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An intramolecular palladium(II)-catalyzed dearomative arylation reaction of indoles via CH bond functionalization was developed, providing access to structurally novel spiroindolenines with moderate to good yields. A one-pot process for the synthesis of spiroindoline derivatives was also realized. [ABSTRACT FROM AUTHOR]

Abstract: Propylphosphonic anhydride (®T3P) promotes cyclization of o-aminobenzenethiol, o-aminophenol, and o-phenylenediamine with carboxylic acids under microwave irradiation. The one-pot procedure is efficient and allows short reaction times, easy workup, and good yields. Thus, we describe here a method for quick preparation of benzothiazoles, benzoxazoles and benzimidazoles. [Copyright &y& Elsevier]

A general method to synthesize N -aryl pyrrole derivatives was realized via the reactions of 2-(3-pyrroline-1-yl)arylaldehydes with indoles under acidic conditions, which underwent [1,5]-hydride shift/isomerization process. The desired products could be obtained in good to high yields with a wide substrate scope. [ABSTRACT FROM AUTHOR]

Abstract: All eight stereoisomers of saxagliptin have been synthesized and evaluated for their inhibitory activity against DPP-IV. It was unambiguously confirmed that the configuration of saxagliptin was critical to potent inhibition of DPP-IV. Docking study was performed to elucidate the configuration–activity relationship of saxagliptin stereoisomers. Tyr662 and Tyr470 have been suggested as the key residues of DPP-IV interacting with the inhibitors. This work provides valuable information for further inhibitor design against DPP-IV. [Copyright &y& Elsevier]