The development of functional group transformations via ipso- substitution of boron moiety of aryl-, heteroaryl- and alkylboronic acids/esters utilizing the hypervalent organoiodine(III) reagents under transition metal-free reaction conditions is one of our prime focal areas. Various important functional moieties such as alcohol, nitro, primary amine, secondary amine, ether, cyano, azido, alkynyl etc. could be introduced through ipso-substitution of the boronic acids or of any other potential substrates. The interesting feature of this work is the utilization of two electron deficient species; boronic acids and hypervalent organoiodine in a proper way to provide different successful reaction products.

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2. Transition Metal-Catalyzed Chemo- and Regioselective Cycloadditions to Various Carbo-/Heterocycles using Bifunctional Reagents : 

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Transition metal-catalyzed [2+2+2] and [3+2] cycloadditions are highly efficient and straightforward routes to the synthesis of variety of fused carbo-/heterocycles and substituted triazoles. The work focusses at employing bifunctional reactant like alkynylnitriles and alkynylthiocyanates, containing both acetylene and nitrile/thiocyanate functionalities, for the development of a cycloaddition protocol in which by simple modification in the reaction conditions such as solvent, temperature, additive, catalyst etc., keeping the reactants and catalyst unchanged, both cyanoarenes/arylthiocyanates and 2-alkynylpyridines/2-thiosubstituted pyridines could be constructed in a chemoselective manner.

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3. Transition Metal-Catalyzed Synthesis of Heteroatom Substituted Carbo-/Heterocycles : 

Efforts are devoted towards the atom-economical synthesis of a variety of heteroatom substituted pyridines/benzenes (incorporating heteroatoms like boron, phosphorus, oxygen, sulphur and selenium) using transition metal-catalyzed [2+2+2] cycloadditions. Such structural forms are an integral part of various bioactive molecules and therefore, there is a need for facile and selective methods for their formation.

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4. Organo-Boron Chemistry in Cancer Therapy :

Boron neutron capture therapy (BNCT) is a promising chemo radiotherapeutic technique for the treatment of cancer by selective delivery of 10B-rich agents to cancer cells followed by irradiation with low-energy neutrons, resulting in highly localized nuclear fission reaction to release the energy that induces cell death. Since the energy deposition is limited to the diameter of a single cell, neoplastic cells with significant boron accumulation will be damaged following thermal neutron irradiation.

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Therapeutic efficacy of BNCT treatment has been demonstrated in patients with head and neck cancers, malignant meningeal tumors and hepatocellular carcinoma. The clinical efficacy of BNCT as cancer treating modality is ultimately limited by the random distribution and subcellular localization of the 10B-containing agents, absence of sound procedures for the prediction and estimation of radiobiological effectiveness, limited availability of suitable neutron sources etc. The important requirements of a BNCT delivery agent are low systemic toxicity, selective in targeting tumor cells, high tumor/brain and tumor/blood concentration ratios (>3-4:1), deliver the therapeutically optimal amount of approximately 109/10B atoms per cell, rapid clearance from blood and normal tissues and persistence in tumor during BNCT. The work involves 1) Development of effective novel targeted boron delivery agents. 2) Improve the efficiency of BPA by increasing its retention time by synthetic modifications. 3) Synthesizing 18F-labelled boronating agents and study the radiotherapeutic potential of the newly synthesized compounds in BNCT.

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