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Imidazo[1,2-a]pyrazin-8(7H)-one, 2-(trifluoromethyl)- synthesis

2synthesis methods
-

Yield:850445-47-5 39%

Reaction Conditions:

Stage #1: 3-chloropyrazin-2-amine;3-chloro-1,1,1-trifluoroacetone at 100; for 16 h;
Stage #2: with sodium hydrogencarbonate in dichloromethane;water;

Steps:

A7

A mixture of 3-chloro-pyrazin-2-ylamine (0.50 g, 3.86 mmol) and l-chloro-3,3,3- trifluoroacetone (4 ml, 0.027 mmol) was stirred at 100 °C for 16 h. The mixture was partitioned between DCM and a saturated solution of sodium hydrogen carbonate. The organic layer was separated, dried (Na2S04), filtered and the solvents evaporated in vacuo to yield intermediate 7 (0.31 g, 39%) as a pale brown solid which was used in next step without further purification.

References:

WO2011/110545,2011,A1 Location in patent:Page/Page column 74-75