6-(5-氯-2-吡啶基)-6,7-二氢-7-羟基-5H-吡咯并[3,4-b]吡嗪-5-酮合成路线 （共 11 条）
反应条件
1: With trifluoroacetic acid in dichloromethane 18 h; Heating / reflux; 2: With water; sodium hydrogencarbonate in dichloromethane T=0°C; pH=7.5 - 8; Product distribution / selectivity;
参考文献
USV LIMITED
Patent: WO2009/63486 A2, 2009 ;
Location in patent: Page/Page column 22; 23 ;
反应条件
propan-1-ol; triethylamine; Novozymereg; 435 in toluene T=45°C; 16 - 24 h; Enzymatic reactionResolution of racemate; Purification / work up;
参考文献
Apotecnia , S.A.
Patent: EP2058313 A2, 2009 ;
Location in patent: Page/Page column 9 ;
反应条件
1: With water; sodium hydrogencarbonate in dichloromethane; acetonitrile T=25 - 30°C; 0.75 h; 2: With hydrogenchloride; formic acid; water T=0 - 68°C; 4 h; Product distribution / selectivity;
参考文献
MATRIX LABORATORIES LTD
Patent: WO2008/126105 A2, 2008 ;
Location in patent: Page/Page column 14-15 ;
反应条件
sodium hydroxide; sodium tetrahydroborate in water T=0 - 5°C; 4 - 5 h; Product distribution / selectivity;
参考文献
MATRIX LABORATORIES LTD
Patent: WO2008/126105 A2, 2008 ;
Location in patent: Page/Page column 9 ;
反应条件
phosphate buffer; Candida antarctica lipase B Chirazyme-L2; triethylamine in water; toluene T=60°C; pH=7; 96 h;
参考文献
Solares, Laura F.; Diaz, Monica; Brieva, Rosario; Sanchez, Victor M.; Bayod, Miguel; Gotor, Vicente
Tetrahedron Asymmetry, 2002 , vol. 13, # 23 p. 2577 - 2582
反应条件
phosphate buffer; Candida antarctica lipase B Novozym 435 in water; toluene T=60°C; pH=7; 96 h;
参考文献
Solares, Laura F.; Diaz, Monica; Brieva, Rosario; Sanchez, Victor M.; Bayod, Miguel; Gotor, Vicente
Tetrahedron Asymmetry, 2002 , vol. 13, # 23 p. 2577 - 2582
反应条件
pyridine in dichloromethane T=20°C; 17 h;
参考文献
Universidad de Oviedo; Astur Pharma, S.A.
Patent: US6969767 B1, 2005 ;
Location in patent: Page/Page column 8; 9 ;
反应条件
1: 4-methylpiperazin-1-ylcarbonyl chloride hydrochloride With triethylamine in dichloromethane T=5°C; 0.416667 h; 2: With 4-(N,N-dimethlyamino)pyridine in dichloromethane 0.0166667 - 0.0333333 h; 3: 6-(5-chloropyridin-2-yl)-7-hydroxy-6,7-dihydropyrrolo[3,4-b]pyrazin-5-one in dichloromethane T=20°C; 7 h; Heating / reflux; Product distribution / selectivity;
参考文献
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2008/2629 A1, 2008 ;
Location in patent: Page/Page column 13 ;
反应条件
1: 6-(5-chloropyridin-2-yl)-7-hydroxy-6,7-dihydropyrrolo[3,4-b]pyrazin-5-one With sodium hydride in N,N-dimethyl-formamide; mineral oil T=-10 - 35°C; 2: 4-methylpiperazin-1-yl-carbonyl chloride in N,N-dimethyl-formamide; mineral oil T=-10 - 20°C; Product distribution / selectivity;
参考文献
USV LIMITED
Patent: WO2009/63486 A2, 2009 ;
Location in patent: Page/Page column 19; 20; 23 ;
反应条件
1: 86 percent / pyridine / CH2Cl2 / 17 h / 20 °C 2: Candida antarctica lipase B Chirazyme-L2; phosphate buffer; triethylamine / toluene; H2O / 96 h / 60 °C / pH 7 3: 90 percent / acetone / 0 - 20 °C View Scheme
参考文献
Solares, Laura F.; Diaz, Monica; Brieva, Rosario; Sanchez, Victor M.; Bayod, Miguel; Gotor, Vicente
Tetrahedron Asymmetry, 2002 , vol. 13, # 23 p. 2577 - 2582
