In the everlasting search for cheaper and more environmentally friendly synthetic methods, the use of organolithium reagents provides crucial advantages over traditional organometallics (B/Sn/Zn/Mg) frequently used in cross coupling reactions. Recent advances with electron rich palladium and nickel complexes have led to increased reactivity and functional group tolerance, and have paved the way for the application of the reactive organolithium reagents. Application is showcased in the diastereoselective synthesis of the neurotrophically active Mastigophorene A , induced by a point to axial chirality transfer, which was achieved by means of a bulky carbene (Pd-PEPPSI) complex. Further application was demonstrated in the fast (2 min) synthesis of radiolabeled COX-2 inhibitor <sup>11</sup>C-Celecoxib and an the high atom economy synthesis of the anti-breast cancer drug Tamoxifen.

Advances in organolithium cross-coupling reactions

253rd National Meeting (2017)

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