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Efficient Synthesis of ESI-09, A Novel Non-cyclic Nucleotide EPAC Antagonist
Haijun Chen1, Chunyong Ding, Christopher Wild
1Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas 77555, United States.
Abstract:
A concise and efficient synthetic approach to producing a novel non-cyclic nucleotide EPAC antagonist ESI-09 and its new analogs is reported. Key features of the synthesis include a mild and reliable one-pot procedure for an isoxazole synthon, as well as a modified one-pot protocol for the cyanomethyl ketone key intermediate. The synthesis requires inexpensive starting materials and only three linear steps for the completion in a total yield of 53%.
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