Regiospecific alkylation of histidine and histamine at N-1 (τ)

Article abstract of DOI:10.1016/0040-4020(96)00187-1

Series of 1-alkyl histidines and histamines have been synthesized by the alkylation of the corresponding 5,6,7,8-tetrahydro-5-oxomidazo[1,5-c]pyrimidines with alkyl halides in aprotic solvents. The method of conversion of the intermediate quaternary salt to the amino acid or amino depends on the nature of the alkyl group.