Coumarin derivatives are widespread in nature and are considered as one of the most important pharmacophores in medicinal chemistry. Dicoumarols are a subcategory of coumarin derivatives. On the other hand, protection of nature is one of the major criteria in modern science and technology and the concept of ‘Green Chemistry’ has been globally adopted to protect human health and environment. Since the last decade of twentieth century, environmental safety has been considering as one of the major issues, both from academia and industry. ‘On water’ systematic green synthetic procedure for the synthesis of diversely substituted dicoumarols is described using 4-hydroxy coumarin and diversely substituted aldehydes under controlled microwave exposure (green technique). Notably, no catalyst/support is required to achieve high yield of the dicoumarols. The newly developed method is very simple, extremely rapid and produces product with almost quantitative yields irrespective of the nature/substituent of the aldehyde. The present synthetic protocol satisfies a number of green chemistry principles by its atom economy, avoiding the use of hazardous solvents, supports or toxic catalysts, rapid reaction period, and simple work-up procedure. The newly synthesized products have been screened against drug-resistant <i>Mycobacterium tuberculosis</i> strains (H37Rv) and some of these derivatives have demonstrated promising antitubercular activity. The present method may find application in the synthesis of potent antitubercular drugs.

Water green synthesis of antitubercular dicoumarols

254th National Meeting (2017)

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