Electrophilic Zinc Homoenolates: Synthesis of Cyclopropylamines from Cyclopropanols and Amines L. Reginald Mills Luis Miguel Barrera Arbelaez Sophie A. L. Rousseaux 10.1021/jacs.7b07104.s001 https://acs.figshare.com/articles/journal_contribution/Electrophilic_Zinc_Homoenolates_Synthesis_of_Cyclopropylamines_from_Cyclopropanols_and_Amines/5311381 Metal homoenolates, produced via C–C bond cleavage of cyclopropanols, have been extensively investigated as nucleophiles for the synthesis of β-substituted carbonyl derivatives. Herein, we demonstrate that zinc homoenolates can react as carbonyl-electrophiles in the presence of nucleophilic amines to yield highly valuable <i>trans-</i>cyclopropylamines in good yields and high diastereoselectivities. GSK2879552, a lysine demethylase 1 inhibitor currently in clinical trials for the treatment of small cell lung carcinoma, was synthesized using this strategy. 2017-08-15 13:18:12 cyclopropylamine presence lysine demethylase 1 inhibitor GSK strategy carbonyl-electrophile diastereoselectivitie nucleophilic amines carbonyl derivatives Cyclopropanol synthesis Electrophilic Zinc Homoenolates β- nucleophile cyclopropanol zinc homoenolates Cyclopropylamine tran cell lung carcinoma Herein yield cleavage Synthesi Amines Metal homoenolates bond