Methanesulfonyl chloride → N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-4-(methanesulfonylamino)methyl-N-(2-methoxyphenyl)benzamide

HRID 2504

反応式

HRID 2504 の反応式
[NH2:1][CH2:2][C:3]1[CH:36]=[CH:35][C:6]([C:7]([N:9]([CH2:18][CH2:19][N:20]2[CH2:25][CH2:24][CH:23]([C:26](=[O:34])[C:27]3[CH:32]=[CH:31][C:30]([F:33])=[CH:29][CH:28]=3)[CH2:22][CH2:21]2)[C:10]2[CH:15]=[CH:14][CH:13]=[CH:12][C:11]=2[O:16][CH3:17])=[O:8])=[CH:5][CH:4]=1.[CH3:37][S:38](Cl)(=[O:40])=[O:39]>>[F:33][C:30]1[CH:29]=[CH:28][C:27]([C:26]([CH:23]2[CH2:24][CH2:25][N:20]([CH2:19][CH2:18][N:9]([C:10]3[CH:15]=[CH:14][CH:13]=[CH:12][C:11]=3[O:16][CH3:17])[C:7](=[O:8])[C:6]3[CH:5]=[CH:4][C:3]([CH2:2][NH:1][S:38]([CH3:37])(=[O:40])=[O:39])=[CH:36][CH:35]=3)[CH2:21][CH2:22]2)=[O:34])=[CH:32][CH:31]=1

参加物

3

反応物 2

HCID 31297Methanesulfonyl chlorideHCID 196898594-aminomethyl-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(2-methoxyphenyl)benzamide

生成物 1

HCID 19689935N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-4-(methanesulfonylamino)methyl-N-(2-methoxyphenyl)benzamide収率 57.5%

実験手順

Using 4-aminomethyl-N-{2-[4-(4-fluorobenzoyl)piperidino]-ethyl}-N-(2-methoxyphenyl)benzamide (60 mg, 0.123 mmol) and methanesulfonyl chloride (11 μl, 0.142 mmol), the procedure of Inventive Example 94 was repeated to obtain 40 mg (57.5%) of the title compound in a colorless amorphous form.

出典と根拠

ORDレコード
ord-19a9af2199cc4a38989a98f4ca8a5f8d
出典データセット
uspto-grants-1998_03
特許番号
US05728835

関連ノート

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