4-chloro-6-cyclopentylpyrimidin-2-amine synthesis

Yield:-

Reaction Conditions:

with tetraethylammonium chloride;N,N-dimethyl-aniline;trichlorophosphate in acetonitrile at 110; for 0.333333 h;

Steps:

1.B

Step B: 2-Amino-4-chloro-6-cyclopentylpyrimidine. A suspension of 2-amino-6-cyclopentyl-3H-pyrimidin-4-one (1.52 g, 8.4 mmol), tetraethyl ammonium chloride (2.8 g 16.9 mmol) and dimethylaniline (1.1 mL, 8.4 mmol) in acetonitrile (16 mL) was treated with phosphorous oxychloride (4.7 mL, 51 mmol) and heated at 110° C. for 20 min. The resulting solution was cooled to rt and concentrated to minimum volume then diluted with CHCl₃ and ice and stirred for 30 min. The layers were separated and the organic layer was washed with water (3*50 mL) and 5% NaHCO₃, dried, and concentrated to yield 2.0 g of crude product that was used without purification.

References:

US2008/194577,2008,A1 Location in patent:Page/Page column 11