[F:1][C:2]([F:25])([F:24])[CH:3]([NH:6][C:7]1[N:8]=[CH:9][C:10]2[CH2:16][CH2:15][N:14](C(OC(C)(C)C)=O)[CH2:13][C:11]=2[N:12]=1)[CH2:4][OH:5].C(O)(C(F)(F)F)=O>C(Cl)Cl>[F:25][C:2]([F:1])([F:24])[CH:3]([NH:6][C:7]1[N:8]=[CH:9][C:10]2[CH2:16][CH2:15][NH:14][CH2:13][C:11]=2[N:12]=1)[CH2:4][OH:5]To a stirred solution of 352 (53 mg, 0.15 mmol) in DCM (750 μL) at RT under nitrogen was added TFA (750 μL). The solution was stirred for 2 h and was then concentrated in a rotovap under high vacuum. The residue was redissolved in DCM (10 mL) and stirred rapidly with 1M Na2CO3 (10 mL) for 5 min. The layers were separated and the aqueous phase was extracted with DCM (2×10 mL). The combined extracts were dried (MgSO4), filtered and concentrated to afford 29 mg (76%) of 3,3,3-trifluoro-2-(5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-ylamino)propan-1-ol (354) as a yellow foam.
Wird geladen…
