A facile two-step method for the construction of fused pyrrole ring leading to 5-substituted 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-1-ones via C-C followed by intramolecular C-N bond forming reaction is described. In vitro pharmacological evaluation and molecular modelling studies of some of the compounds synthesized are presented.

A one-pot Yb(III)-mediated cascade reaction has been developed leading to small molecules based on a novel structural motif, i.e. quinazolin-4-one moiety fused with an isoquinoline ring, for potential inhibition of TNF-α.

SummaryA bis-imine (prepared via a new FeCl3-based method) in combination with CoCl2 facilitated lipase-mediated acetylation of the (R)-isomer of a racemic benzylic secondary alcohol with 91% ees. The methodology was used for the preparation of the known drug rivastigmine.

Transition Metal Mediated Construction of Pyrrole Ring on 2,3-Dihydroquinolin-4(1H)-one: Synthesis and Pharmacological Evaluation of Novel Tricyclic Heteroarenes. -A new two-step synthesis of the title compounds includes C-C followed by intramolecular C-N bond forming reaction. The in vitro test of compound (IVf) exhibits significant SIRT1 activation. -(LAYEK, M.; REDDY, M. A.; RAO, A. V. D.; ALVALA, M.; ARUNASREE, M. K.; ISLAM, A.; MUKKANTI, K.; IQBAL*, J.; PAL, M.; Org. Biomol. Chem. 9 (2011) 4, 1004-1007, http://dx.doi.org/10.1039/c0ob00771d ; Inst. Life Sci., Univ. Hyderabad, Hyderabad 500 046, India; Eng.) -Bartels 25-159