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Note | Special issue | Vol 70, No. 1, 2006, pp.587-598
Published online, 17th November, 2006
DOI: 10.3987/COM-06-S(W)31
A Novel One-Pot Synthesis of N-Substituted Thieno[3,2-d]pyrimidin-4(3H)-ones

Andrew J. Peat,* Paul L. Feldman, Dulce Garrido, Yu C. Guo, and Donald L. Hertzog

*Room 3.4244, Medicinal Chemistry Department, 5 Moore Drive, Research Triangle Park, NC 27709, U.S.A.


A novel synthetic route for the construction of thieno[3,2-d]pyrimidin-4(3H)-ones has been developed with the key step involving an AlMe3-promoted ester-to-amide conversion. The yields within this initial set of analogs are comparable to those obtained via our previously reported routes and in at least one case far superior, thus serving to compliment other approaches to this useful chemical scaffold.