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      Ultrasound-promoted Brønsted acid ionic liquid-catalyzed hydrothiocyanation of activated alkynes under minimal solvent conditions

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          Abstract

          A facile, practical and eco-friendly protocol for the synthesis of various Z-vinyl thiocyanates under minimal solvent conditions was developed.

          Abstract

          By using water as the hydrogen source, an eco-friendly and practical protocol for the synthesis of Z-vinyl thiocyanates through ultrasound-promoted Brønsted acid ionic liquid-catalyzed hydrothiocyanation of activated alkynes under minimal solvent conditions has been developed. This process effectively avoids the use of organic solvents, metal catalysts and harsh reaction conditions. This reaction shows attractive characteristics such as operational simplicity, broad substrate scope with good to excellent yields, ease of scale-up and high energy efficiency and recyclable and reusable catalysts.

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          Sulfur Containing Scaffolds in Drugs: Synthesis and Application in Medicinal Chemistry.

          The impact of the development of sulfur therapeutics is instrumental to the evolution of the pharmaceutical industry. Sulfur-derived functional groups can be found in a broad range of pharmaceuticals and natural products. For centuries, sulfur continues to maintain its status as the dominating heteroatom integrated into a set of 362 sulfur-containing FDA approved drugs (besides oxygen or nitrogen) through the present. Sulfonamides, thioethers, sulfones and Penicillin are the most common scaffolds in sulfur containing drugs, which are well studied both on synthesis and application during the past decades. In this review, these four moieties in pharmaceuticals and recent advances in the synthesis of the corresponding core scaffolds are presented.
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            Green chemistry oriented organic synthesis in water.

            The use of water as solvent features many benefits such as improving reactivities and selectivities, simplifying the workup procedures, enabling the recycling of the catalyst and allowing mild reaction conditions and protecting-group free synthesis in addition to being benign itself. In addition, exploring organic chemistry in water can lead to uncommon reactivities and selectivities complementing the organic chemists' synthetic toolbox in organic solvents. Studying chemistry in water also allows insight to be gained into Nature's way of chemical synthesis. However, using water as solvent is not always green. This tutorial review briefly discusses organic synthesis in water with a Green Chemistry perspective.
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              Data-mining for sulfur and fluorine: an evaluation of pharmaceuticals to reveal opportunities for drug design and discovery.

              Among carbon, hydrogen, oxygen, and nitrogen, sulfur and fluorine are both leading constituents of the pharmaceuticals that comprise our medicinal history. In efforts to stimulate the minds of both the general public and expert scientist, statistics were collected from the trends associated with therapeutics spanning 12 disease categories (a total of 1969 drugs) from our new graphical montage compilation: disease focused pharmaceuticals posters. Each poster is a vibrant display of a collection of pharmaceuticals (including structural image, Food and Drug Administration (FDA) approval date, international nonproprietary name (INN), initial market name, and a color-coded subclass of function) organized chronologically and classified according to an association with a particular clinical indication. Specifically, the evolution and structural diversity of sulfur and the popular integration of fluorine into drugs introduced over the past 50 years are evaluated. The presented qualitative conclusions in this article aim to promote innovative insights into drug development.
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                Author and article information

                Contributors
                Journal
                GRCHFJ
                Green Chemistry
                Green Chem.
                Royal Society of Chemistry (RSC)
                1463-9262
                1463-9270
                2018
                2018
                : 20
                : 16
                : 3683-3688
                Affiliations
                [1 ]Hunan Provincial Engineering Research Center for Ginkgo biloba
                [2 ]Hunan University of Science and Engineering
                [3 ]Yongzhou 425100
                [4 ]China
                [5 ]Hunan Provincial Key Laboratory of Materials Protection for Electric Power and Transportation
                [6 ]State Key Laboratory of Chemo/Biosensing and Chemometrics
                [7 ]Hunan University
                [8 ]Changsha
                [9 ]Changsha University of Science and Technology
                [10 ]Key Laboratory of Theoretical Organic Chemistry and Functional Molecule of Ministry of Education
                [11 ]Hunan University of Science and Technology
                [12 ]Xiangtan 411201
                Article
                10.1039/C8GC00491A
                72b288da-d02a-4708-ac8b-1088e189d916
                © 2018

                http://rsc.li/journals-terms-of-use

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