Synfacts 2014; 10(5): 0515
DOI: 10.1055/s-0033-1341218
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart · New York

Stereospecific Kumada Cross-Coupling of Alkyl and Aryl Grignards

Contributor(s):
Paul Knochel
,
Diana Haas
Yonova IM, Johnson AG, Osborne CA, Moore CE, Morrissette NS, Jarvo ER * University of California, Irvine and University of California, San Diego, USA
Stereospecific Nickel-Catalyzed Cross-Coupling Reactions of Alkyl Grignard Reagents and Identification of Selective Anti-Breast-Cancer Agents.

Angew. Chem. Int. Ed. 2014;
53: 2422-2427
Further Information

Publication History

Publication Date:
17 April 2014 (online)

 

Significance

Herein, the authors report an efficient nickel-catalyzed cross-coupling reaction of long-chain alkyl and various aryl Grignards with benzylic ethers providing the corresponding products with high enantiospecificity. Furthermore, applying this reaction protocol, compounds that show promising inhibition of breast cancer cell proliferation could be prepared.


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Comment

Decreasing the reaction concentration raised the efficiency of the transformation and less elimination byproduct was generated. Also, the use of more than two equivalents of Grignard reagent was disadvantageous for the reaction.


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