A novel, short, and efficient synthetic pathway to 3-{4-[2-(3-chlorophenylamino)-pyrimidin-4-yl]-pyridin-2-ylamino}-propanol (CGP 60474) and a series of analogues was developed. The synthetic sequence consisted of a Negishi-type cross-coupling reaction in the key step followed by two subsequent nucleophilic substitution reactions. This strategy represents a versatile and robust protocol to access diverse analogues of the title compound for subsequent SAR studies as potential phenylamino-pyrimidine type protein kinase C inhibitors.

The 1 H, 13 C, and 15 N shifts of 10 nitrogen-containing bi-and triaryls are reported, including the coupling constants of the fluoro substituents with all nuclei. The proton and carbon resonances of the hetaryl structures are completely assigned.

A straight forward synthesis of the 1,4,2‐benzodithiazine system bearing an ester functionality as potential inducers of systemic acquired resistance in plants was developed utilizing the ring expansion reaction of 1,3‐benzodithioles. The structure of the isomers obtained was established using x‐ray diffraction. The reactivity of the products towards activated alkynes and ring contraction reactions in the presence of base is discussed.

other 6-membered heterocycles other 6-membered heterocycles (with 3 or more heteroatoms) R 0670 -160Synthesis of 1,4,2-Benzodithiazine Carboxylates via Ring Expansion Reaction of 1,3-Benzodithioles.-In order to find a novel compound as potential inducer of systemic acquired resistance in plants the substance (VIII) is synthesized. The structure of the corresponding benzyl ester of (VIII) is determined by X-ray analysis. -(STANETTY, PETER; HATTINGER, GREGOR; MIHOVILOVIC, MARKO D.; MEREITER, KURT; J. Heterocycl. Chem. 37 (2000) 4, 955-958; Inst. Org. Chem., Tech. Univ., A-1060 Wien, Austria; EN)