硼替佐米的合成路線scifinder

硼替佐米的合成路線scifinder

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1、SciFinder?Page1TaskHistoryTaskBeganJuly23,201210:45PMExplorereactionsbystructurevariableonlyatspecifiedpositions(ID5)AnswerType:ReactionsResultCount:159SciFinder?Page21.10Steps(Converging)Sequence1

2、Sequence2

3、Sequence3SingleStepStepStagesNotesYield1Reactants:2,Solvents:1,Steps:1.1S:CH2

4、Cl2,17h,rt1,Stages:1Sequence1

5、Sequence2

6、Sequence32Steps1StepStagesNotesYield1Reactants:2,Solvents:1,Steps:1.1S:CH2Cl2,10min,rt;17h,rt1,Stages:12[Reactant]StepStagesNotesYield2Reactants:2,Steps:1,Stages:197%2.130min,-40--30°C;2h,-30°C?rt;17h,rtSequence1

7、Sequence2

8、Sequence3SciFinder?Pag

9、e37Steps1StepStagesNotesYield1Reactants:1,Reagents:3,41%1.1R:Mg,C:BrCH2CH2Br,S:Et2O,rt;30min,rtCatalysts:1,Solvents:2,Steps:1,1.2R:(MeO)3B,S:Et2O,3h,-70°C;45min,-60--70°CStages:31.3R:H2SO4,S:H2O,1h,rt2[Reactant]StepStagesNotesYield2Reactants:2,Solvents:1,Steps:95%2.1S:Et2O,48h,rt1,Sta

10、ges:13[Reactant]StepStagesNotesYield3Reactants:2,Reagents:4,77%3.1R:BuLi,R:i-Pr2NH,S:Et2O,S:Me(CH2)4Me,-15°C;30min,-Solvents:3,Steps:1,Stages:410--15°C;45min,-10°C?rt3.2S:Et2O,rt?-90°C;1.5h,-80--90°C;30min,-80--70°C;-70°C?-50°C;50min,-50°C3.3R:ZnCl2,S:Et2O,25min,-45°C;17h,-45°C?rt3.4R

11、:H2SO4,S:H2O,25min,rtSciFinder?Page44[Reactant]StepStagesNotesYield4Reactants:2,Reagents:1,87%4.1R:BuLi,S:Et2O,S:Me(CH2)4Me,rt?-40°C;10min,-40°CSolvents:2,Steps:1,Stages:24.2S:Et2O,45min,-25--30°C;-30°C?0°C5[Reactant]StepStagesNotesYield5Reactants:2,Solvents:1,Steps:78%5.1S:Et2O,1h,-1

12、5--10°C;1.5h,-25--10°C1,Stages:16[Reactant]StepStagesNotesYield6Reactants:2,Reagents:2,84%6.1R:TBTU,R:EtN(Pr-i)2,S:CH2Cl2,2h,-5°C;1.5h,-5°C;-Solvents:1,Steps:1,Stages:15°C?rt7StepStagesNotesYieldSciFinder?Page57Reactants:1,Reagents:3,83%7.1R:HCl,S:H2O,S:MeOH,S:Me(CH2)4Me,rt?10°CSolven

13、ts:3,Steps:1,Stages:37.2R:17h,rt7.3R:NaHCO3,S:H2O,30min,rtSourceMethodofobtainingpyrazinoyl-(L)-phenylalanyl-(L)-leucineboronicacidoritsanhydrideIvanov,A.S.;Zhalnina,A.A.;Shishkov,S.V.;Fedorov,V.E.;Perminov,S.V.AssigneeZAO"Farm-Sintez",Russia2010PatentInformationOct27,2010RU2402564C2N

14、umber

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