反应详情

Place 3-[({6-{(4′-fluoro-biphenyl-4-carbonyl)-amino]-benzothiazol-2-yl}-methyl-amino)-methyl]-pyrrolidine-1-carboxylic acid tert-butyl ester in DCM (50 mL). Add trifluoroacetic acid (100 mL) and stir at rt for 6 h. Concentrate in vacuo and then add DCM:Hexane and concentrate in vacuo. Dissolve the residue in 1:1 MeOH:DCM and add polyvinyl pyridine (3 g) and stir for 15 min. Filter the solution and wash the resin with DCM. Collect the filtrate and concentrate in vacuo to yield 1.50 g (95%) of the title compound. mass spectrum (ion-spray): (m/z)=461.0 (M+1).

1. concentrationConcentrate in vacuo
2. concentrationadd DCM:Hexane and concentrate in vacuo
3. dissolutionDissolve the residue in 1:1 MeOH
4. additionDCM and add polyvinyl pyridine (3 g)
5. filtrationFilter the solution
6. washwash the resin with DCM
7. customCollect the filtrate
8. concentrationconcentrate in vacuo