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 469061노트

반응식

HRID 469061 반응식
[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

참가 물질

7

반응물 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

생성물 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

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-279c2212368149ae9bef432626d7388c
출처 데이터셋
uspto-grants-2014_01
특허 번호
US08623859B2

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