反応式
Cl[C:2]1[C:11]2[C:6](=[CH:7][C:8]([F:15])=[C:9]([N+]([O-])=O)[CH:10]=2)[N:5]=[CH:4][N:3]=1.NC1C=C(F)C=CC=1C(O)=[O:20].C(N)=N.C(O)(=O)C>COCCO>[F:15][C:8]1[CH:7]=[C:6]2[C:11]([C:2](=[O:20])[NH:3][CH:4]=[N:5]2)=[CH:10][CH:9]=1参加物
実験手順
4-Chloro-7-fluoro-6-nitroquinazoline (7) can be prepared by methods similar to those described in J. Med. Chem. 1996, 39, 918-928. Generally, 2-amino-4-fluoro-benzoic acid (1) can be reacted with formamidine (2) and acetic acid (3) in the presence of 2-methoxyethanol to provide 7-Fluoro-3H-quinazolin-4-one (4). The 7-fluoro-3H-quinazolin-4-one (4) can then be nitrated to 7-fluoro-6-nitro-3H-quinazolin-4-one (5), which can be treated with thionyl chloride to yield 4-chloro-6-nitro-7-fluoro-3H-quinazoline (6). The 4-chloro-quinazoline compound (6) can be combined with a desirably substituted aniline, represented above by 4-fluoro-3-chloro-aniline, in the presence of a tertiary amine and isopropanol to provide the 4-anilino-6-nitro-7-fluoro-quinazoline (7).
出典と根拠
- ORDレコード
- ord-5939c849420149fa8a0b323f9319daef
- 出典データセット
- uspto-grants-2014_01
- 特許番号
- US08623883B2
関連ノート
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