Microwave-based synthesis of novel thienopyrimidine bioisosteres of gefitinib

MS Phoujdar, MK Kathiravan, JB Bariwal, AK Shah…

Index: Phoujdar, Manisha S.; Kathiravan, Muthu K.; Bariwal, Jitender B.; Shah, Anamik K.; Jain, Kishor S. Tetrahedron Letters, 2008 , vol. 49, # 7 p. 1269 - 1273

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Citation Number: 35

Abstract

A series of novel 2-unsubstituted 4-(substituted) anilinothieno [2, 3-d] pyrimidines is synthesized through the chlorination of the corresponding 2-unsubstituted-thieno [2, 3-d]- pyrimidin-4-ones, followed by the nucleophilic displacement of the 4-Cl group of 9, with a variety of anilines. All four steps of this synthesis involve microwave irradiation (MWI) and the entire synthesis requires only 2h.