2-Thiazolecarboxaldehyde, 4-trifluoroMethyl- synthesis

Yield:-

Reaction Conditions:

Stage #1: (4-(trifluoromethyl)-1,3-thiazol-2-yl)methanolwith Dess-Martin periodane in dichloromethane at 0 - 20; for 3 h;
Stage #2: with sodium hydrogencarbonate in dichloromethane; for 0.166667 h;

Steps:

1.1.16

To the alcohol, (4-(trifluoromethyl)thiazol-2-yl)methanol (245 mg, 1.34 mmol) in DCM (10 ml) at 0°C, DMP (681 mg, 1.61 mmol) was added. Reaction was allowed to come to rt and stirred for 3h. Then saturated sodium bicarbonate, hypo mixture was added and stirred for 10 min. Then reaction mixture was further diluted with DCM and product was extracted into DCM. Volatiles were removed under vacuum and the resulting aldehyde, 4- (trifluoromethyl) thiazole-2-carbaldehyde was carried to the next step without further purification.

References:

WO2012/54510,2012,A1 Location in patent:Page/Page column 91