25 with the reagent derived from 1,1-diiodoethane and diethylzinc (eq 12). 43,44 The level of induction was highly dependent on the nature of the nitrogen protecting group.An interesting cyclopropanation of an exocyclic olefin was reported by Ronald (eq 13). 45 The cyclopropanation of 2-methylenecyclohexanol using 13 Table 4. Cyclopropanation of (E)-3-Penten-2-ol 47 conditions ratio 31:32

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In this report, we disclose our findings regarding the remarkable effect of a low-level impurity found in the solvent used for a ruthenium-catalyzed direct arylation reaction. This discovery allowed for the development of a robust and high-yield arylation protocol that was demonstrated on a multikilogram scale using carboxylate as the cocatalyst. Finally, a practical, scalable, and chromatography-free synthesis of the biaryl core of Anacetrapib is described.