3-Benzyloxy-1-ethyl-5,6,8-trifluoro-7-pyrrolidin-1-yl-1H-quinazoline-2,4-dione → 1-Ethyl-5,6,8-trifluoro-3-hydroxy-7-pyrrolidin-1-yl-1H-quinazoline-2,4-dione
反応式
C([O:8][N:9]1[C:18](=[O:19])[C:17]2[C:12](=[C:13]([F:27])[C:14]([N:22]3[CH2:26][CH2:25][CH2:24][CH2:23]3)=[C:15]([F:21])[C:16]=2[F:20])[N:11]([CH2:28][CH3:29])[C:10]1=[O:30])C1C=CC=CC=1.FC(F)(F)C([O-])=O.FC(F)(F)C([O-])=O.FC(F)(F)C([O-])=O.[B+3]>FC(F)(F)C(O)=O>[CH2:28]([N:11]1[C:12]2[C:17](=[C:16]([F:20])[C:15]([F:21])=[C:14]([N:22]3[CH2:23][CH2:24][CH2:25][CH2:26]3)[C:13]=2[F:27])[C:18](=[O:19])[N:9]([OH:8])[C:10]1=[O:30])[CH3:29]参加物
4
実験手順
A solution of 3-benzyloxy-1-ethyl-5,6,8-trifluoro-7-pyrrolidin-1-yl-1H-quinazoline-2,4-dione (Example X-3, 0.15 g, 0.36 mmol) in trifluoroacetic acid (5.0 mL) was reacted with a 1.0 M solution of boron tris(trifluoroacetate) (1.8 mL, 1.8 mmol) in TFA and allowed to stir for 1 hour. The mixture was then concentrated and the residue dissolved in methanol and concentrated. This process was repeated three times. The residue was then triturated from diethyl ether and filtered to provide 0.11 g of the title compound as a solid, mp 223-225° C.