
[4,4'-Bipyrimidin]-6(1H)-one, 2-[(2S)-2-(4-fluorophenyl)-4-morpholinyl]-1-methyl- synthesis
- Product Name:[4,4'-Bipyrimidin]-6(1H)-one, 2-[(2S)-2-(4-fluorophenyl)-4-morpholinyl]-1-methyl-
- CAS Number:503860-57-9
- Molecular formula:C19H18FN5O2
- Molecular Weight:367.38
Yield:503860-57-9 74%
Reaction Conditions:
with triethylamine in tetrahydrofuran at 20;
Steps:
1.3; 2.3
A solution of (2S) -2- (4-fluorophenyl) morpholine hydrochloride (108.6 mg, 0.60 mmol), 2-chloro-l-methyl- IH- [4, 4' ] bipyrimidinyl-6-one (88.4. mg, 0.40 mmol) and triethylamine (0.27 ml, 2.0 mmol) in tetrahydrofuran .(2 ml) was stirred at room temperature for several hours. The precipitate was filtered off after cooling, and the solvent was evaporated in vacuo. The residue was washed with ethyl acetate to give the title compound (100 mg, 74%) .1H-NMR(CDCI3) δ: 3.09 (dd, J=12.9, 10.8 Hz, IH), 3.29 (m, IH), 3.52-3.64 (m, 2H), 3.59 (s, 3H), 4.00 (m, IH), 4.21 (m, IH), 4.72 (dd, J=1.0.5, 2.1 Hz, IH), 7.07-7.13 (m, 2H)', 7.38-7.43 (m, 3H),, 8.13 (dd, J=5.4, 1.2 Hz, IH), . 8.88 (d, J=5.1 Hz, IH), 9.28 (s, IH). MS [M+H]+: 367.
References:
WO2007/11065,2007,A2 Location in patent:Page/Page column 90; 94

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