2-[2-[(3S)-3-[3-[(E)-2-(7-氯-2-喹啉基)乙烯基]苯基]-3-[(甲烷磺酰基)氧基]丙基]苯基]-2-丙醇合成路线 （共 11 条）
反应条件
1: 1-(mercaptomethyl)-cyclopropaneacetic acid With n-butyllithium in tetrahydrofuran T=-12.5°C; 0.666667 h; 2: 2-(3-(S)-(3-(2-(7-chloroquinolinyl)ethenyl)phenyl)-3-methanesulfonyloxypropyl)phenyl-2-propanol in tetrahydrofuran T=-2°C; 3.5 h; 3: N,N-dicyclohexylamine in isopropyl alcohol; acetonitrile T=29°C; 15.5 h; Product distribution / selectivity;
参考文献
DR. REDDY'S LABORATORIES LTD.; DR. REDDY'S LABORATORIES, INC.; FOX, Martin Edward; BOLLIKONDA, Satyanarayana; MOHANARANGAM, Saravanan; JINNA, Rajender Reddy; KANDIRELLI, Venkata Kiran Kumar
Patent: WO2010/148209 A2, 2010 ;
Location in patent: Page/Page column 21 ;
反应条件
1: in tetrahydrofuran T=-45 - -10°C; 12 h; 2: With acetic acid in tetrahydrofuran; water; ethyl acetate pH=3.5;
参考文献
SANDOZ AG
Patent: WO2008/23044 A1, 2008 ;
Location in patent: Page/Page column 11-12 ;
反应条件
1: With sodium hydroxide in N,N-dimethyl-formamide T=-5 - 0°C; 6 h; 2: With water; sodium chloride in isopropanol acetate; N,N-dimethyl-formamide 0.5 h; 3: With 2,3-dihydroxybutanedioic acid in water Product distribution / selectivity;
参考文献
MEDICHEM, S.A.
Patent: WO2006/58545 A1, 2006 ;
Location in patent: Page/Page column 9-11; 19 ;
反应条件
1: With sodium hydroxide in water; N,N-dimethyl-formamide T=25°C; 2 h; 2: With sodium chloride in water; ethyl acetate; N,N-dimethyl-formamide T=25°C; 0.25 h; 3: With 2,3-dihydroxybutanedioic acid in water; ethyl acetate; N,N-dimethyl-formamide T=25°C; 0.25 h;
参考文献
ZENTIVA, A.S.
Patent: WO2008/83635 A1, 2008 ;
Location in patent: Page/Page column 9 ;
反应条件
1: 1-(mercaptomethyl)-cyclopropaneacetic acid With sodium hydroxide in water; N,N-dimethyl-formamide T=20°C; 0.166667 h; 2: 2-(3-(S)-(3-(2-(7-chloroquinolinyl)ethenyl)phenyl)-3-methanesulfonyloxypropyl)phenyl-2-propanol in tetrahydrofuran; water; N,N-dimethyl-formamide T=25°C; 2 h; 3: With 2,3-dihydroxybutanedioic acid in tetrahydrofuran; water; ethyl acetate; N,N-dimethyl-formamide T=25°C; 0.25 h; Product distribution / selectivity;
参考文献
Chemagis Ltd.
Patent: US2007/208178 A1, 2007 ;
Location in patent: Page/Page column 6 ;
反应条件
1: With sodium methylate in dimethyl sulfoxide T=-5 - 0°C; 10 h; 2: With water; acetic acid T=10 - 20°C; pH=6.6; Product distribution / selectivity;
参考文献
TEVA PAHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARAMCEUTICAL USA, INC.
Patent: WO2007/5965 A1, 2007 ;
Location in patent: Page/Page column 17 ;
反应条件
1.1: sodium methylate / N,N-dimethyl-formamide; methanol / 1.5 h / -10 °C / Inert atmosphere 1.2: 15 h / -5 °C / Inert atmosphere 1.3: 0.17 - 0.25 h 2.1: ethyl acetate / 0.5 h / 20 °C 3.1: 2,3-dihydroxybutanedioic acid / dichloromethane; water / 0.25 - 0.33 h 3.2: 0.08 - 0.17 h View Scheme
参考文献
IND-SWIFT LABORATORIES LIMITED; BHIRUD SHEKHAR, Bhaskar; SARIN, Gurdeep Singh; TRIPATHI RATNAKAR, Mani
Patent: WO2012/77133 A1, 2012 ;
反应条件
sodium t-butanolate in tetrahydrofuran; toluene T=-10 - 21°C; Inert atmosphereLarge scale reaction;
参考文献
Halama, Ales; Jirman, Josef; Bouskova, Olga; Gibala, Petr; Jarrah, A. Kamal
Organic Process Research and Development, 2010 , vol. 14, # 2 p. 425 - 431
反应条件
sodium t-butanolate in tetrahydrofuran; toluene T=-10 - 20°C; Inert atmosphereLarge scale reaction;
参考文献
Organic Process Research and Development, , vol. 14, # 2 p. 425 - 431
反应条件
1.1: tetrahydrofuran; hexane / 10 h / -15 - 5 °C 1.2: 24 h / 25 - 35 °C 2.1: acetic acid / dichloromethane; water / 25 - 30 °C / pH 4 - 4.5 2.2: 0.5 h View Scheme
参考文献
LAURUS LABS PRIVATE LIMITED; SIMHADRI, Srinivas; MOHAMMAD, Yaseen; INDUKURI, Venkata, Sunil, Kumar; GORANTLA, Seeta, Ramanjaneyulu; CHAVA, Satyanarayana
Patent: WO2014/1860 A1, 2014 ;
