(5R)-3-[3-氟-4-(4-吗啡啉基)苯基]-5-羟甲基-2-恶唑烷酮合成路线 （共 20 条）
反应条件
1: [3-fluoro-4-(4-morpholinyl)phenyl]carbamic acid phenylmethyl ester With n-butyllithium in tetrahydrofuran; hexane T=-78°C; 1 h; Inert atmosphere; 2: (-)-(R)-glycidyl butyrate in tetrahydrofuran; hexane T=-78 - 20°C; 3: With ammonium chloride in tetrahydrofuran; hexane; water
参考文献
Chen, Lei; Wang, Jian-Wei; Hai, Li; Wang, Guang-Ming; Wu, Yong
Synthetic Communications, 2010 , vol. 40, # 6 p. 789 - 798
反应条件
water; sodium t-butanolate in tetrahydrofuran T=0 - 15°C; 0.5 h;
参考文献
WO2012/114355 A1, ;
Page/Page column 11 ;
反应条件
1.1: N,N-diisopropylethylamine 2.1: ammonium formate / 10 percent Pd/C / methanol; tetrahydrofuran 3.1: NaHCO3 4.1: n-BuLi / tetrahydrofuran; hexane / -78 °C 4.2: hexane; tetrahydrofuran / -78 - 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 12, # 6 p. 857 - 859
反应条件
1.1: ammonium formate / 10 percent Pd/C / methanol; tetrahydrofuran 2.1: NaHCO3 3.1: n-BuLi / tetrahydrofuran; hexane / -78 °C 3.2: hexane; tetrahydrofuran / -78 - 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry Letters, , vol. 12, # 6 p. 857 - 859
反应条件
1: N-carboethoxy-3-fluoro-4-morpholinylaniline With n-butyllithium in tetrahydrofuran; hexane T=-78°C; 3.5 h; Inert atmosphere; 2: (-)-(R)-glycidyl butyrate in tetrahydrofuran; hexane T=-78 - 20°C; 3: With ammonium chloride in tetrahydrofuran; hexane; water T=20°C; 0.5 h; Product distribution / selectivity;
参考文献
JUBILANT LIFE SCIENCES LIMITED; GUPTA, Ashish, Kumar; SINGH, Shishupal; PANDA, Atulya, Kumar; BISWAS, Sujay; VIR, Dharam
Patent: WO2011/114210 A2, 2011 ;
Location in patent: Page/Page column 20 ;
反应条件
sodium hydride in tetrahydrofuran T=0°C;
参考文献
Narina, Srinivasarao V.; Sudalai, Arumugam
Tetrahedron Letters, 2006 , vol. 47, # 38 p. 6799 - 6802
反应条件
1.1: NaI; Na2CO3 / dimethylformamide / 65 °C 2.1: aq. NaHCO3 / acetone 3.1: 95 percent / (COCl)2; DMSO; Et3N / CH2Cl2 / -78 - -60 °C 4.1: nitrosobenzene; D-proline / acetonitrile / 24 h / -20 °C 4.2: NaBH4 / methanol 4.3: 86 percent / CuSO4 / methanol 5.1: 96 percent / sodium hydride / tetrahydrofuran / 0 °C View Scheme
参考文献
Tetrahedron Letters, , vol. 47, # 38 p. 6799 - 6802
反应条件
1: N-[4(R)-(2,2-dimethyl-1,3-dioxolane-4-yl)methyl]-3-fluoro-4-morpholinylaniline With hydrogenchloride; water in methanol T=20°C; 8 h; 2: bis(trichloromethyl) carbonate With sodium carbonate T=20°C; 24 h; Further stages.;
参考文献
Guangyu, Xu; Yi, Zhou; Chunhao, Yang; Yuyuan, Xie
Heteroatom Chemistry, 2008 , vol. 19, # 3 p. 316 - 319
反应条件
1.1: nitrosobenzene; D-proline / acetonitrile / 24 h / -20 °C 1.2: NaBH4 / methanol 1.3: 86 percent / CuSO4 / methanol 2.1: 96 percent / sodium hydride / tetrahydrofuran / 0 °C View Scheme
参考文献
Tetrahedron Letters, , vol. 47, # 38 p. 6799 - 6802
反应条件
1.1: 95 percent / (COCl)2; DMSO; Et3N / CH2Cl2 / -78 - -60 °C 2.1: nitrosobenzene; D-proline / acetonitrile / 24 h / -20 °C 2.2: NaBH4 / methanol 2.3: 86 percent / CuSO4 / methanol 3.1: 96 percent / sodium hydride / tetrahydrofuran / 0 °C View Scheme
参考文献
Tetrahedron Letters, , vol. 47, # 38 p. 6799 - 6802
