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2004
Fused pyrimidine derivatives
R 0515
Tandem Michael-Addition/Cyclization Synthesis and EGFR Kinase Inhibition
of Pyrido[2,3-d]pyrimidin-7(8H)-ones. — Propynoate (V) and pyrimidino44- 178 Activity
nes (VII) and (IX) are synthesized as alkynyl and conformationally constrained versions of a benzyloxyanilinoquinazoline containing substructure. Methoxy and anilinopyridopyrimidinones (VII) and (IX) are readily accessible from (V) by using the tandem Michael addition-cyclization procedure which incorporates the 5-substituent and
forms the pyridopyrimidinone ring in one step, furnishing the products in reasonable
yields without chromatography. Treatment of (V) with aminopyridine (X) yields the unacticipated product (XI) while reaction of (V) with imidazole (XII) affords the Michael-adduct (XIII). Compounds (V) and (IX) are submicromolar inhibitors of EGFR tyrosine kinase. — (BOROS*, E. E.; WOOD, E. R.; MCDONALD, O. B.; SPITZER, T.
D.; SEFLER, A. M.; REEP, B. R.; THOMPSON, J. B.; J. Heterocycl. Chem. 41
(2004) 3, 355-358; Dep. Med. Chem., GlaxoSmithKline Res. Dev., Research Triangle
Park, NC 27709, USA; Eng.) — H. Hoennerscheid
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