Benzenecarboximidamide, 4-hydroxy-, hydrochloride (1:1) → 3-[5-(4-Amidinophenoxycarbonyl)thiophen-2-yl]-2-methylpropenoic acid tert-butyl ester

HRID 332598

反応式

HRID 332598 の反応式
[C:1]([O:5][C:6]([C:8]([CH3:18])=[CH:9][C:10]1[S:14][C:13]([C:15]([OH:17])=[O:16])=[CH:12][CH:11]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2].Cl.O[C:21]1[CH:29]=[CH:28][C:24]([C:25]([NH2:27])=[NH:26])=[CH:23][CH:22]=1.CCN=C=NCCCN(C)C.Cl>N1C=CC=CC=1>[C:1]([O:5][C:6](=[O:7])[C:8]([CH3:18])=[CH:9][C:10]1[S:14][C:13]([C:15]([O:17][C:21]2[CH:29]=[CH:28][C:24]([C:25](=[NH:26])[NH2:27])=[CH:23][CH:22]=2)=[O:16])=[CH:12][CH:11]=1)([CH3:4])([CH3:2])[CH3:3]

参加物

5

反応物 3

HCID 217124Benzenecarboximidamide, 4-hydroxy-, hydrochloride (1:1)HCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 774784945-(2-(tert-Butoxycarbonyl)-1-propenyl)-2-thiophenecarboxylic acid

生成物 1

HCID 866733173-[5-(4-Amidinophenoxycarbonyl)thiophen-2-yl]-2-methylpropenoic acid tert-butyl ester収率 86.3%

試薬・触媒・溶媒 1

HCID 1049Pyridine溶媒

実験手順

5-(2-(tert-Butoxycarbonyl)-1-propenyl)-2-thiophenecarboxylic acid (0.51 g, 1.89 mmol) and 4-hydroxybenzamidine hydrochloride (0.33 g, 1.89 mmol) were dissolved in pyridine (10 mL), WSC hydrochloride (0.54 g, 2.8 mmol) was added, and the mixture was stirred overnight. The mixture was purified by high performance liquid chromatography and freeze-dried to give the title compound (0.63 g).

後処理

  1. customThe mixture was purified by high performance liquid chromatography
  2. customfreeze-dried

出典と根拠

ORDレコード
ord-5e0432ef141d42db9586f1e6a148c2eb
出典データセット
uspto-grants-2014_11
特許番号
US08877805B2

関連ノート

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