Chemical process

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

Reexamination Certificate

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Details

C548S503000

Reexamination Certificate

active

07851623

ABSTRACT:
The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-[(4-fluoro-2-methy-1-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline starting from a compound of Formula IX:wherein R4is a protecting group; or an intermediate there between, using process steps, reagents and conditions as described.

REFERENCES:
patent: 2003/0220357 (2003-11-01), Bankston et al.
patent: 2004-269805 (2004-09-01), None
patent: 2006-024785 (2006-01-01), None
patent: WO 95/15758 (1995-06-01), None
patent: WO 00/47212 (2000-08-01), None
patent: WO 02/12227 (2002-02-01), None
patent: WO 03/064413 (2003-08-01), None
patent: WO 2004/009542 (2004-01-01), None
patent: WO 2005/061488 (2005-07-01), None
patent: WO 2005/097137 (2005-10-01), None
Sorbera et al. “Cediranib. VEGFR inhibitor, Antiangiogenic agent, Oncolytic” Drugs of the future 32(7): 577-589 (2007).
Doherty et al. “Synthesis of Aminoisothiuronium salts and their conversion to mercaptoalkylguanidines and thiazolines” Journal of the American Chemical Society 79: 5667-5671 (1957).

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