title: Transition-Metal-Free Synthesis of Tertiary Aminocyclopropanes.
abstract: A transition-metal-free methodology for the construction of pharmaceutically relevant tertiary aminocyclopropanes is reported. Hydrazonamides, safe and stable carbene precursors, undergo smooth cyclopropanation with vinyl arenes in the presence of a base. The reaction proceeds with stereoselectivity to favor the Z isomer and provides facile access to a variety of substitution patterns through variation of the coupling partners.
authors.affiliation: Discovery Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
authors.forename: Patrick
authors.identifier: 0000-0001-5320-3483
authors.initials: P
authors.lastname: Cyr
authors.affiliation: Discovery Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
authors.forename: Alexandre
authors.initials: A
authors.lastname: Côté-Raiche
authors.affiliation: Discovery Chemistry, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
authors.forename: Sarah M
authors.initials: SM
authors.lastname: Bronner