NOPR Community:

P2O5-mediated Friedel-Crafts acylation of activated arenes with carboxylic acid as acylating agent

Tue, 01 Dec 2020 00:00:00 GMT

Title: P2O5-mediated Friedel-Crafts acylation of activated arenes with carboxylic acid as acylating agent Authors: Kalshetti, Rupali G; Mandle, Ram D; Kamble, Sanjay P; Sudalai, Arumugam Abstract: P₂O₅ has been found to be a highly efficient and environmental friendly catalyst for the liquid-phase acylation of activated aromatic substrates giving aromatic ketones (45-93%) in a regioselective manner. Both aromatic and aliphatic carboxylic acids can be employed as acylating source. The process is particularly demonstrated at 100 g scale in the case of anisole and acetic acid to produce 4-methoxyacetophenone. Page(s): 1861-1867

Synthetic approach to oxa-triquinanes via olefin metathesis as a key step

Tue, 01 Dec 2020 00:00:00 GMT

Title: Synthetic approach to oxa-triquinanes via olefin metathesis as a key step Authors: Kotha, Sambasivarao; Pulletikurti, Sunil Abstract: Earlier, a simple synthetic approach to cis, syn, cis-triquinanes and propellanes from exo-nadic anhydride through metathesis approach had been demonstrated. In the present work is discussed a distinct course of observations when this methodology has been extended to oxygenated exo-nadic anhydride derivatives and the importance of stereochemistry and the role of hetero atom in the outcome of olefin metathesis has been demonstrated. Page(s): 1868-1874

Synthesis of spiro-annulated cyclobutane derivatives through ketene [2+2] cycloaddition and ring-rearrangement metathesis

Tue, 01 Dec 2020 00:00:00 GMT

Title: Synthesis of spiro-annulated cyclobutane derivatives through ketene [2+2] cycloaddition and ring-rearrangement metathesis Authors: Kotha, Sambasivarao; Pulletikurti, Sunil Abstract: Herein is reported a concise synthesis of spiro-annulated cyclobutane tetracyclic and pentacyclic derivatives by ketene addition, and ring-rearrangement metathesis (RRM) as key steps, starting with commercially available norbornadiene and dicyclopentadiene. The tetracyclic spiro-derivative contains a [5/5/4] core unit, which is the key building block to angular triquinanes synthesis. Whereas, the pentacyclic spiro-derivative contains a basic core skeleton of presilphiperfolanes, and other sesquiterpenoids. Page(s): 1875-1880

QSAR of 1,3,5-triazine compounds towards inhibition of toxoplasmosis utilizing computed molecular descriptors

Tue, 01 Dec 2020 00:00:00 GMT

Title: QSAR of 1,3,5-triazine compounds towards inhibition of toxoplasmosis utilizing computed molecular descriptors Authors: Tanya; Nandi, Sisir Abstract: Growing attention has been focussed towards a considerable amount of experimental and theoretical study of anti toxoplasmosis compounds having inhibitory activities against toxoplasmosis. Toxoplasmosis is a dangerous disease in both urban as well as rural areas. It is caused by Toxoplasma gondii. The life cycle involves feline species such as both domestic and wild cats, and other felids such as lions, etc. There are various targets for developing anti toxoplasmosis agents. One of the most promising targets is dihydrofolate reductase (DHFR). 1,3,5-Triazine compounds have been reported to inhibit the T. gondii. But there is hardly any formulation of quantitative structure-activity relationship (QSAR) involving 1,3,5-triazine inhibitors to date. Therefore, it is our target in the present study to develop QSAR models based on the computed theoretical molecular descriptors to scale the essential features responsible for the DHFR inhibition. These screened features of the selected compounds will help to design the potent congeneric series. Page(s): 1881-1886