The development of a 'click, click, cy-click' process utilizing a double aza-Michael reaction to generate functionalized 1,2,5-thiadiazepane 1,1-dioxides is reported. Optimization in flow, followed by scale out of the inter-/intramolecular double aza-Michael addition has also been realized using a microwave-assisted, continuous flow organic synthesis platform (MACOS). In addition, a facile one-pot, sequential strategy employing in situ Huisgen cycloaddition post-double aza-Michael has been accomplished, and is applicable to library synthesis.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3171749 | PMC |
| http://dx.doi.org/10.1055/s-0030-1260112 | DOI Listing |
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