De Novo Synthesis of a Potent LIMK1 Inhibitor
20 January 2010 (eFirst)
A potent LIMK1 inhibitor, BMS4, was synthesised in six steps starting from pyrazine-2-carboximidamide, offering a significant improvement over current methods available in the literature.
kinase inhibitor - nitrogen heterocycles - pyrimidine - Suzuki coupling - cyclization
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Bristol-Myers Squibb did not assign compound 1 a BMS compound number. However in the Bristol-Myers Squibb publication,³ compound 1 was referred to as ‘compound 4’. Hence, for identification purposes, we named compound 1 ‘BMS4’.5
Communication with SYNthesis Med Chem.6
The authors noted that the quality of Pd(PPh3)4 dramatically influences the reaction outcome.8
Experimental details and conditions for the LIMK1 Transcreener Fluorescence Polarisation assay are available from the authors on request.