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

HRID 1820170노트

반응식

HRID 1820170 반응식
[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

참가 물질

6

반응물 3

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

생성물 1

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

시약·촉매·용매 2

HCID 887Methanol용매HCID 6344Dichloromethane용매

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-d801b4343de94278b94e906181c14093
출처 데이터셋
uspto-grants-2009_10
특허 번호
US07601844B2

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