O-Xylene → 5-Allyl-4-(3-chloro-4-fluoro-phenylamino)-7-methoxy-quinazolin-6-ol

HRID 1351210ノート

反応式

HRID 1351210 の反応式
C([O:4][C:5]1[CH:6]=[C:7]2[C:12](=[CH:13][C:14]=1[O:15][CH3:16])[N:11]=[CH:10][N:9]=[C:8]2[NH:17][C:18]1[CH:23]=[CH:22][C:21]([F:24])=[C:20]([Cl:25])[CH:19]=1)C=C.[CH3:26][C:27]1C=CC=C[C:32]=1C>>[CH2:32]([C:6]1[C:5]([OH:4])=[C:14]([O:15][CH3:16])[CH:13]=[C:12]2[C:7]=1[C:8]([NH:17][C:18]1[CH:23]=[CH:22][C:21]([F:24])=[C:20]([Cl:25])[CH:19]=1)=[N:9][CH:10]=[N:11]2)[CH:27]=[CH2:26]

参加物

3

反応物 2

HCID 7237O-XyleneHCID 21098401(6-Allyloxy-7-methoxy-quinazolin-4-yl)-(3-chloro-4-fluoro-phenyl)-amine

生成物 1

HCID 114625295-Allyl-4-(3-chloro-4-fluoro-phenylamino)-7-methoxy-quinazolin-6-ol

実験手順

A solution of (6-allyloxy-7-methoxy-quinazolin-4-yl)-(3-chloro-4-fluoro-phenyl)-amine (0.92 g, 2.55 mmol) (from Example 18, Step C, supra) in o-xylene (150 mL) was heated at 150° C. for 7 hours. At the end of this period, TLC analysis indicated almost complete consumption of the starting material and the formation of desired product as the major spot. The solution was concentrated and filtered. The solid was collected and dried in vacuo to give the desired 5-allyl-4-(3-chloro-4-fluoro-phenylamino)-7-methoxy-quinazolin-6-ol as an off white solid. (Yield 0.65 g, 71%).

後処理

  1. customconsumption of the starting material
  2. concentrationThe solution was concentrated
  3. filtrationfiltered
  4. customThe solid was collected
  5. customdried in vacuo

出典と根拠

ORDレコード
ord-09ea2d8b417a48c78b48bc0f6ef45f3b
出典データセット
uspto-grants-2007_05
特許番号
US07217717B2

反応ノート

読み込み中…