1159680-21-3Relevant articles and documents
Preparation method of eptifibatide key raw material L-higher arginine
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, (2021/02/20)
The invention discloses a preparation method of an eptifibatide key raw material L-higher arginine, and belongs to the field of synthesis of medical intermediates. The preparation method comprises thefollowing steps: reacting 1,3-bis(tert-butyloxycarbonyl)guanidine with p-toluenesulfonyl chloride to obtain 1,3-bis-Boc-2-(p-toluenesulfonyl)guanidine, then reacting the 1,3-bis-Boc-2-(p-toluenesulfonyl)guanidine with N-fluorenylmethoxycarbonyl-N'-tert-butyloxycarbonyl-L-lysine Fmoc-hArg(Boc2)-OH, removing Boc protection, and feeding Pbf-Cl to obtain N-(9-fluorenylmethoxycarbonyl)-2,2,4,6,7-pentamethyl-2H-benzofuran-5-sulfonyl-L-arginine. According to the invention, a p-toluenesulfonyl polypeptide guanidinylating agent is adopted in the route, so that ultralow-temperature reaction and the useof trifluoromethanesulfonyl chloride or trifluoromethanesulfonic anhydride with high corrosivity are avoided, and a simple and efficient way is provided for the synthesis of the intermediate.