3-(4-甲基哌嗪-1-基)苯硼酸合成路线 (共 4 条)
反应条件
1: 1-(3-bromophenyl)-4-methylpiperazine With n-butyllithium in tetrahydrofuran; hexane
T=-78 - -70°C;
2: tri-isopropoxy-borane in tetrahydrofuran; hexane
T=-78 - 20°C;
3: With water; ammonium chloride in tetrahydrofuran; hexane
参考文献
SENEXIS LIMITED; HORWELL, David Christopher; SCOPES, David Ian Carter
Patent: WO2011/144578 A1, 2011 ;
Location in patent: Page/Page column 34 ;
反应条件
1: With n-butyllithium in tetrahydrofuran; hexane
T=-70 - -65°C; 1 h;
2: With tri-isopropoxy-borane in tetrahydrofuran; hexane
T=-70 - 20°C;
3: With water; ammonium chloride in tetrahydrofuran; hexane
参考文献
SENEXIS LIMITED
Patent: US2010/298325 A1, 2010 ;
Location in patent: Page/Page column 22 ;
反应条件
1.1: sodium t-butanolate; 1,8-diazabicyclo[5.4.0]undec-7-ene / 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl; tris-(dibenzylideneacetone)dipalladium(0) / toluene / 60 - 100 °C / Inert atmosphere
2.1: n-butyllithium / hexane; tetrahydrofuran / -78 - -70 °C
2.2: -78 - 20 °C
View Scheme
参考文献
SENEXIS LIMITED; HORWELL, David Christopher; SCOPES, David Ian Carter
Patent: WO2011/144578 A1, 2011 ;
反应条件
1.1: sodium t-butanolate; 1,8-diazabicyclo[5.4.0]undec-7-ene / 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl; tris-(dibenzylideneacetone)dipalladium(0) / toluene / 60 - 100 °C / Inert atmosphere
2.1: n-butyllithium / hexane; tetrahydrofuran / -78 - -70 °C
2.2: -78 - 20 °C
View Scheme
参考文献
SENEXIS LIMITED; HORWELL, David Christopher; SCOPES, David Ian Carter
Patent: WO2011/144578 A1, 2011 ;