Central Drug Research Institute

About: Central Drug Research Institute is a facility organization based out in Lucknow, Uttar Pradesh, India. It is known for research contribution in the topics: Leishmania donovani & Brugia malayi. The organization has 4357 authors who have published 7257 publications receiving 143871 citations. The organization is also known as: Central Drug Research Institute, Lucknow & CDRI.

Iron Nitrate/TEMPO: a Superior Homogeneous Catalyst for Oxidation of Primary Alcohols to Nitriles in Air

Abstract: A highly practical, one-step, facile synthesis of aromatic, heteroaromatic, allylic and aliphatic nitriles from primary alcohols catalyzed by ferric nitrate [Fe(NO3)3⋅9H2O] in the presence of TEMPO, aqueous ammonia and air at room temperature is described.

Synthesis of 3,4,5‐Trisubstituted Isoxazoles from Morita–Baylis–Hillman Acetates by an NaNO2/I2‐Mediated Domino Reaction

Abstract: An efficient NaNO2 /I2 -mediated one-pot transformation of Morita-Baylis-Hillman (MBH) acetates into alkyl 3-nitro-5-(aryl/alkyl)isoxazole-4-carboxylates is described. In a cascade event, initial Michael addition of NaNO2 to the MBH acetate furnishes the allylnitro intermediate which undergoes I2 -catalyzed oxidative α-CH nitration of the nitromethyl subunit followed by [3+2] cycloaddition to afford the title compounds. Structural elaborations of these highly substituted isoxazoles by SN Ar reactions and hydrogenolysis allows access to useful products.

Organocatalytic asymmetric Mannich cyclization of hydroxylactams with acetals: total syntheses of (-)-epilupinine, (-)-tashiromine, and (-)-trachelanthamidine.

Abstract: An asymmetric, organocatalytic, one-pot Mannich cyclization between a hydroxylactam and acetal is described to provide fused, bicyclic alkaloids bearing a bridgehead N atom. Both aliphatic and aromatic substrates were used in this transformation to furnish chiral pyrrolizidinone, indolizidi- none, and quinolizidinone derivatives in up to 89 % yield and 97 % ee. The total syntheses of (� )-epilupinine, (� )-tashir- omine, and (� )-trachelanthamidine also achieved to demon- strate the generality of the process. Naturally occurring izidine alkaloids (pyrrolizidine, indoli- zidine, and quinolizidine; Figure 1 A) and their synthetic variants are of considerable importance because of their diverse biological activities. (1) While the polyhydroxylated izidines inhibit glycosidase and glycosyl-transfer enzymes, and show anti-HIV, anti-dengue virus, anticancer, anti- inflammatory, and antidiabetic activities, (2) the alkylated