N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-nitroquinazolin-4-amine → N4-(3-Chloro-4-fluorophenyl)-7-methoxy-4,6-quinazolinediamine

HRID 500702ノート

反応式

HRID 500702 の反応式
[Cl:1][C:2]1[CH:3]=[C:4]([NH:9][C:10]2[C:19]3[C:14](=[CH:15][C:16]([O:23][CH3:24])=[C:17]([N+:20]([O-])=O)[CH:18]=3)[N:13]=[CH:12][N:11]=2)[CH:5]=[CH:6][C:7]=1[F:8]>[Ni].C1COCC1>[Cl:1][C:2]1[CH:3]=[C:4]([NH:9][C:10]2[C:19]3[C:14](=[CH:15][C:16]([O:23][CH3:24])=[C:17]([NH2:20])[CH:18]=3)[N:13]=[CH:12][N:11]=2)[CH:5]=[CH:6][C:7]=1[F:8]

参加物

4

反応物 1

HCID 21847811N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-nitroquinazolin-4-amine

生成物 1

HCID 21847826N4-(3-Chloro-4-fluorophenyl)-7-methoxy-4,6-quinazolinediamine収率 99%

試薬・触媒・溶媒 2

HCID 935Nickel触媒HCID 8028Tetrahydrofuran溶媒

実験手順

7.1 g of (3-Chloro-4-fluoro-phenyl)-(7-methoxy-6-nitro-quinazolin-4-yl)-amine was reduced using Raney nickel catalyst in THF, then filtered and evaporated to give 6.4 g N4-(3-Chloro-4-fluoro-phenyl)-7-methoxy-quinazoline-4,6-diamine (99% yield). This product was reacted with 4-Chloro-but-2-enoyl chloride as described in Scheme 1 to provide 4-Chloro-but-2-enoic acid [4-(3-chloro-4-fluoro-phenylamino)-7-methoxy-quinazolin-6-yl]-amide.

後処理

  1. filtrationfiltered
  2. customevaporated

出典と根拠

ORDレコード
ord-6fce9690bdba4702add5b871463c9db1
出典データセット
uspto-grants-2010_08
特許番号
US07772243B2

反応ノート

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