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

HRID 467610노트

반응식

HRID 467610 반응식
[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]

참가 물질

4

반응물 1

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

생성물 1

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

시약·촉매·용매 2

HCID 935Nickel촉매HCID 8028Tetrahydrofuran용매

실험 절차

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.

후처리

  1. filtrationfiltered
  2. customevaporated

출처 및 근거

ORD 기록
ord-d6f336a46b874fbfb2ede5451ddb1aec
출처 데이터셋
uspto-grants-2014_01
특허 번호
US08623883B2

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