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Literature DB >> 23459418

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

Haijun Chen¹, Chunyong Ding, Christopher Wild, Huiling Liu, Tianzhi Wang, Mark A White, Xiaodong Cheng, Jia Zhou.

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%.

Entities: Chemical Disease Gene Species

Keywords: EPAC antagonist; ESI-09; cyanomethyl ketone; isoxazole; modified Kowalski's protocol

Year: 2013 PMID： 23459418 PMCID： PMC3580859 DOI： 10.1016/j.tetlet.2013.01.024

Source DB: PubMed Journal: Tetrahedron Lett ISSN： 0040-4039 Impact factor: 2.415

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