Copper-mediated N-arylation of methyl 2-aminothiophene-3-carboxylate with organoboron reagents

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• 作者：Komal Rizwan^a ; ^b ; Idris Karakaya^a ; ^c ; Drew Heitz^a ; Muhammad Zubair^b ; Nasir Rasool^b ; Gary A. Molander^a ; ^{gmolandr@sas.upenn.edu" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Thiophene ; Cross-coupling ; Copper ; Amine ; Carboxylate ; Aryltrifluoroborate
• 刊名：Tetrahedron Letters
• 出版年：2015
• 出版时间：9 December 2015
• 年：2015
• 卷：56
• 期：49
• 页码：6839-6842
• 全文大小：380 K

文摘

A practical protocol for the synthesis of N-arylated methyl 2-aminothiophene-3-carboxylate has been developed via Chan–Lam cross-coupling. The desired products were synthesized by cross-coupling of methyl 2-aminothiophene-3-carboxylate with both arylboronic acids and potassium aryltrifluoroborate salts in moderate to good yields. A broad range of functional groups was well tolerated.