| 摘要 |
PURPOSE: Provided is a useful method for synthesizing 1-substituted-2-mercapto-5-hydroxymethyl imidazole that is represented by formula (1) and an intermediate used in the synthesis of various antitumor agents. CONSTITUTION: The synthesizing method is characterized by reacting 1,3-dihydroxyacetone dimer of formula (2) and potassium thiocyanate of formula (4) of KSCN with amine hydrochloride of formula (3) of RNH2·HCl in lower alcohol solvent in the presence of acid catalyst. In formulae (1) and (3), R is alkyl, allyl, arylmethyl or diarylmethyl. The catalyst is organic acid comprising properly acetic acid, propionic acid or other conventional organic acids. The lower alcohol solvent comprises properly linear or branched alcohol of C1-4, or a mixture thereof, preferably isopropanol or n-butanol. The temperature of reaction ranges from 10 to 100 deg.C, preferably from 20 to 80 deg.C. The 1,3-dihydroxyacetone dimer of formula (2) is used in a molar ratio of 0.5 to 2 times, preferably 1 to 1.5 times, based on that of amine hydrochloride of formula (3) of RNH2·HCl. The potassium thiocyanate of formula (4) of KSCN is used in a molar ratio of 1 to 3 times, preferably 1 to 2 times, based on that of amine hydrochloride of formula (3) of RNH2·HCl.
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