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Efficient Synthesis of ESI-09, A Novel Non-cyclic Nucleotide EPAC Antagonist.

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%.

SUBMITTER: Chen H

PROVIDER: S-EPMC3580859 | biostudies-literature | 2013 Mar

REPOSITORIES: biostudies-literature

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Efficient Synthesis of ESI-09, A Novel Non-cyclic Nucleotide EPAC Antagonist.

Chen Haijun H Ding Chunyong C Wild Christopher C Liu Huiling H Wang Tianzhi T White Mark A MA Cheng Xiaodong X Zhou Jia J

Tetrahedron letters 20130301 12

A concise and efficient synthetic approach to producing a novel non-cyclic nucleotide EPAC antagonist <b>ESI-09</b> 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%. ...[more]

PMID: 23459418

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