, trifluoroacetyl and formyl, while the β-carboxyl group of the aspartyl radical is blocked by a protecting group taken from the group const This is carried out by methyl, ethyl, tertiary butyl, benzyl and p-nitrophenyl, said condensation being carried out in the presence of a carbodiimide taken from the group consisting of dicylohexylcarbodiimide and 1-cyclohexyl-3-morpholinylethylcarbodiimide, at a temperature of -10º to 20º C and in a period of 10 to 70 hours, to form the protected undecapeptide L-pyroglutamyl-L-alanyl-L-aspartyl-L-prolyl-L-asparaginyl-L-lysyl-L-phenylalanyl-L-tyrosyl-glycyl-L -leucyl-L-methioninamide, in which the imino group of the pyroglutamyl radical, the ε -amino group of the lysyl radical and the beta-carboxyl group of the aspartyl radical are blocked by the protective groups mentioned above, and by being obtained from this undecapeptide protected, by elimination of the protective groups, in a known manner, with a splitting agent taken from the group consisting of hydrogen in the presence of palladium, sodium in liquid ammonia, anhydrous hydrogen halides in acetic acid and trifluoric acid. uoroacetic, the free undecapeptide, in the form of the addition salt of an organic or inorganic acid, from which the free undecapeptide is obtained in a known manner. (Machine-translation by Google Translate, not legally binding)