Phenylsulphonyl isocyanate → 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(2-{[(phenylsulfonyl)amino]carbonyl}-2,3-dihydro-1H-isoindol-5-yl)-1H-indole-7-carboxamide

HRID 1806515

反応式

HRID 1806515 の反応式
[CH2:1]1[C:9]2[C:4](=[CH:5][C:6]([C:10]3[CH:11]=[C:12]4[C:16](=[C:17]([C:19]([NH2:21])=[O:20])[CH:18]=3)[NH:15][CH:14]=[C:13]4[CH:22]3[CH2:27][CH2:26][N:25]([S:28]([CH2:31][CH3:32])(=[O:30])=[O:29])[CH2:24][CH2:23]3)=[CH:7][CH:8]=2)[CH2:3][NH:2]1.[C:33]1([S:39]([N:42]=[C:43]=[O:44])(=[O:41])=[O:40])[CH:38]=[CH:37][CH:36]=[CH:35][CH:34]=1>CS(C)=O>[CH2:31]([S:28]([N:25]1[CH2:26][CH2:27][CH:22]([C:13]2[C:12]3[C:16](=[C:17]([C:19]([NH2:21])=[O:20])[CH:18]=[C:10]([C:6]4[CH:5]=[C:4]5[C:9](=[CH:8][CH:7]=4)[CH2:1][N:2]([C:43]([NH:42][S:39]([C:33]4[CH:34]=[CH:35][CH:36]=[CH:37][CH:38]=4)(=[O:41])=[O:40])=[O:44])[CH2:3]5)[CH:11]=3)[NH:15][CH:14]=2)[CH2:23][CH2:24]1)(=[O:29])=[O:30])[CH3:32]

参加物

4

反応物 2

HCID 76096Phenylsulphonyl isocyanateHCID 42630496HCID 42630496、化合物

生成物 1

HCID 577327473-[1-(ethylsulfonyl)-4-piperidinyl]-5-(2-{[(phenylsulfonyl)amino]carbonyl}-2,3-dihydro-1H-isoindol-5-yl)-1H-indole-7-carboxamide収率 36.9%

試薬・触媒・溶媒 1

HCID 679Dimethyl Sulfoxide溶媒

実験手順

To a solution of 5-(2,3-dihydro-1H-isoindol-5-yl)-3-[1-(ethylsulfonyl)-4-piperidinyl]-1H-indole-7-carboxamide (30 mg, 0.066 mmol) in DMSO (1.0 mL), was added benzenesulfonyl isocyanate (15 mg, 0.079 mmol). The resultant mixture was stirred overnight at room temperature. Mixture purified by Gilson Preparatory HPLC to give 15.5 mg of the title compound.

後処理

  1. customMixture purified by Gilson Preparatory HPLC

出典と根拠

ORDレコード
ord-f16077c90462462a89871949a26336e2
出典データセット
uspto-grants-2013_01
特許番号
US08354406B2

関連ノート

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