Facile Synthesis of Substituted 5-Amino- and 3-Amino-1,2,4-Thiadiazoles from a Common Precursor

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• 作者：Paul M. Wehn ; Paul E. Harrington ; John E. Eksterowicz
• 刊名：Organic Letters
• 出版年：2009
• 出版时间：December 17, 2009
• 年：2009
• 卷：11
• 期：24
• 页码：5666-5669
• 全文大小：257K
• 年卷期：v.11,no.24(December 17, 2009)
• ISSN：1523-7052

文摘

A novel approach to the synthesis of substituted 5-amino- and 3-amino-1,2,4-thiadiazoles beginning from a common precursor has been achieved. Derivatization by palladium-catalyzed Suzuki−Miyaura coupling enables the rapid preparation of analogs around this pharmaceutically relevant core. FMO calculations rationalize the observed chemoselectivity for coupling at chlorine.