1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 2-({Cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-N-methyl-N-{[2-(pyrrolidin-1-ylmethyl)-1,3-thiazol-4-yl]methyl}-1,3-oxazole-4-carboxamide

HRID 469061ノート

反応式

HRID 469061 の反応式
[CH3:1][NH:2][CH2:3][C:4]1[N:5]=[C:6]([CH2:9][N:10]2[CH2:14][CH2:13][CH2:12][CH2:11]2)[S:7][CH:8]=1.[CH:15]1([N:18]([CH2:32][C:33]2[O:34][CH:35]=[C:36]([C:38]([OH:40])=O)[N:37]=2)[S:19]([C:22]2[C:27]([CH3:28])=[CH:26][C:25]([O:29][CH3:30])=[CH:24][C:23]=2[CH3:31])(=[O:21])=[O:20])[CH2:17][CH2:16]1.CCN(C(C)C)C(C)C.CCN=C=NCCCN(C)C.C1C=C2N=NN(O)C2=CC=1.O>CN(C=O)C>[CH:15]1([N:18]([CH2:32][C:33]2[O:34][CH:35]=[C:36]([C:38]([N:2]([CH3:1])[CH2:3][C:4]3[N:5]=[C:6]([CH2:9][N:10]4[CH2:14][CH2:13][CH2:12][CH2:11]4)[S:7][CH:8]=3)=[O:40])[N:37]=2)[S:19]([C:22]2[C:23]([CH3:31])=[CH:24][C:25]([O:29][CH3:30])=[CH:26][C:27]=2[CH3:28])(=[O:21])=[O:20])[CH2:17][CH2:16]1

参加物

7

反応物 5

HCID 159081-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 81531DiisopropylethylamineHCID 27960291-Hydroxybenzotriazole hydrateHCID 46785587N-methyl-1-[2-(pyrrolidin-1-ylmethyl)-1,3-thiazol-4-yl]methanamineHCID 583930982-({Cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-1,3-oxazole-4-carboxylic acid

生成物 1

HCID 583933672-({Cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-N-methyl-N-{[2-(pyrrolidin-1-ylmethyl)-1,3-thiazol-4-yl]methyl}-1,3-oxazole-4-carboxamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

The title compound was prepared according to general procedure AH using N-methyl-1-[2-(pyrrolidin-1-ylmethyl)-1,3-thiazol-4-yl]methanamine (40 mg, 189 μmol), 2-({cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-1,3-oxazole-4-carboxylic acid (72 mg, 189 μmol), DIPEA (0.1 mL, 575 μmol), EDCI (72 mg, 378 μmol), HOBt monohydrate (58 mg, 378 μmol) and DMF (1.5 mL). The resulting crude compound was purified by FCC eluting with 99:1 DCM:7N NH3 in MeOH.

後処理

  1. customThe resulting crude compound was purified by FCC
  2. washeluting with 99:1 DCM

出典と根拠

ORDレコード
ord-279c2212368149ae9bef432626d7388c
出典データセット
uspto-grants-2014_01
特許番号
US08623859B2

反応ノート

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