The Regiospecific Alkylation of Histidine Side Chains

Abstract
Further work on the regiospecific alkylation of histidine and imidazole derivatives is reported, including convenient preparations of N(α)-benzyloxycarbonyl-N(π)-benzyl-L-histidine and N(α)-benzyloxycarbonyl-N(π)-benzyloxymethyl-L-histidine, and a sequence of reactions enabling controlled exclusive alkylation of the least hindered im-nitrogen (tritylation, phenacylation, detritylation, alkylation, and finally dephenacylation with zinc/acetic acid) in 4(5)-alkylimidazoles.

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