Piperidine → (4R)-1-(5-chloro-3-[2-methoxy-5-(2-piperidin-1-ylethyl)phenyl]-1-{[4-methoxy-2-(trifluoromethoxy)phenyl]sulfonyl}-2-oxo-2,3-dihydro-1H-indol-3-yl)-4-hydroxy-N,N-dimethyl-L-prolinamide

反応式

[Cl:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[N:7]([S:11]([C:14]1[CH:19]=[CH:18][C:17]([O:20][CH3:21])=[CH:16][C:15]=1[O:22][C:23]([F:26])([F:25])[F:24])(=[O:13])=[O:12])[C:6](=[O:27])[C:5]2([N:39]1[CH2:48][C@H:47]([OH:49])[CH2:46][C@H:40]1[C:41]([N:43]([CH3:45])[CH3:44])=[O:42])[C:28]1[CH:33]=[C:32]([CH2:34][CH:35]=O)[CH:31]=[CH:30][C:29]=1[O:37][CH3:38].[NH:50]1[CH2:55][CH2:54][CH2:53][CH2:52][CH2:51]1>>[Cl:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[N:7]([S:11]([C:14]1[CH:19]=[CH:18][C:17]([O:20][CH3:21])=[CH:16][C:15]=1[O:22][C:23]([F:25])([F:24])[F:26])(=[O:12])=[O:13])[C:6](=[O:27])[C:5]2([N:39]1[CH2:48][C@H:47]([OH:49])[CH2:46][C@H:40]1[C:41]([N:43]([CH3:44])[CH3:45])=[O:42])[C:28]1[CH:33]=[C:32]([CH2:34][CH2:35][N:50]2[CH2:55][CH2:54][CH2:53][CH2:52][CH2:51]2)[CH:31]=[CH:30][C:29]=1[O:37][CH3:38]

参加物

反応物 2

HCID 8082Piperidine

HCID 59867806HCID 59867806、化合物

生成物 1

HCID 59867945(4R)-1-(5-chloro-3-[2-methoxy-5-(2-piperidin-1-ylethyl)phenyl]-1-{[4-methoxy-2-(trifluoromethoxy)phenyl]sulfonyl}-2-oxo-2,3-dihydro-1H-indol-3-yl)-4-hydroxy-N,N-dimethyl-L-prolinamide収率 38%

実験手順

With 600 mg of the compound obtained in Example 219 and 129 mg of piperidine as starting materials, 250 mg of the title compound (light yellow amorphous) was obtained by a similar method to Example 220.

出典と根拠

ORDレコード: ord-576f2fe24c084d5d91fffed61f93e37a
出典データセット: uspto-grants-2011_10
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08030499B2

反応ノート

読み込み中…