反応式
CO[C:3]1[CH:4]=[C:5]2[N:22]=[CH:21][N:20]=[C:19](NC3C=CC(F)=C(Cl)C=3)[C:6]2=[CH:7][C:8]=1OCCCN1CCOCC1.OC1C=C(C=CC=1OC)C#N.O1CCN(CCCCl)CC1.S(S([O-])=O)([O-])=O.[Na+].[Na+].C(N)=O>>[N:22]1[C:5]2[C:6](=[CH:7][CH:8]=[CH:3][CH:4]=2)[CH:19]=[N:20][CH:21]=1参加物
6
実験手順
WO 2004/024703 discloses a process for the preparation of gefitinib starting from 3-hydroxy-4-methoxy benzonitrile which involves condensation of 3-hydroxy-4-methoxy benzonitrile with morpholino propyl chloride, nitration, reduction with sodium dithionite to amino compound, hydrolysis of nitrile to amide, cyclisation in the presence of formamide to obtain quinazoline, chlorination with phosphorous oxychloride and finally condensation with chloro-fluoro aniline to obtain gefitinib. The process involves multiple steps and hence is time consuming.
出典と根拠
- ORDレコード
- ord-03eb032aa21040a8a01c2c7707c6ff57
- 出典データセット
- uspto-grants-2013_01
- 特許番号
- US08350029B2
関連ノート
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