反応 #2439979

ord-5066559d288e4aa8a7a0f5f6adcc9827

反応方程式

O=C1Nc2cc(C(=O)c3ccc(NC(=O)c4cccs4)cc3)ccc2C1=CO
Thiophene-2-carboxylic acid [4-(3-hydroxymethylene-2-oxo-2,3-dihydro-1H-indole-6-carbonyl)-phenyl]-amide
COc1ccc(N)cc1O
5-amino-2-methoxyphenol
COc1ccc(NC=C2C(=O)Nc3cc(C(=O)c4ccc(NC(=O)c5cccs5)cc4)ccc32)cc1O
title compound
収率 57.2%
COc1ccc(NC=C2C(=O)Nc3cc(C(=O)c4ccc(NC(=O)c5cccs5)cc4)ccc32)cc1O
Thiophene-2-carboxylic acid (4-{3-[(3-hydroxy-4-methoxy-phenylamino)-methylene]-2-oxo-2,3-dihydro-1H-indole-6-carbonyl}-phenyl)-amide
収率 57.2%

反応条件

温度
65°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他A small screw cap test tube
  2. 2
    温度Subsequently, the reaction mixture was cooled to room temperature
  3. 3
    その他The solid precipitate that formed

実験手順

A small screw cap test tube was charged with Thiophene-2-carboxylic acid [4-(3-hydroxymethylene-2-oxo-2,3-dihydro-1H-indole-6-carbonyl)-phenyl]-amide (as prepared in Example 20, 100 mg, 0.257 mmol) and THF (2 mL). To the resulting solution was added 5-amino-2-methoxyphenol (39.2 mg, 0.282 mmol), and the mixture was stirred for 24 h at 65° C. Subsequently, the reaction mixture was cooled to room temperature. Hexanes were added to the reaction mixture. The solid precipitate that formed was washed with ˜1 mL of i-prOH yielding 57% (75 mg, 0.147 mmol) of the title compound.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07749530B2uspto-grants-2010_07