Patent · US Expired

Synthesis of thiazole derivatives

US5856500A · kind A · utility

0Cited by
7References
20Claims
0Family size

Assignee

Inventors

Key dates

Filing dateMar 11, 1997
Grant dateJan 5, 1999
Priority date
Expiry dateMar 11, 2017

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D277/48
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

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 about -10.degree. to about 25.degree. C., and agitating the mixture at about -10.degree. to about 60.degree. C. for at least about 1 hour; (b) heating the resultant mixture at about 40.degree. to about 60.degree. C. for at least about 0.5 hour; (c) mixing with the mixture from (b), thiourea and then water at about 40.degree. to about 60.degree. 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.degree. 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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.