Synthesis 2010(7): 1091-1096  
DOI: 10.1055/s-0029-1219230
PAPER
© Georg Thieme Verlag Stuttgart ˙ New York

De Novo Synthesis of a Potent LIMK1 Inhibitor

Brad E. Sleebs*a,b, Ian P. Streeta,b, Xian Buc, Jonathan B. Baella,b
a The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, Victoria 3052, Australia
b Cancer Therapeutics-CRC P/L, 4 Research Ave, La Trobe R&D Park, Bundoora, Victoria 3086, Australia
Fax: +61(3)93452129; e-Mail: sleebs@wehi.edu.au;
c SYNthesis Med Chem P/L, 528 Ruiqing Road, Heqing, Zhangjiang Modern Medical Device Park, Shanghai 201203, P. R. of China
Further Information

Publication History

Received 27 November 2009
Publication Date:
20 January 2010 (eFirst)

Abstract

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.

    References

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4

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.