A One-Pot, 3 Component, Domino Heck-aza-Michael Approach to Libraries of Functionalized 1, 1-Dioxido-1, 2-benzisothiazoline-2-acetic acids
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2009Article Version
Scholarly/refereed, author accepted manuscript
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A sequential three-component synthesis of functionalized benzisothiazoline-3-acetic acid 1,1- dioxides utilizing a domino Heck-aza-Michael pathway is reported. This one-pot procedure rapidly assembles functionalized benzylsulfonamides, which undergo a palladium-catalyzed, domino, Heckaza- Michael transformation in an experimentally straightforward manner. This attractive protocol has been utilized to synthesize three combinatorial sub-libraries (I-III) comprising a total of 95 compounds in high purities (≥95% for 75 compounds), yield and quantities.
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This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Combinatorial Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://doi.org/10.1021/cc900025e.
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Rolfe, A., Young, K., Volp, K., Schoenen, F., Neuenswander, B., Lushington, G. H., & Hanson, P. R. (2009). A One-Pot, 3-Component, Domino Heck-aza-Michael Approach to Libraries of Functionalized 1,1-Dioxido-1,2-benzisothiazoline-3-acetic acids. Journal of Combinatorial Chemistry, 11(4), 732–738. http://doi.org/10.1021/cc900025e
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