Automated Synthesis of a Library of Triazolated 1,2,5-Thiadiazepane 1,1-Dioxides via a Double Aza-Michael Strategy

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• 作者：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
• 刊名：ACS Combinatorial Science
• 出版年：2012
• 出版时间：August 13, 2012
• 年：2012
• 卷：14
• 期：8
• 页码：456-459
• 全文大小：353K
• 年卷期：v.14,no.8(August 13, 2012)
• ISSN：2156-8944

文摘

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.

Keywords:

aza-Michael; triazolated 1,2,5-thiadiazepane 1,1-dioxides; parallel synthesis