反应详情

To 1-(2-fluorobenzyl)-5-(thiazol-2-yl)-1H-1,2,4-triazole-3-carbonitrile (Intermediate-5, 0.74 mmol) was added sodium methoxide/MeOH (0.5M, 4 equiv, 5.9 mL). After stirring at ambient temperature for 3 h, additional portion of sodium methoxide/MeOH (1 equiv) was added. After 2 h, ammonium chloride (10 equiv) was added and the resultant mixture was stirred at ambient for 17 h. The reaction mixture was conc. Half-saturated NaHCO3/1N NaOH solution (10:1) was added and the aqueous mixture was extracted with EtOAc. The organic phases were dried over Na2SO4, filtered and conc. to afford 1-(2-fluorobenzyl)-5-(thiazol-2-yl)-1H-1,2,4-triazole-3-carboximidamide as a white solid (>99% yield).

1. waitAfter 2 h
2. additionwas added
3. extractionthe aqueous mixture was extracted with EtOAc
4. dry with materialThe organic phases were dried over Na2SO4
5. filtrationfiltered