Water → 4-[((1R)-1-{3-[(3-fluoro-4-methoxybenzoyl)amino]phenyl}ethyl)amino]quinazoline-8-carboxamide

HRID 578677

反応式

HRID 578677 の反応式
[NH2:1][C:2]1[CH:3]=[C:4]([C@H:8]([NH:10][C:11]2[C:20]3[C:15](=[C:16]([C:21]([NH2:23])=[O:22])[CH:17]=[CH:18][CH:19]=3)[N:14]=[CH:13][N:12]=2)[CH3:9])[CH:5]=[CH:6][CH:7]=1.[F:24][C:25]1[CH:26]=[C:27]([CH:31]=[CH:32][C:33]=1[O:34][CH3:35])[C:28](Cl)=[O:29].O>N1C=CC=CC=1>[F:24][C:25]1[CH:26]=[C:27]([CH:31]=[CH:32][C:33]=1[O:34][CH3:35])[C:28]([NH:1][C:2]1[CH:3]=[C:4]([C@H:8]([NH:10][C:11]2[C:20]3[C:15](=[C:16]([C:21]([NH2:23])=[O:22])[CH:17]=[CH:18][CH:19]=3)[N:14]=[CH:13][N:12]=2)[CH3:9])[CH:5]=[CH:6][CH:7]=1)=[O:29]

参加物

5

反応物 3

HCID 962WaterHCID 27792553-Fluoro-4-methoxybenzoyl chlorideHCID 667628924-{[(1R)-1-(3-aminophenyl)ethyl]amino}quinazoline-8-carboxamide

生成物 1

HCID 667623114-[((1R)-1-{3-[(3-fluoro-4-methoxybenzoyl)amino]phenyl}ethyl)amino]quinazoline-8-carboxamide収率 98%

試薬・触媒・溶媒 1

HCID 1049Pyridine溶媒

実験手順

A suspension of 4-{[(1R)-1-(3-aminophenyl)ethyl]amino}quinazoline-8-carboxamide (2.0 g, 6.51 mmol) in dry pyridine (50 mL) was treated with 3-fluoro-4-methoxybenzoyl chloride (1.51 g, 8.01 mmol, 1.23 eq), and the contents were stirred at room temp for 45 min. The clear-yellow solution was slowly added to water (1000 mL), and the white precipitate was filtered, washed with water (300 mL) and dried under vacuum at 35° C. to get the title compound in 98% yield (2.93 g).

後処理

  1. filtrationthe white precipitate was filtered
  2. washwashed with water (300 mL)
  3. customdried under vacuum at 35° C.

出典と根拠

ORDレコード
ord-ce3f7c298a474967b172d856ac7c97ef
出典データセット
uspto-grants-2015_05
特許番号
US09040560B2

関連ノート

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