No abstract

Thiazole frame work represents a vital pharmacophore in several areas of chemistry. Consequently, several synthetic protocols to construct and functionalize this core, in an attempt to generate diverse thiazole containing architectures have been developed by various researchers across the globe. These wide range of methodologies developed will allow the access to fully decorated thiazole containing new chemical entities that can find various application in the field of medicinal chemistry, agrochemicals and material science. This review will provide an insight in to the various synthons used in construction and diversification of this core. Diversely functionalized thiazole analogs are considered as a vital azole framework present in many natural products. This prominent heterocycle also constitutes an important pharmacophore in medicinal chemistry, in agrochemicals and in molecules for material science applications. All these above‐mentioned features of thiazole necessitates the continuous development of efficient methods to access this heterocycle. Accordingly, various researchers across the globe have come up with efficient synthetic protocols in an attempt functionalize different positions of this important scaffold. This review aims at highlighting some of the latest synthetic approaches to di/tri‐substituted thiazole analogs which are known to possess a wide spectrum of biological activities.

No abstract

We present an approach to utilize water as the hydride source via Pd(II)/Pd(0) catalysis. As a case study, we have achieved a diboron mediated Pd(II)-catalyzed hydroarylation of alkynes using arylboronic acids. This approach not only complements conventional reactivity of Pd via Pd(0)/Pd(II) cycle for the hydroarylation but also utilizes water as the hydride source. We believe this would particularly be beneficial in utilizing water as a reagent.

No abstract

A novel series of analogues based on 5-(1-(4-chloro-3-methoxyphenyl)piperidin-4-yl)-4-phenyl-2H-1,2,4-triazole-3(4H)-thione core have been synthesized and their potential as antibacterial, antifungal and antitubercular agents was examined. The structure-activity relationship (SAR) studies of these derivatives 5 (a-k) clearly indicate the vital role of lipophilicity as a major factor in enhancing the biological activity of these compounds. Among the compounds screened, 5a, 5c, 5d, 5j and 5k displayed significant activity against Mycobacterium tuberculosis H37Rv strain.

A phenyliodine(III) diacetate mediated umpolung reactivity of the tertiary amines with suitably substituted o-hydroxybenzyl and phenyl groups is exploited to facilitate o-C(sp)-H functionalization to afford diaryl ethers. The presence of an o-CHO and secondary amine functionalities in the resulting diaryl ether, generated in situ, were utilized for synthesis of dibenzoxazepines and dibenzoxazepinones. Mild conditions and relative broad substrate scope, and potential for further diversification of the diaryl ethers are highlights of this methodology.

No abstract