Sai Prathima Parvathaneni

An atom-economical protocol for direct conversion of Baylis–Hillman alcohols to β-chloro aldehydes in water

This paper describes an atom-economical strategy for the direct conversion of Baylis–Hillman alcohols to β-chloro aldehydes under metal free conditions with excellent functional group tolerance. The use of stable-nontoxic Oxone as a terminal oxidant along with an inexpensive salt (sodium chloride) as a halogen source and water as the reaction medium makes this chemical synthetic process more viable and environmentally benign contributing towards green chemistry.

Iodosobenzoic Acid (IBA) Catalysed Benzylic and Aromatic C–H Oxidations

AbstractA metal-free reusable hypervalent iodine(III) reagent is employed as a stable catalyst for the selective oxidation of active methylenes, indoles and styrene C–H bond to corresponding carbonyl compounds. From both economic and environmental point of view use of 2-Iodosobenzoic acid for oxidations replacing metals, makes the reaction interesting.Graphical AbstractA metal-free reusable hypervalent iodine(III) reagent is employed as a stable catalyst for the selective oxidation of active methylenes, Indoles and styrene C–H bond to corresponding carbonyl compounds. From both an economic and environmental point of view use of oxygen as the oxidant, makes the reaction interesting.

PhI(OAc)2/NaX-mediated Halogenation Providing Access to Valuable Synthons 3-Haloindole derivatives

This paper describes a mild phenyliodine diacetate mediated method for selective chlorination, bromination, and iodination of indole C–H bonds using sodium halide as a source for analogous halogenations. The combination of NaX and phenyliodine diacetate provides an invincible system for halogenation of indoles. This protocol was compatible with a wide array of indole substrates and provides straight forward access to potential halogenated arenes.

Copper(I) Halide for Regioselective Ortho- Halogenation of Directed Arenes

We describe a copper(I) mediated halogenation via direct C–H functionalization of arenes. The combination of Cu(I)X and (diacetoxyiodo)benzene provides a robust system for halogenation of 2-arylpyridines. High regio- and mono-selectivity was achieved for chlorination, bromination, and iodination of arene C–H bonds.Graphical Abstract

Synthesis and Bioevaluation of Quaternary Centered 3-hydroxy-3 (alkynyl)indolin-2- one Derivatives as Potential Cytotoxic Agents and Akt Kinase Inhibitors

BACKGROUND Alkynes are fundamental building blocks in synthetic chemistry with high pharmaceutical applications. Among the bioactive acetylenic molecules, propargylic alcohol is most important as almost all the marketed drugs contains quaternary centered propargylic alcohol functionality. OBJECTIVE In this study we have synthesised and evaluated 3-hydroxy-3-ethynylindolin-2-one derivatives for in vitro cytotoxic activity. METHOD An expeditious method for direct alkynylation of isatins (ketones) has been developed using tetrabutylammonium fluoride (TBAF) as a catalyst in THF solvent at room temperature under metal-free conditions. Furthermore, this method is an economically viable process that also compliments green aspects like being a ligand/metal free process under ambient conditions. This reaction tolerated a wide range of substrates with good to excellent yields (80-94%). RESULTS The results showed that the synthesized compounds (4m, 4n and 4p) has the ability to inhibit Akt kinase activity with IC50 values ranging from 7.7 to 9.8 µM. CONCLUSION All the 3-hydroxy-3-ethynylindolin-2-one derivatives were subjected for in vitro cytotoxic activity on five different cancer cell lines. Further, the synthesized compounds (4m, 4n and 4p) were evaluated for their ability to inhibit Akt kinase activity and exhibited good inhibition with IC50 values ranging from 7.7 to 9.8 µM..