Hydrochloric Acid → 5-({[(4-chloro-2,5-dimethylphenyl)sulfonyl](methyl)amino}methyl)-N-{2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]ethyl}-N-methylfuran-3-carboxamide

HRID 469006ノート

反応式

HRID 469006 の反応式
[Cl:1][C:2]1[C:7]([CH3:8])=[CH:6][C:5]([S:9]([N:12]([CH2:14][C:15]2[O:19][CH:18]=[C:17]([C:20]([OH:22])=O)[CH:16]=2)[CH3:13])(=[O:11])=[O:10])=[C:4]([CH3:23])[CH:3]=1.C1N=CN(C(N2C=NC=C2)=O)C=1.[NH:36]1[CH2:40][CH2:39][N:38]=[C:37]1[C:41]1[CH:46]=[CH:45][C:44]([CH2:47][CH2:48][NH:49][CH3:50])=[CH:43][CH:42]=1.Cl.CCN(C(C)C)C(C)C>CN(C=O)C>[Cl:1][C:2]1[C:7]([CH3:8])=[CH:6][C:5]([S:9]([N:12]([CH2:14][C:15]2[O:19][CH:18]=[C:17]([C:20]([N:49]([CH2:48][CH2:47][C:44]3[CH:43]=[CH:42][C:41]([C:37]4[NH:38][CH2:39][CH2:40][N:36]=4)=[CH:46][CH:45]=3)[CH3:50])=[O:22])[CH:16]=2)[CH3:13])(=[O:11])=[O:10])=[C:4]([CH3:23])[CH:3]=1

参加物

7

反応物 5

HCID 313Hydrochloric AcidHCID 682631,1'-CarbonyldiimidazoleHCID 81531DiisopropylethylamineHCID 583930295-({[(4-Chloro-2,5-dimethylphenyl)sulfonyl](methyl)amino}methyl)furan-3-carboxylic acidHCID 672171912-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-N-methylethanamine

生成物 1

HCID 583930965-({[(4-chloro-2,5-dimethylphenyl)sulfonyl](methyl)amino}methyl)-N-{2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]ethyl}-N-methylfuran-3-carboxamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒2 回

実験手順

5-({[(4-chloro-2,5-dimethylphenyl)sulfonyl](methyl)amino}methyl)furan-3-carboxylic acid (30 mg, 0.08 mmol) was dissolved in DMF (1 mL) and CDI (20 mg, 0.12 mmol) was added. The mixture was stirred until acid activation was complete. 2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-N-methylethanamine.HCl (19 mg, 0.08 mmol) and DIPEA (0.042 mL, 0.24 mmol) were sonicated in DMF (1 mL) for 15 min, 0.5 mL of activated acid solution was added to 0.25 mL of amine solution and the reaction was microwaved (120° C., 200 W) for 20 min, then 2×60 min. A portion of the reaction was concentrated and purified using prep method A.

後処理

  1. customthe reaction was microwaved (120° C., 200 W) for 20 min
  2. custom2×60 min
  3. concentrationA portion of the reaction was concentrated
  4. custompurified

出典と根拠

ORDレコード
ord-4d14727ff2774839ac87213170d252f8
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…