Sen S.,GVK Bioscience |
Kamma S.R.,GVK Bioscience |
Potti V.R.,GVK Bioscience |
Murthy Y.L.N.,Andhra University |
Chaudhary A.B.,GVK Bioscience
Tetrahedron Letters | Year: 2011
We report a facile diversity oriented synthesis of α- and β-amino acids, by utilizing the pluripotent α-methylene group in a chiral bicyclic lactam as our key point of transformation. © 2011 Elsevier Ltd. All rights reserved.
Mamidala R.,GVK Bioscience |
Babu Damerla V.S.,GVK Bioscience |
Gundla R.,GVK Bioscience |
Chary M.T.,Jawaharlal Nehru Technological University Anantapur |
And 2 more authors.
RSC Advances | Year: 2014
A versatile stereoselective diversity oriented synthetic pathway to the possible spiro and fused diverse heterocyclic small molecules is described. The strategy involved the "build-couple-pair" approach involving an S NAr, Michael addition and Mannich reaction on chiral acyl bicyclic lactams 2a/b, followed by a cyclization onto the inbuilt scaffold electrophile, thereby leading to asymmetric fused and spirocyclic nitrogen heterocycles. A "post-pair" phase has been incorporated to generate more polar compounds. We used Principal Component Analysis (PCA) and polar moment of inertia to evaluate the shape-space diversity of our scaffolds with respect to a commercial database and observed extraordinary diversity within the scaffold network. We further calculated the polar surface area (PSA) of our molecules which is an indicator for drug cell permeability. © 2014 The Royal Society of Chemistry.