Diisopropylcarbodiimide → N-Cyclopropyl-4-methoxy-2,6-dimethyl-N-{[4-({4-[(1-methylpiperidin-4-yl)methyl]piperazin-1-yl}carbonyl)furan-2-yl]methyl}benzenesulfonamide

HRID 469035ノート

反応式

HRID 469035 の反応式
[CH:1]1([N:4]([CH2:18][C:19]2[O:23][CH:22]=[C:21]([C:24](O)=[O:25])[CH:20]=2)[S:5]([C:8]2[C:13]([CH3:14])=[CH:12][C:11]([O:15][CH3:16])=[CH:10][C:9]=2[CH3:17])(=[O:7])=[O:6])[CH2:3][CH2:2]1.[CH3:27][N:28]1[CH2:33][CH2:32][CH:31]([CH2:34][N:35]2[CH2:40][CH2:39][NH:38][CH2:37][CH2:36]2)[CH2:30][CH2:29]1.CC(C)N=C=NC(C)C.C1C=C2N=NN(O)C2=CC=1.O>C(Cl)Cl>[CH:1]1([N:4]([CH2:18][C:19]2[O:23][CH:22]=[C:21]([C:24]([N:38]3[CH2:37][CH2:36][N:35]([CH2:34][CH:31]4[CH2:32][CH2:33][N:28]([CH3:27])[CH2:29][CH2:30]4)[CH2:40][CH2:39]3)=[O:25])[CH:20]=2)[S:5]([C:8]2[C:9]([CH3:17])=[CH:10][C:11]([O:15][CH3:16])=[CH:12][C:13]=2[CH3:14])(=[O:6])=[O:7])[CH2:2][CH2:3]1

参加物

6

反応物 4

HCID 12734DiisopropylcarbodiimideHCID 27369421-((1-Methyl-4-piperidinyl)methyl)piperazineHCID 27960291-Hydroxybenzotriazole hydrateHCID 583933505-({Cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)furan-3-carboxylic acid

生成物 1

HCID 58393158N-Cyclopropyl-4-methoxy-2,6-dimethyl-N-{[4-({4-[(1-methylpiperidin-4-yl)methyl]piperazin-1-yl}carbonyl)furan-2-yl]methyl}benzenesulfonamide

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

The title compound was prepared according to general procedure AM using 5-({cyclopropyl[(4-methoxy-2,6 dimethylphenyl)sulfonyl]amino}methyl)furan-3-carboxylic acid (126 mg, 0.33 mmol), 1-[(1-methylpiperidin-4-yl)methyl]piperazine (59 mg, 0.30 mmol), DIC (79 μL, 0.5 mmol) and HOBt monohydrate (76 mg, 0.5 mmol) in DCM (2.5 mL). The crude product was purified by FCC eluting with 95:5 DCM:7N NH3 in MeOH.

後処理

  1. customThe crude product was purified by FCC
  2. washeluting with 95:5 DCM

出典と根拠

ORDレコード
ord-f00203ed808a4b9da22260b157a6b144
出典データセット
uspto-grants-2014_01
特許番号
US08623859B2

反応ノート

読み込み中…