Abstract
An improved procedure for the synthesis an analog of the p38 inhibitor compound VX- 745 is reported.
Highlights
Mitogen-activated protein (MAP) kinases are key enzymes involved in signal transduction and the amplification of cellular responses to stumuli
Vertex discovered the 3D structure of p38MAP kinase in 1996 and computer modeling and testing suggested the design of VX475 [1]
When pure 4 was reacted with dimethylformamide dimethyl acetal the VX-745 analog 5 was formed as a yellow precipitate, which crystallized from AcOH/water with a yield of 41%
Summary
Mitogen-activated protein (MAP) kinases are key enzymes involved in signal transduction and the amplification of cellular responses to stumuli. Abstract: An improved procedure for the synthesis an analog of the p38 inhibitor compound VX745 is reported. For comparison purposes we needed a sample of a VX-745 analog and followed the synthesis as described in a general procedure for the preparation of p38 inhibitor compounds by Bemis and coworkers [2,3].
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