Current Organic Chemistry - Volume 4, Issue 7, 2000

The 4-(phenylamino)pyrimidine pharmacophore is found in a variety of different compounds that function as ATP-competitive inhibitors of several important protein kinase enzymes. Specific inhibitors of the epidermal growth factor receptor (EGFR) tyrosine kinase have received the most attention, and several elaborations of the fundamental 4-(phenyl­amino)­­pyrimidine pharma­co­phore have now been reported as potent a Read More

N-alkyl-1,2-benzenediamines, 4-substituted-3-nitro-1,2-benzenediamines and 3,4-diamino-2-nitrophenols are readily obtained by deselenation of alkyl quaternary salts of 2,1,3-benzoselenadiazoles (bsd) and 5-substituted-4-nitro-bsd. The latter are easily obtained by nitration of 5-X-bsd (X = Me, Br, Cl, F, OMe, NHMe). Nitration of 5-fluoro-bsd yields the 4-nitro derivatives that are accompanied by substantial amounts of the co Read More

This article presents a comprehensive review of synthetically useful intramolecular annulation reactions of nitrene and nitrenoid intermediates leading to heterocyclic compounds. Thermal, photochemical, and metal mediated reactions of aryl- and vinylazides, azirines, nitroso, and nitro compounds leading to synthetically useful yields of heterocycles are discussed.

The structures, origins, biogenesis, synthesis and bioactivity of a selection of N-heterocyclic marine alkaloids are reviewed. The emphasis is on compounds poised as potential anticancer drugs: lamellarins (pyrroles), cephalostatins/ritterazines (pyrazines) and ecteinascidins (isoquinolines). Also discussed are examples of bioactive marine alkaloids that have emerged as novel leads. These include manzamines (beta-carbolin Read More