Heteromonocyclic compound and use thereof
A compound, heterocyclyl technology, applied in the field of novel heteromonocyclic compounds
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Embodiment 222
[0857] 6-Butyl-3-(4-ethoxyphenyl)-2-methyl-5-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadi Azol-3-yl)biphenyl-4-yl]methyl}pyrimidin-4(3H)-one (Example 222);
[0858] 3-[4-(1-ethylpropoxy)phenyl]-2-methyl-5-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxa Oxadiazol-3-yl)biphenyl-4-yl]methyl}-6-propylpyrimidin-4(3H)-one (Example 256);
[0859] 3-(4-tert-butoxyphenyl)-2-ethyl-5-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazole-3 -yl)biphenyl-4-yl]methyl}-6-propylpyrimidin-4(3H)-one (Example 364);
[0860] 2-Ethyl-3-[4-(2-hydroxy-1,1-dimethylethoxy)phenyl]-5-{[2'-(5-oxo-4,5-dihydro- 1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-6-propylpyrimidin-4(3H)-one (Example 377); or
[0861] 2-Ethyl-3-[4-(2-hydroxy-1,1-dimethylpropoxy)phenyl]-5-{[2'-(5-oxo-4,5-dihydro- 1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-6-propylpyrimidin-4(3H)-one (Example 444);
[0862] or their salts.
[0863] [Compound A-III]
[0864] Compound A, wherein R3a is
[0865] (1) C1-C6 alkyl, which is optionally substituted by 1-3 substituents se...
Embodiment 1
[1703] 3-(2,2-Dimethyl-2,3-dihydro-1-benzofuran-5-yl)-2-methoxy-5-{[2'-(5-oxo-4, 5- Dihydro-1,2,4- evil Oxadiazol-3-yl)biphenyl-4-yl]methyl}-6-propylpyrimidin-4(3H)-one
[1704]
[1705] 1a) 4'-[(2-Methoxy-6-oxo-4-propyl-1,6-dihydropyrimidin-5-yl)methyl]biphenyl-2-carbonitrile
[1706] At room temperature, methyl imidocarbamate sulfate (methyl imidocarbamate sulfate) (10 g), 28% sodium methoxide (26 mL) and 2-[(2'-cyanobiphenyl-4-yl)methyl]-3 - A solution of ethyl oxohexanoate (15.8 g) in methanol (100 mL) was stirred overnight. The solvent was evaporated under reduced pressure, then water and acetic acid were added. The precipitated solid was collected by filtration and washed with water and diethyl ether to give the title compound (2.62 g, 16%) as a colorless solid.
[1707] 1 H NMR (300MHz, DMSO-d 6 )δ0.86(3H, t, J=7.2), 1.46-1.64(2H, m), 2.46(2H, t, J=7.2), 3.82(2H, s), 3.86(3H, s), 7.32( 2H, d, J = 8.4), 7.47 (2H, d, J = 8.4), 7.52-7.63 (2H, m), 7.72-7.82...
Embodiment 2
[1717] 2-(dimethylamino)-3-(2,2-dimethyl-2,3-dihydro-1-benzofuran-5-yl)-5-{[2'-(5-oxo Generation-4,5-dihydro-1,2,4- evil Oxadiazol-3-yl)biphenyl-4-yl]methyl}-6-propylpyrimidin-4(3H)-one
[1718]
[1719] 2a) 4'-{[2-(Dimethylamino)-6-oxo-4-propyl-1,6-dihydropyrimidin-5-yl]methyl}biphenyl-2- Formaldehyde
[1720] To ethyl 2-[(2'-cyanobiphenyl-4-yl)methyl]-3-oxohexanoate (6.41g) and N,N-dimethylguanidine sulfate (5.0g) in ethanol (100 mL) was added 20% sodium ethoxide-ethanol solution (11 mL), and the mixture was heated under reflux for 24 hrs. The reaction mixture was cooled to room temperature, and the solvent was evaporated under reduced pressure. The residue was washed with water and diethyl ether to give the title compound (2.06 g, 30%) as a pale yellow solid.
[1721] 1 H NMR (300MHz, DMSO-d 6 )δ0.85(3H, t, J=7.5), 1.42-1.63(2H, m), 2.37(2H, t, J=7.5), 3.02(6H, s), 3.78(2H, s), 7.31( 2H, d, J = 7.8), 7.46 (2H, d, J = 7.8), 7.50-7.63 (2H, m), 7.70-7.82 (1H,...
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