Preparation fo N(#PI#)-alkyl-histmine andhistidine derivatives through efficient alkylation follwed by deprotection using activiated silica gel

摘要

Efficient N(#PI#)-alkylation of L-histidine and histamine derivatives through employment of N(#tau#)-tritylprotection wa achieved and regioselective removal of the N(#tau#)-trityl group in thepresence of either Bocor trityl-protected primaryamine wa efected based on a mild hydrolysis mediated by activated silica gel with 0.1-0.2% trifluoroacetic acid.