5-(Difluoromethoxy)-2-methylbenzoic acid → 2-(1-{[5-(Difluoromethoxy)-2-methylphenyl]carbonyl}piperidin-4-yl)-5-(7-methoxy-3H-spiro[1-benzofuran-2,1'-cyclopentan]-4-yl)-4,4-dimethyl-2,4-dihydro-3H-pyrazol-3-one
反応式
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.[F:31][CH:32]([F:44])[O:33][C:34]1[CH:35]=[CH:36][C:37]([CH3:43])=[C:38]([CH:42]=1)[C:39](O)=[O:40]>>[F:31][CH:32]([F:44])[O:33][C:34]1[CH:35]=[CH:36][C:37]([CH3:43])=[C:38]([C:39]([N:25]2[CH2:26][CH2:27][CH:22]([N:20]3[C:19](=[O:28])[C:18]([CH3:30])([CH3:29])[C:17]([C:7]4[C:8]5[CH2:9][C:10]6([O:15][C:16]=5[C:4]([O:3][CH3:2])=[CH:5][CH:6]=4)[CH2:11][CH2:12][CH2:13][CH2:14]6)=[N:21]3)[CH2:23][CH2:24]2)=[O:40])[CH:42]=1参加物
3
反応物 2
生成物 1
実験手順
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 5-(difluoromethoxy)-2-methylbenzoic acid (compound F4) 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.
後処理
- customThe title compound is prepared analogously
- customThe crude product is purified by chromatography (amino phase silica gel and DCM) and by crystallization from DCM and diethyl ether
出典と根拠
- ORDレコード
- ord-fd9275f80460416c866ea06c89051edf
- 出典データセット
- uspto-grants-2013_12
- 特許番号
- US08609848B2
反応ノート
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