title: 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 antagonistESI-09and 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%.
authors: Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas 77555, United States.
authors: Haijun
authors: H
authors: Chen
authors: Chunyong
authors: C
authors: Ding
authors: Christopher
authors: C
authors: Wild
authors: Huiling
authors: H
authors: Liu
authors: Tianzhi
authors: T
authors: Wang
authors: Mark A
authors: MA
authors: White
authors: Xiaodong
authors: X
authors: Cheng
authors: Jia
authors: J
authors: Zhou
keywords: EPAC antagonist; ESI-09; cyanomethyl ketone; isoxazole; modified Kowalski's protocol