&ldquo;IIT Jodhpur is committed to impart quality education to facilitate the creation of qualified, competent and responsible human resources to meet the emerging technological challenges of the world. It is working towards creating an equitable learning platform that is positive, accessible and effective in the face of the modern societal and scientific advancements.

Flexibility in curriculum, in all its academic programs, encompassing elements of teaching, research, creativity, innovation and entrepreneurship is the most unique feature of IIT Jodhpur. The Department of Science and Technology (DST), under the National Mission on Cyber Physical Systems, has identified IIT Jodhpur as a Technology &amp; Innovation Hub in the area of Augmented Reality and Virtual Reality. The institute has also been nominated as the coordinator for the Jodhpur City and Knowledge Cluster by the Office of Principal Scientific Adviser, Government of India.

The sprawling 852-acre IIT Jodhpur campus is a majestic tribute to the deep-rooted diverse cultural heritage of the region. The campus is an architectural masterpiece, which is slated to become an international exemplar of sustainability with net-zero energy, and advanced water and waste management strategies.&rdquo;

IIT Jodhpur

K-Ras is one of the most frequently mutated signal transducing human oncogenes. Ras signaling activity requires correct cellular localization of the GTPase. The spatial organization of K-Ras is controlled by the prenyl binding protein PDEδ, which enhances Ras diffusion in the cytosol. Inhibition of the Ras-PDEδ interaction by small molecules impairs Ras localization and signaling. Here we describe in detail the identification and structure guided development of Ras-PDEδ inhibitors targeting the farnesyl binding pocket of PDEδ with nanomolar affinity. We report kinetic data that characterize the binding of the most potent small molecule ligands to PDEδ and prove their binding to endogenous PDEδ in cell lysates. The PDEδ inhibitors provide promising starting points for the establishment of new drug discovery programs aimed at cancers harboring oncogenic K-Ras. © 2014 American Chemical Society.

World University root node

Department of Chemistry

Journal of Medicinal Chemistry

Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site

A simple and efficient direct radical arylation of unactivated arenes is described which uses cheap and commercially available phenyl hydrazine as an initiator. The reaction occurs through a base promoted homolytic aromatic substitution (BHAS) mechanism involving aryl radicals and aryl radical anions as intermediates and offers a practical approach for preparation of an array of substituted biaryls. © 2013 American Chemical Society.

Fulltext

Organic Letters

Phenyl hydrazine as initiator for direct arene C-H arylation via base promoted homolytic aromatic substitution

Radicals and anions: The TEMPO-mediated oxidation of magnesiated iodoarenes A provides highly regioregular poly(m-phenylenes) by strictly alternating anionic/radical cross-over chain-growth polymerization. Poly(m-phenylenes) with mean molecular weight (Mn) of up to 20 000 g mol-1 can be prepared under mild conditions by this method. The approach is a new concept for transition-metal-free polyarene synthesis. TEMPO=2,2,6,6-tetramethylpiperidine- N-oxyl radical. Copyright © 2012 WILEY-VCH Verlag GmbH &amp; Co. KGaA, Weinheim.

Angewandte Chemie - International Edition

Radical/anionic SRN1-type polymerization for preparation of oligoarenes

The application of nitroxides for the development of new synthetic methods and their implementation in polymer chemistry, material science and beyond is one of the major research topics in our laboratory in the institute of organic chemistry at the WWU Münster. This short review focuses on our recent progress towards nitroxidebased transition-metal-free oxidative coupling reactions. The demand for organic surrogates for transition metals in such transformations is in our eyes unquestionable, since environmental and economic issues have become progressively more important in recent years. For this purpose, the 2,2,6,6-tetramethylpiperidine-N-oxyl radical (TEMPO) is shown to be a highly efficient oxidant for the homo- and cross-coupling of Grignard reagents. This powerful C-C bond forming strategy allows the generation of conjugated polymers from bifunctional Grignard reagents. Moreover, cross-coupling of alkynyl Grignard compounds and nitrones can be accomplished under aerobic atmosphere with catalytic amounts of TEMPO. It is also shown that TEMPO-derived N-oxoammonium salts can act as suitable oxidants for formation of C-N bonds between non-preactivated benzoxazoles and secondary amines under metal-free conditions. © Schweizerische Chemische Gesellschaft.

Chimia

Transition-metal-free oxidative coupling reactions for the formation of C-C and C-N bonds mediated by TEMPO and its derivatives

An efficient mild one-pot protocol for the cross-coupling of nitrones and alkynyl-magnesium compounds using a catalytic amount of 2,2,6,6- tetramethylpiperidine-N-oxyl radical (TEMPO) as an environmentally benign organic oxidant and dioxygen as terminal oxidant is described. These coupling reactions can be performed without adding any transition metal on various N-tert-butylnitrones and alkynyl-Grignard reagents. Moreover, the alkynylated nitrone products are readily transformed to regioisomerically pure 3,5-disubstituted isoxazoles. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Advanced Synthesis and Catalysis

Transition metal-free TEMPO-catalyzed oxidative cross-coupling of nitrones with alkynyl-grignard reagents

A mild, operationally simple cross-dehydrogenative coupling between nitrones and terminal alkynes is described by using cheap, readily available 3,3′,5,5′-tetra-tert-butyldipheno-quinone and dioxygen as oxidants. These cross-couplings can be performed on various nitrones and alkynes with good to excellent yields. Product nitrones are readily transformed to pharmaceutically important 3,5-disubstituted isoxazoles. © 2011 American Chemical Society.

Zinc triflate catalyzed aerobic cross-dehydrogenative coupling (CDC) of alkynes with nitrones: A new entry to isoxazoles

Cross coupling of aryl, alkenyl, and alkynyl magnesium compounds by using 2,2,6,6-tetramethylpiperidine-N-oxyl radical (TEMPO) as an environmentally benign organic oxidant is described. This coupling reaction can be performed without adding any transition metal on various ortho-substituted aryl and alkynyl Grignard reagents. Importantly, functional groups such as esters, amides, and cyanides are shown to be tolerated under the reaction conditions. © 2010 American Chemical Society.

Transition-metal-free sonogashira-type coupling of ortho-substituted aryl and alkynyl grignard reagents by using 2,2,6,6-tetramethylpiperidine-N-oxyl radical as an oxidant

(Chemical Equation Presented) The first example of a catalytic enantioselective intramolecular hydride shift/ring closure reaction is reported. This redox neutral reaction cascade allows for the efficient formation of ring-fused tetrahydroquinolines in high enantioselectivities. © 2009 American Chemical Society.

Journal of the American Chemical Society

Catalytic enantioselective intramolecular redox reactions: Ring-fused tetrahydroquinolines

(Chemical Equation Presented) Cyclic aminals were prepared through a Brønsted acid-promoted reaction. This redox neutral process involves iminium ion formation, 1,5 H-transfer, followed by ring closure. © 2009 American Chemical Society.

Journal of Organic Chemistry

Facile formation of cyclic aminals through a Brønsted acid-promoted redox process

Polycyclic tetrahydroquinolines were prepared by an efficient Lewis acid catalyzed 1,5-hydride shift, ring closure sequence. Gadolinium triflate was identified as a catalyst that is superior to scandium triflate as well as other Lewis acids. An approach toward a catalytic enantioselective variant is also described. © 2009 American Chemical Society.