| 摘要 |
PURPOSE: A new alkylation reaction of pyrrol is provided, which is characterized by manufacturing high yield of a panethyl transfer enzyme inhibitor(formula 3), having improved safety and reliance of synthesis and doing mass production. CONSTITUTION: The panethyl transfer enzyme inhibitor(formula 3) is obtained by making a pyrrol derivative(formula 1) into an imidazole derivative(formula 2) by N-alkylation reacting in non-aqueous polar solvent under existence of an alkali metal t-alkoxide base and a polyethylene glycol monomethyl ether catalyst. In the formula 1, 2, and 3, R represents hydrogen or substituted/not substituted alkyl, aryl or aralkyl of a straight chain or a side chain having 1-8 of carbon number; R1 and R2 represent alkyl of a straight chain or a side chain having 1-4 of carbon number isolated/not isolated or substituted/not substituted by O, S, SO2 or NR4(R4 represents hydrogen or alkyl of a straight chain or a side chain having 1-4 of carbon number) respectively, or constitute 5-6 of heterocycle by reducing O, S, SO2 or NR4 with nitrogen attaching R1 and R2, and R3 represents substituted/not substituted alkyl, aryl or aralkyl of a straight chain or a side chain having 1-4 of carbon number.
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