August 10, 2014 – All About Drugs

All About Drugs

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Catalyst-free sulfonylation of activated alkenes for highly efficient synthesis of mono-substituted ethyl sulfones in water

Green Chem., 2014, Advance Article
DOI: 10.1039/C4GC00932K, Communication

Yu Yang,^a Lin Tang,^a Sheng Zhang,^a Xuefeng Guo,^a Zhenggen Zha^a and Zhiyong Wang*^a

Corresponding authors

Hefei National Laboratory for Physical Sciences at Microscale, CAS Key Laboratory of Soft Matter Chemistry & Collaborative Innovation Center of Suzhou Nano Science and Technology, University of Science and Technology of China, Hefei, P. R. China
E-mail: zwang3@ustc.edu.cn;
Fax: (+86) 551-360-3185

Green Chem., 2014, Advance Article

DOI: 10.1039/C4GC00932K

A catalyst-free sulfonylation of activated alkenes developed under mild conditions in water.

http://pubs.rsc.org/en/Content/ArticleLanding/2014/GC/C4GC00932K?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

A catalyst-free sulfonylation reaction of activated alkenes with sulfonyl hydrazides was efficiently developed under mild and environmentally benign conditions, in water without any ligand or additive. The reaction gave a range of structurally diverse mono-substituted ethyl sulfones with excellent yields, in which the by-product was nitrogen.

Figure 2 :Reaction vessel for microsponge preparation by liquid- liquid suspension polymerization

Microsponges are polymeric delivery systems composed of porous microspheres. They are tiny sponge-like spherical particles with a large porous surface. Moreover, they may enhance stability, reduce side effects and modify drug release favorably. Microsponge technology has many favorable characteristics, which make it a versatile drug delivery vehicle. Microsponge Systems are based on microscopic, polymer-based microspheres that can suspend or entrap a wide variety of substances, and can then be incorporated into a formulated product such as a gel, cream, liquid or powder. The outer surface is typically porous, allowing a sustained flow of substances out of the sphere. Microsponges are porous, polymeric microspheres that are used mostly for topical use and have recently been used for oral administration. Microsponges are designed to deliver a pharmaceutical active ingredient efficiently at the minimum dose and also to enhance stability, reduce side effects, and modify drug release.

http://www.japtr.org/article.asp?issn=2231-4040;year=2010;volume=1;issue=3;spage=283;epage=290;aulast=Kaity

Kaity S, Maiti S, Ghosh AK, Pal D, Ghosh A, Banerjee S. Microsponges: A novel strategy for drug delivery system. J Adv Pharm Technol Res 2010;1:283-90

Kaity S, Maiti S, Ghosh AK, Pal D, Ghosh A, Banerjee S. Microsponges: A novel strategy for drug delivery system. J Adv Pharm Technol Res [serial online] 2010 [cited 2014 Aug 10];1:283-90. Available from: http://www.japtr.org/text.asp?2010/1/3/283/72416

Figure 3 :Preparation of microsponges by the quasi-emulsion solvent diffusion method