| 摘要 |
N-[4-(Cyanoethylthiomethyl)-2-thiazolyl]guanidine, is prepared by (a) mixing 1,3-dihaloacetone and 2-imino-4-thiobiuret in a suitable polar organic solvent at initial temperatures of -10 to 25 DEG C, and agitating the mixture at -10 to 60 DEG C for at least about 1 hour; (b) heating the resultant mixture at 40 to 60 DEG C for at least 0.5 hour; (c) mixing with the mixture from (b), thiourea and then water at 40 to 60 DEG C for a period of at least about 1 hour; (d) removing liquid polar solvent from the mixture of (c); and (e) mixing with the mixture from (d), 3-halopropionitrile and water-soluble alcohol, ether, or ether-alcohol, followed by aqueous alkali metal hydroxide while maintaining the temperature at below about 20 DEG C, to form N-[4-(cyanoethylthiomethyl)-2-thiazolyl]guanidine. The process avoids isolating and purifying any of the intermediates, and can be conducted in the same vessel, as a "one-pot" synthesis.
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