Phenylmethanesulfonyl chloride → N-(1-(4-(4-Chlorophenyl)piperidin-1-yl)-3-methyl-1-oxobutan-2-yl)(phenyl)methanesulfonamide

HRID 1820170ノート

反応式

HRID 1820170 の反応式
[CH2:1]([S:8](Cl)(=[O:10])=[O:9])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.CCN(C(C)C)C(C)C.Cl.[NH2:22][CH:23]([CH:39]([CH3:41])[CH3:40])[C:24]([N:26]1[CH2:31][CH2:30][CH:29]([C:32]2[CH:37]=[CH:36][C:35]([Cl:38])=[CH:34][CH:33]=2)[CH2:28][CH2:27]1)=[O:25]>C(Cl)Cl.CO>[Cl:38][C:35]1[CH:36]=[CH:37][C:32]([CH:29]2[CH2:28][CH2:27][N:26]([C:24](=[O:25])[CH:23]([NH:22][S:8]([CH2:1][C:2]3[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=3)(=[O:10])=[O:9])[CH:39]([CH3:41])[CH3:40])[CH2:31][CH2:30]2)=[CH:33][CH:34]=1

参加物

6

反応物 3

HCID 74740Phenylmethanesulfonyl chlorideHCID 81531DiisopropylethylamineHCID 672994912-Amino-1-(4-(4-chlorophenyl)piperidin-1-yl)-3-methylbutan-1-one hydrochloride

生成物 1

HCID 57888688N-(1-(4-(4-Chlorophenyl)piperidin-1-yl)-3-methyl-1-oxobutan-2-yl)(phenyl)methanesulfonamide

試薬・触媒・溶媒 2

HCID 887Methanol溶媒HCID 6344Dichloromethane溶媒

実験手順

A reaction tube was charged with benzylsulfonyl chloride (14 mg), DIEA (50 μL) and 2-amino-1-(4-(4-chlorophenyl)piperidin-1-yl)-3-methylbutan-1-one hydrochloride (20 mg) in DCM (0.3 mL). The reaction mixture was shaken overnight at rt. At the conclusion of this period, the resulting solution was diluted with MeOH and purified by preparative LC-MS to provide Example 200. MS found: (M+H)+=450.

後処理

  1. custompurified by preparative LC-MS
  2. customto provide Example 200

出典と根拠

ORDレコード
ord-d801b4343de94278b94e906181c14093
出典データセット
uspto-grants-2009_10
特許番号
US07601844B2

反応ノート

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