Natco Pharma (India)

<i>meta</i>-Chloroperbenzoic acid (mCPBA) is a readily available peroxide that is a powerful oxidizing agent utilized in a range of oxidative reactions. Metal-free oxidations mediated by mCPBA involving selective oxidation of aliphatic amines to oximes, selective oxidation of organosulphides/ aldehydes, synthesis of heterocyclic N-oxides, domino C[sp<sup>2</sup>] hydroxylation/ annulation of enaminones (heterocyclic ring formation), acid to phenol conversion, oxidation of exocyclic C=C bond, oxidative ring contraction, etc. have been comprehensively and critically examined in this review from 2015 to date.

This study reviews the oxidative applications of 2-iodoxybenzoic acid (IBX) in organic synthesis, focusing on C-H functionalization, hetero-hetero bond formations, ring cleavage reactions, dehydrogenation, heterocyclic ring formations, and some miscellaneous reactions in a comprehensive and critical way. It compiles the literature starting from mid-2015 to date.

Abstract: Dess-Martin periodinane (DMP) is one of the hypervalent iodines that is most frequently utilized as an oxidizing agent in organic chemistry. The authors of this septennial review have critically and methodically presented representative applications of DMP in organic synthesis from 2015 to the present, including oxidations, dehydrogenations, hetero and homo-dimerizations, aromatizations, thiocyanations, halogenations, dearylations, ring expansions, cyclizations, heterocyclic ring formation, and other miscellaneous reactions. This review discusses the range and constraints of these transformations.

Abstract Diacetoxyiodobenzene (PhI(OAc)2), commonly referred to asDAIBor phenyliodine(III) diacetate (PIDA), is one of the most frequently used hypervalent iodines employed as an oxidizing agent in organic chemistry. In this review,PIDAis highlighted exclusively in relation to its applications in organic synthesis involving heterocyclic ring formations and is critically and in‐depth examined from the summer of 2015 to the present with a specific focus on the mechanistic pathway.

In the present work, synthesis of phthalimide and naphthalimide derived Biginelli compounds was performed. Allylation of phthalic & naphthalic anhydride, followed by ozonolysis resulted in the formation of N-phathalimido/naphpthalimido acetaldehyde (2 and 7). These aldehydes were subjected to Biginelli reaction using urea/thiourea and divergent β-keto esters in the presence of sulfated tin oxide (5 mol%) as catalyst in ethanol reflux to produce the corresponding dihydropyrimidinone compounds (5a-j and 8a-h). Additionally, both their antioxidant and anti-inflammatory functions were carried out. Compounds 5e, 5f, 5i, and 5j have shown potent to moderate potent activity for both antioxidant and anti-inflamamtory activities when compared to standard. Compounds 8c and 8g have shown potent antioxidant and anti-inflamamtory activities when compared to other compounds.

Chemotherapeutics and biotherapeutics agents have been explored as a potential treatment for COVID-19. This study was aimed to elucidate latest update related to biotherapeutics and chemotherapeutics against COVID-19 and its variants as well as the product specifications and marketing dynamics of its pharmacotherapies. There are several chemotherapeutics that have been studied for the treatment of COVID-19, including Paxlovid (Nirmatrelvir & Ritonavir) fixed dose combination, nirmatrelvir and ritonavir fixed dose combination, Remdesivir (Vekulary/Covifor) fixed dose combination, chloroquine and hydroxychloroquine, molnupiravir, favipiravir, Infliximab (Remsima®) fixed dose combination tocilizumab (Actimera), casirivimab+imdevimab (Ronapreve) fixed dose combination, ivermectin, methylprednisole. These drugs have been repurposed for use in COVID-19 due to their antiviral properties and ability to reduce inflammation. The COVID-19 death cases have significantly reduced because of tested efficacy of advanced biotherapeutics and chemotherapeutics. As for marketing dynamics, the demand for chemotherapeutics for the treatment of COVID-19 has increased significantly since the outbreak of the pandemic. Hence, the prices of anti-viral and monoclonal antibodies in top COVID-19 affected countries is also presented here. Considering the molecular interactions, therapeutic activity, efficacy, and adverse effects, the USFDA and the WHO recommended the aforementioned drugs. The chances of approval seems favouring biotherapeutics as these have the best characteristics among the chemotherapeutics. Overall, this review contributes to the scientific understanding of the COVID-19. This can help to inform future research and development efforts and contribute to the overall advancement of knowledge in the field of medicine.

Abstract This work describes the highly efficient acetylation (acylation) of alcohols with acetic acid for the ester synthesis in the presence of newly designed a new composite zirconium (IV) chloride and magnesium catalyst which is used bimetallic acidic catalyst ZrCl4‐Mg(ClO4)2, which is formed by grinding ZrCl4 and Mg(ClO4)2 in the molar ratio of 1:2, respectively. Thus, the powder X‐ray diffraction, scanning electron microscopy, Brunauer–Emmett–Teller surface area, and thermogravimetric analysis of the ZrCl4, Mg(ClO4)2, and non‐calcined ZrCl4‐Mg(ClO4)2 were recorded. In each case, structural analysis was carried by grinding the catalyst in mortar and pestle.

: Zn(OAc)2•2H2O-catalyzed one-pot multicomponent reaction of Betti bases using β- naphthol, aldehydes, and amines, under neat conditions in moderate to excellent yields (68- 96%) is reported in this study. This synthetic protocol offers several advantages, such as operational simplicity, shorter reaction period, high yields, and easy work-up procedures.

An efficient metal-free domino reaction leading to structural/electronically divergent 1,2-dihydropyridines from easily accessible propargyl vinyl anilines via N-phenyl 3-aza-Cope sigmatropic rearrangement is reported with good to excellent yields using 1,2-dichlorobenzene as solvent under thermal conditions. Spirocyclic substitution is also tolerated under the present optimized conditions.