2-Methyl-5-(trifluoromethoxy)benzoic acid → 5-(7-Methoxy-3H-spiro[1-benzofuran-2,1'-cyclopentan]-4-yl)-4,4-dimethyl-2-(1-{[2-methyl-5-(trifluoromethoxy)phenyl]carbonyl}piperidin-4-yl)-2,4-dihydro-3H-pyrazol-3-one
Reaktionsgleichung
Cl.[CH3:2][O:3][C:4]1[C:16]2[O:15][C:10]3([CH2:14][CH2:13][CH2:12][CH2:11]3)[CH2:9][C:8]=2[C:7]([C:17]2[C:18]([CH3:30])([CH3:29])[C:19](=[O:28])[N:20]([CH:22]3[CH2:27][CH2:26][NH:25][CH2:24][CH2:23]3)[N:21]=2)=[CH:6][CH:5]=1.[CH3:31][C:32]1[CH:40]=[CH:39][C:38]([O:41][C:42]([F:45])([F:44])[F:43])=[CH:37][C:33]=1[C:34](O)=[O:35]>>[CH3:2][O:3][C:4]1[C:16]2[O:15][C:10]3([CH2:11][CH2:12][CH2:13][CH2:14]3)[CH2:9][C:8]=2[C:7]([C:17]2[C:18]([CH3:30])([CH3:29])[C:19](=[O:28])[N:20]([CH:22]3[CH2:27][CH2:26][N:25]([C:34]([C:33]4[CH:37]=[C:38]([O:41][C:42]([F:43])([F:44])[F:45])[CH:39]=[CH:40][C:32]=4[CH3:31])=[O:35])[CH2:24][CH2:23]3)[N:21]=2)=[CH:6][CH:5]=1Komponenten
3
Edukt 2
Produkt 1
Versuchsvorschrift
The title compound is prepared analogously as described for GP2-WU2 using 5-(7-methoxy-3H-spiro[1-benzofuran-2,1′-cyclopentan]-4-yl)-4,4-dimethyl-2-piperidin-4-yl-2,4-dihydro-3H-pyrazol-3-one (compound B6) and 2-methyl-5-(trifluoromethoxy)benzoic acid (compound F5) as starting compounds. The crude product is purified by chromatography (amino phase silica gel and DCM) and by crystallization from DCM and diethyl ether to yield the title compound.