Formamide → Quinazoline

HRID 1803014

반응식

HRID 1803014 반응식
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

참가 물질

6

실험 절차

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.

출처 및 근거

ORD 기록
ord-03eb032aa21040a8a01c2c7707c6ff57
출처 데이터셋
uspto-grants-2013_01
특허 번호
US08350029B2

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