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ChemicalBook CAS DataBase List 4-(4-BROMOPYRIMIDIN-2-YL)MORPHOLINE

4-(4-BROMOPYRIMIDIN-2-YL)MORPHOLINE synthesis

2synthesis methods
-

Yield:663194-10-3 87%

Reaction Conditions:

with phosphorus(V) oxybromide in acetonitrile; for 1 h;Heating / reflux;

Steps:

2c

2c) 4- (4-BROMO-PVRIMIDIN-2-VL)-MORPHOLINE A mixture of 2-morpholin-4-yl-pyrimidin-4-ol (6.08 g, 33.6 MMOL) and phosphorus OXYBROMIDE (12.5 g, 43.7 MMOL) in 330 mL MECN is heated to reflux for 1 hour. The reaction is cooled to room temperature, concentrated to half volume, and poured over ice. The resulting mixture is neutralized with a saturated solution of NaHCOs, and then extracted with methylene chloride. The organic phase is washed with saturated NACI (aqueous), dried over ANHYDROUS MGS04, FILTERED, concentrated and dried to an off-white solid (7.11 g, 87%). M+H'= 245.97. H NMR (CDC13) ; a 8.05 (d, 1H), 6.70 (d, 1H), 3.75 (m, 8H).

References:

WO2005/28444,2005,A1 Location in patent:Page/Page column 50-51