反应详情

To a solution of (R)-3-(2-{(S)-1-[9-(tetrahydropyran-2-yl)-9H-purin-6-ylamino]ethyl}benzoimidazol-1-yl)piperidine-1-carboxylic acid tertbutyl ester (2.27 g, 4.15 mmol) in DCM (25 mL) was added TFA (15 mL) and the mixture was stirred at RT for 1 h. Volatiles were removed under reduced pressure and the resulting residue was loaded onto an Isolute® SCX-2 cartridge. The cartridge was washed with a 1:1 mixture MeOH:DCM and the product was eluted with 2M NH3/MeOH (100 mL) in DCM (150 mL). The product containing fractions were combined and concentrated in vacuo affording [(S)-1-((R)-1-Piperidin-3-yl-1H-benzoimidazol-2-yl)ethyl]-(9H-purin-6-yl)amine as a pale yellow solid (1.53 g, quantitative). LCMS: RT 1.63 min [M+H]+ 363.2.

1. customVolatiles were removed under reduced pressure
2. washThe cartridge was washed with a 1:1 mixture MeOH
3. washDCM and the product was eluted with 2M NH3/MeOH (100 mL) in DCM (150 mL)
4. additionThe product containing fractions
5. concentrationconcentrated in vacuo