| 摘要 |
<p>An improvement is described in the synthesis method for N< alpha >-trityl-N<G>-trityl-arginine within a process for preparing N< alpha >-fluorenylmethoxycarbonyl-N<G>-trityl-arginine from arginine, comprising: a) forming N< alpha >-trityl-N<G>-trityl-arginine b) selectively detaching the trityl group from the alpha -NH2 and c) introducing the fluorenylmethoxycarbonyl group in its place. The improvement consists of preparing the N< alpha >-trityl-N<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< alpha >-fluorenylmethoxycarbonyl-N<G>-di-trityl-arginine. This new compound, to which the present invention also relates, can also be used as such in peptide synthesis.</p> |
