Process for the synthesis of N.sup..alpha. -fluorenylmethoxycarbonyl-N.sup.G trityl-arginine
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United States of America Patent
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Jul 14, 1992
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N/A
app pub date -
May 28, 1991
filing date -
Dec 23, 1988
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Expired
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Abstract
An improvement is described in the synthesis method for N.sup..alpha. -trityl-N.sup.G -trityl arginine within a process for preparing N.sup..alpha. -fluorenylmethoxycarbonyl-N.sup.G -trityl-arginine from arginine, comprising: a) forming N.sup..alpha. -trityl-N.sup.G -trityl-arginine b) selectively detaching the trityl group from the .alpha.-NH.sub.2 and c) introducing the fluorenylmethoxycarbonyl group in its place. The improvement consists of preparing the N.sup..alpha. -trityl-N.sup.G -trityl-arginine by solubilizing the arginine in an aprotic organic solvent by tri-alkylsilylation both of the amino nitrogen and of the carboxyl group, followed by tritylation, with trityl chloride, of the .alpha.-amino nitrogen, and of the guanidino group after deprotonating this latter with a bicyclic guanidine. The new improved process can also lead to variable quantities of the arginine analogue di-tritylated at the guanidino group, namely N.sup..alpha. -fluorenylmethoxycarbonyl-N.sup.G -di-trityl-arginine. This new compound, to which the present invention also relates, can also be used as such in peptide synthesis.
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