2002 fused pyridine derivatives

fused pyridine derivativesR 0450

13 - 153An Anion-Induced Regio- and Chemoselective Acylation and ItsApplication to the Synthesis of an Anticancer Agent. — A numberof tricyclic ketones is prepared by a Grignard- and organolithium-induced regio-and chemoselective anionic acylation. This method is complementary to theFriedel–Crafts acylation for electron-deficient substrates. A novel anisole-basedGrignard reagent is used to effect the cyclization of sterically hindered sub-strates. Thus, the method allows the preparation of moiety (XIV) of Sch 66336.— (POIRIER, MARC; CHEN, FRANK; BERNARD, CHARLES; WONG,YEE-SHING; WU, GEORGE G.; Org. Lett. 3 (2001) 23, 3795-3798; Chem.Process Dev., Schering-Plough Res. Inst., Union, NJ 07083, USA; EN)

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