| 摘要 |
Produced 2-guanidino- 4-amidino- thiomethyl thiazole has formula (I). Cpd. (I) is obtd. by cyclisation of amidino-thiourea of formula (II) with 1,3-dihaloacetone, in an organic solvent, followed by reacting the cyclisation prod. of formula (III) (where X is halide ion), with thiourea in the presence of water, with heating, and conversion of obtd. dihydrohalide of (I) into a free base. Cyclisation is conducted in presence of catalyst comprising alkali metal (pref. sodium) iodide, using aliphatic 3-6C ketone (pref. acetone) or aliphatic 2-4C nitrile as solvent, in which the catalyst is dissolved. The reaction temp. is 20-40 deg.C. Prod. of cyclisation (III) is reacted with thiourea directly in the reaction mixt. obtd. at cyclisation stage. Alkali metal iodide (catalyst) is taken in amt. 4-6 mol.%. The yield of (I) is 85-90% and the content of biologically active substance is up to
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