(5S)-7-[4-(4-氟苯基)-6-异丙基-2-(N-甲基-N-甲磺酰基)嘧啶-5-yl]-5-羟基-3-氧代-6(E)-庚烯酸乙酯合成路线 (共 5 条)
反应条件
1: With diethyl methoxy borane in tetrahydrofuran; methanol T=-78 - -75°C; 0.833333 h; 2: With sodium tetrahydroborate in tetrahydrofuran; methanol T=-78°C; 2 h; 3: With acetic acid in tetrahydrofuran; methanol
参考文献
AUROBINDO PHARMA LIMITED
Patent: WO2008/96257 A1, 2008 ;
Location in patent: Page/Page column 24 ;
反应条件
1: trans-N-(4-(4-fluorophenyl)-6-isopropyl-5-(3-oxoprop-1-enyl)pyrimidin-2-yl)-N-methylmethanesulfonamide With lithium chloride; (S)-(-)-1,1'-bi-(2-naphthyloxy)(diisopropoxy)titanium in tetrahydrofuran
T=20°C; 0.166667 h;
2: 1-ethoxy-1,3-bis-(trimethylsilanyloxy)-buta-1,3-diene With N,N,N',N,-tetramethylethylenediamine in tetrahydrofuran
T=20°C;
3: With phosphoric acid; trifluoroacetic acid
more than 3 stages;
参考文献
ASTRAZENECA UK LIMITED
Patent: WO2007/7119 A1, 2007 ;
Location in patent: Page/Page column 20 ;
WO 2007/007119 A1
反应条件
hydrogenchloride; water in tetrahydrofuran
T=0 - 25°C; 1.5 h;
参考文献
ASTRAZENECA UK LIMITED
Patent: WO2008/65410 A1, 2008 ;
Location in patent: Page/Page column 27 ;
WO 2008/065410 A1
反应条件
1: trans-N-(4-(4-fluorophenyl)-6-isopropyl-5-(3-oxoprop-1-enyl)pyrimidin-2-yl)-N-methylmethanesulfonamide With lithium chloride; (S)-(-)-1,1'-bi-(2-naphthyloxy)(diisopropoxy)titanium in tetrahydrofuran
T=18 - 25°C; 0.0833333 h;
2: Brassard's diene in tetrahydrofuran
T=0 - 25°C; 42.17 h;
3: With hydrogenchloride in tetrahydrofuran; water
T=0°C; Product distribution / selectivity;
参考文献
ASTRAZENECA UK LIMITED
Patent: WO2008/65410 A1, 2008 ;
Location in patent: Page/Page column 36 ;
WO 2008/065410 A1
反应条件
1: With hydrogen fluoride in water; acetonitrile
T=0 - 30°C; 0.333333 - 2.25 h;
2: With sodium hydrogencarbonate in water; acetonitrile
Product distribution / selectivity;
参考文献
AUROBINDO PHARMA LIMITED
Patent: WO2008/96257 A1, 2008 ;
Location in patent: Page/Page column 21-24 ;