Abstract. A method for regiospecific N‐alkylation of 4 (or 5)‐methylimidazoles (1a‐c) to 1,5‐disubstituted and 1,2,5‐trisubstituted derivatives has been elaborated. The process consists of the regiospecific N‐acetylation of 1a‐c to give isomerically pure 3a‐c; these are quaternized and deacetylated to 5a‐j. When simplified to a one‐pot synthesis, yields up to 40% of N‐substituted products are realized.
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Godefroi et al. (1974) studied this question.
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