Literature DB >> 22853708

Automated synthesis of a library of triazolated 1,2,5-thiadiazepane 1,1-dioxides via a double aza-Michael strategy.

Qin Zang, Salim Javed, David Hill, Farman Ullah, Danse Bi, Patrick Porubsky, Benjamin Neuenswander, Gerald H Lushington, Conrad Santini, Michael G Organ, Paul R Hanson.   

Abstract

The construction of a 96-member library of triazolated 1,2,5-thiadiazepane 1,1-dioxides was performed on a Chemspeed Accelerator (SLT-100) automated parallel synthesis platform, culminating in the successful preparation of 94 out of 96 possible products. The key step, a one-pot, sequential elimination, double-aza-Michael reaction, and [3 + 2] Huisgen cycloaddition pathway has been automated and utilized in the production of two sets of triazolated sultam products.

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Year:  2012        PMID: 22853708      PMCID: PMC3656823          DOI: 10.1021/co300049u

Source DB:  PubMed          Journal:  ACS Comb Sci        ISSN: 2156-8944            Impact factor:   3.784


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2.  Synthesis of a Library of 1,5,2-Dithiazepine 1,1-Dioxides. Part 1: A One-Pot Sulfonylation/Thia-Michael Protocol.

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