Jhillu Singh Yadav

Herein, we demonstrate an efficient amidation strategy employing aldehyde‐bisulfite adducts with aliphatic/aromatic amines mediated by sodium chlorite. Unlike Lindgren oxidation, this method operates under acid‐free conditions and addresses issues of aldehyde oxidation, which remains a concern with sodium chlorite. This strategy enables a broader scope of both aliphatic and aromatic amines, furnishing useful products in very good to excellent yields. The gram‐scale synthesis demonstrates the protocol's scalability, while applying the strategy to synthesize ester and benzothiazole derivatives broadens the scope for further applications.

2,3‐Diphenylacrylonitriles are widely used in synthetic and medicinal chemistry and have attracted considerable attention for their accessibility. Their synthetic approaches primarily employ metal‐catalyzed coupling reactions between arylacetonitriles and alcohols. Herein, we present an attractive strategy for the synthesis of ( Z )‐2,3‐diarylacrylonitrile derivatives by acceptorless cross‐dehydrogenative coupling between arylacetonitrile and benzyl bromide through isothiouronium salts. This α‐olefination method is operationally simple and proceeds under open‐air, metal‐free conditions. With a broader substrate scope and high product yields, the developed protocol offers a useful strategy for synthesizing acrylonitrile derivatives for further academic and industrial exploration.

Thioamide‐containing molecules represent a valuable class of candidates widely utilized in medicinal chemistry and hence have attracted great attention. Herein, we disclose an efficient protocol for the transformation of aryl and alkyl acetonitriles to their corresponding thioamides with elemental sulfur and malonic acid in the presence of a base. The developed protocol offers advantage of broader substrate scope and operates under operationally simple conditions, delivering high yield of products in just one hour. The observations from test experiments reveals malonic acid as hydrogen donor, and found essential for this thioamidation reaction. The gram‐scale synthesis demonstrates the scalability of the method, whereas further synthetic transformation highlights synthetic potentials of derivatives.

Herein, we present a quick and efficient method for the synthesis of trans ‐cinnamic acid employing DBU as a base in the presence of elemental sulfur. Without the requirement of any chromatographic purification, the developed method offers a broader scope of aldehyde and furnishes products with very good to excellent yields. The role of elemental sulfur was found to be substantial, as without elemental sulfur, the progress of the reaction was observed to be slow. The scalability of the reaction was demonstrated by performing gram‐scale synthesis, whereas the transformation of trans ‐cinnamic acid to thioamide derivative highlights the synthetic utility of the method.

Bempedoic acid is an oral medication for hypercholesterolemia, a disorder, if not controlled could lead to severe heart disease. Therefore, several synthetic approaches have been developed for Bempedoic acid. Herein, we wish to report an efficient synthesis of bempedoic acid utilizing Grignard reaction on ethyl formate serving as one carbon synthon. The highlights of the synthesis is double Grignard reagent addition on ethyl formate furnishing required secondary alcohol which is otherwise obtained by reduction of carbonyl. The developed synthetic route employs pentane‐1,5‐diol as starting precursor and Bempedoic acid is achieved in nine steps with 33% overall yield with all steps with very good to excellent yields.

Pyrimidine‐2,4(1 H ,3 H )‐dione derivatives serve as feedstock chemicals in the drug discovery process due to their structural analogy with pyrimidine bases and therefore have largely attracted attention to develop synthetic protocol. Herein, we report an effective aroylation strategy of cyclic vinamidinium salt employing aromatic aldehydes utilizing thiazolium salt as N ‐heterocyclic carbene precursor delivering 6‐aroyl‐1,3‐dimethylpyrimidine‐2,4( 1H , 3H )‐dione derivatives. The developed protocol employs operationally simple experimental conditions and furnishes good to very good yield of medicinally relevant products.

The development of synthetic approaches leading to 2,3‐Dihydroquinazolin‐4(1 H )‐one derivatives is one of the prime concern due to their contribution as a valuable precursors in the synthesis of medicinal and pharmaceutical agents. Herein, we wish to report a FeCl ₃ ‐promoted efficient synthesis of 2‐Aryl‐2,3‐dihydroquinazolin‐4(1 H )‐ones scaffold in water containing ammonium thiocyanate. During this study, we have demonstrated that presence of ammonium thiocyanate in aqueous media greatly influence the formation of products possibly due to in situ generation of Fe(SCN) ₃ . With operationally simple procedures and broader substrate scope, the developed protocol provides very good to excellent yield of medicinally‐relevant compounds.

The effective C-C bond-forming reactions by deaminative alkylation with N-alkylpyridinium salts are frequently accomplished by nickel-based or photoredox catalysis. Herein, we report an alkylative dearomatization of Katritzky salts employing N-hydroxyphthalimide (NHPI) and Zn metal for the efficient synthesis of 4-alkyl-1,4-dihydropyridine derivatives. This process harnesses N-alkylpyridinium salts as a source of both an alkyl radical donor and a radical acceptor, with selective addition at the 4-position. While reaction with only Zn metal as a reductant furnishes triphenylpyridine, the NHPI in combination with Zn delivers 4-alkyl-1,4-dihydropyridine derivatives with good-to-excellent yields, shorter reaction time, and broader substrate scope. The mechanistic studies reveal that the reaction proceeds via a radical intermediate through single-electron transfer (SET).

Herein, we disclose an efficient synthesis of α-iminonitriles facilitated by elemental sulfur through the dehydrogenative transformation of phenylacetonitriles with aliphatic amines. This useful strategy for α-iminonitriles operates at low temperature with a broader substrate scope, furnishing synthetically useful compounds in very good to excellent yields. Mechanistic investigations and observations from the literature suggest that the reaction proceeds via a dehydrogenative dithiolation sequence. Gram-scale synthesis and further synthetic transformation demonstrate the synthetic efficacy and utility of the developed protocol.