(4S)-3-[5-(4-氟苯基)-1,5-二氧代戊基]-4-苯基-2-恶唑烷酮合成路线 （共 10 条）
反应条件
4-(N,N-dimethlyamino)pyridine; dicyclohexyl-carbodiimide in dichloromethane
参考文献
HANMI PHARM. CO., LTD.; KIM, Gi Jeong; KIM, Choong Hahn; CHANG, Ji Yeon; KIM, Nam Du; CHANG, Young Kil; LEE, Gwan Sun
Patent: WO2010/71358 A2, 2010 ;
Location in patent: Page/Page column 14-15 ;
反应条件
1: pivaloyl chloride; 5-(4-fluorophenyl)-5-oxopentanoic acid With 4-(N,N-dimethlyamino)pyridine in N,N-dimethyl-formamide T=2 - 20°C; 1.5 h; 2: (S)-5-phenyl-1,3-oxazolidine-2-one With 4-(N,N-dimethlyamino)pyridine in N,N-dimethyl-formamide T=30 - 35°C; 2 h;
参考文献
MICROBIA, INC.
Patent: US2008/287663 A1, 2008 ;
Location in patent: Page/Page column 23 ;
反应条件
1: With 4-(N,N-dimethlyamino)pyridine in N,N-dimethyl-formamide 7 h; Heating / reflux; 2: With sulfuric acid in water; N,N-dimethyl-formamide 0.5 h; 3: With sodium hydrogencarbonate in water; N,N-dimethyl-formamide
参考文献
US2006/135755 A1, ;
Page/Page column 16 ;
反应条件
1: Candida antarctica B lipase / toluene / 120 h / 35 °C / |Enzymatic reaction 2: pyridinium chlorochromate / dichloromethane / 2 h / 40 °C View Scheme
参考文献
Journal of Molecular Catalysis B: Enzymatic, , vol. 85-86, p. 99 - 104
反应条件
1: With dimethylsulfide borane complex; (R)-tetrahydro-1-methyl-3,3-diphenyl-1H,3H-pyrrolo[1,2-c]-[1,3,2]oxazaborole in dichloromethane; toluene T=-5 - 0°C; 4 - 6 h; 2: With sulfuric acid; dihydrogen peroxide in methanol; dichloromethane; water; toluene 0.25 h;
参考文献
SCHERING CORPORATION
Patent: EP1137634 B1, 2005 ;
Location in patent: Page/Page column 7 ;
反应条件
1: With BH3*N,N-diethylanilline; (R)-tetrahydro-1-methyl-3,3-diphenyl-1H,3H-pyrrolo[1,2-c]-[1,3,2]oxazaborole in tetrahydrofuran; toluene T=18 - 20°C; 1 h; 2: With water; potassium carbonate in tetrahydrofuran; toluene T=20 - 30°C; 0.5 h;
参考文献
Kotobuki Pharmaceutical Co., Ltd.
Patent: EP1988071 A1, 2008 ;
Location in patent: Page/Page column 11-12 ;
反应条件
magnesium sulfate in triethanolamine(chloride)
参考文献
Codexis, Inc.
Patent: US2010/62499 A1, 2010 ;
反应条件
borane-THF; boron trifluoride diethyl etherate; (R)-tetrahydro-1-methyl-3,3-diphenyl-1H,3H-pyrrolo[1,2-c]-[1,3,2]oxazaborole in tetrahydrofuran T=25°C; Product distribution; Further Variations:CatalystsTemperaturesacid additives, water content;
参考文献
Bertrand, Blandine; Durassier, Sonia; Frein, Stephane; Burgos, Alain
Tetrahedron Letters, 2007 , vol. 48, # 12 p. 2123 - 2125
反应条件
1: borane-THF / dichloromethane / 6 h / 0 - 20 °C / |Inert atmosphere 2: Candida rugosa lipase / di-isopropyl ether / 120 h / 35 °C / |Enzymatic reaction View Scheme
参考文献
Singh, Amit; Goel, Yogesh; Rai, Amit Kumar; Banerjee
Journal of Molecular Catalysis B: Enzymatic, 2013 , vol. 85-86, p. 99 - 104
反应条件
1.1: hydroxylamine hydrochloride / pyridine / 0 - 20 °C 2.1: titanium(IV) isopropylate; N-ethyl-N,N-diisopropylamine; titanium tetrachloride / dichloromethane / 0 °C 2.2: -15 °C 3.1: N,O-bis-(trimethylsilyl)-acetamide / toluene / 0.5 h / 60 °C 3.2: 8 h / 60 °C 3.3: 20 h / 20 °C 4.1: hydrogenchloride; formaldehyd / water; tetrahydrofuran / 6 h / 20 °C View Scheme
参考文献
PHARMATHEN S.A.; KOFTIS, Theocharis V.; ANDREOU, Thanos; ZITROU, Asteria
Patent: WO2012/76030 A1, 2012 ;
