Synthesis of 2, 3-substituted thienylboronic acids and esters

C Christophersen, M Begtrup, S Ebdrup…

Index: Christophersen, Claus; Begtrup, Mikael; Ebdrup, Soren; Petersen, Henning; Vedso, Per Journal of Organic Chemistry, 2003 , vol. 68, # 24 p. 9513 - 9516

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Citation Number: 47

Abstract

A noncryogenic protocol for the synthesis of 2-substituted 3-thienylboronic acids and esters as well as 3-substituted 2-thienylboronic acids and esters has been developed. Electrophiles were introduced regiospecifically in the 2-position of 2, 3-dibromothiophene and in the 3-position of 2-bromo-3-iodothiophene by halogen-magnesium exchange followed by quenching with electrophiles. Palladium-catalyzed borylation of the 2, 3- ...