1-(Bromomethyl)-4-(trifluoromethyl)benzene → cis-2-[(4-Chlorobenzenesulfonyl)-(4-trifluoromethyl-benzyl)-amino]-cycloheptanecarboxylic acid amide

HRID 7046

反応式

HRID 7046 の反応式
[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([S:8]([NH:11][C@H:12]2[CH2:18][CH2:17][CH2:16][CH2:15][CH2:14][C@H:13]2[C:19]([NH2:21])=[O:20])(=[O:10])=[O:9])=[CH:4][CH:3]=1.Br[CH2:23][C:24]1[CH:29]=[CH:28][C:27]([C:30]([F:33])([F:32])[F:31])=[CH:26][CH:25]=1>>[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([S:8]([N:11]([CH2:23][C:24]2[CH:25]=[CH:26][C:27]([C:30]([F:31])([F:32])[F:33])=[CH:28][CH:29]=2)[C@H:12]2[CH2:18][CH2:17][CH2:16][CH2:15][CH2:14][C@H:13]2[C:19]([NH2:21])=[O:20])(=[O:9])=[O:10])=[CH:4][CH:3]=1

参加物

3

反応物 2

HCID 1230621-(Bromomethyl)-4-(trifluoromethyl)benzeneHCID 69656232cis-2-(4-Chlorobenzenesulfonylamino)-cycloheptanecarboxylic acid amide

生成物 1

HCID 69655570cis-2-[(4-Chlorobenzenesulfonyl)-(4-trifluoromethyl-benzyl)-amino]-cycloheptanecarboxylic acid amide収率 58%

実験手順

The titled compound (127 mg) was prepared in 58% yield from cis-2-(4-chlorobenzenesulfonylamino)-cycloheptanecarboxylic acid amide (150 mg, 0.45 mmol) and 1-bromomethyl-4-trifluoromethyl-benzene according to the N-alkylation procedure described in Example 11: 1H NMR (DMSO-d6) δ 7.80 (m, 2 H, J=8.0 Hz), 7.62 (m, 4 H), 7.52 (d, 2 H, J=8.0 Hz), 7.35 (s br, 1 H), 6.70 (s br, 1 H), 4.61 (AB2,2 H,Δv=20,Jab=104 Hz), 3.98 (m, 1 H), 2.80 (m, 1 H), 2.29 (m, 1 H), 1.74 (m, 2 H), 1.43 (m, 5 H), 1.22 (m, 2 H); MS m/e 511.05 (M+Na)+.

出典と根拠

ORDレコード
ord-6b5454ca797445e19ec258975c3d6f82
出典データセット
uspto-grants-2006_08
特許番号
US07084178B2

関連ノート

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