title: One-Pot Synthesis of α-Branched N-Acylamines via Titanium-Mediated Condensation of Amides, Aldehydes, and Organometallics.
abstract: A three-component, titanium-mediated synthesis of α-branched N-acylamines from commercial or readily accessible amides, aldehydes, and organometallic reagents is reported. The transformation proceeds under mild reaction conditions and tolerates a variety of functional groups (including nitrile, carbamate, olefin, basic amine, furan, and other sensitive heteroaromatics) to generate a large umbrella of α-branched N-acylamine products in high yields. The operationally practical procedure enables the use of this method in parallel chemical synthesis, a valuable feature that can facilitate the screening of bioactive molecules by medicinal chemists.
authors.affiliation: Neuroscience and Pain and ‡Cardiovascular, Endocrine, and Metabolic Diseases, Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Chunhui
authors.initials: C
authors.lastname: Dai
authors.affiliation: Neuroscience and Pain and ‡Cardiovascular, Endocrine, and Metabolic Diseases, Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Julien
authors.identifier: 0000-0001-5879-2491
authors.initials: J
authors.lastname: Genovino
authors.affiliation: Neuroscience and Pain and ‡Cardiovascular, Endocrine, and Metabolic Diseases, Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Bruce M
authors.initials: BM
authors.lastname: Bechle
authors.affiliation: Neuroscience and Pain and ‡Cardiovascular, Endocrine, and Metabolic Diseases, Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Matthew S
authors.initials: MS
authors.lastname: Corbett
authors.affiliation: Neuroscience and Pain and ‡Cardiovascular, Endocrine, and Metabolic Diseases, Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Chan Woo
authors.initials: CW
authors.lastname: Huh
authors.affiliation: Neuroscience and Pain and ‡Cardiovascular, Endocrine, and Metabolic Diseases, Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Colin R
authors.initials: CR
authors.lastname: Rose
authors.affiliation: Neuroscience and Pain and ‡Cardiovascular, Endocrine, and Metabolic Diseases, Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Jianmin
authors.initials: J
authors.lastname: Sun
authors.affiliation: Neuroscience and Pain and ‡Cardiovascular, Endocrine, and Metabolic Diseases, Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Joseph S
authors.initials: JS
authors.lastname: Warmus
authors.affiliation: Neuroscience and Pain and ‡Cardiovascular, Endocrine, and Metabolic Diseases, Pfizer Worldwide Medicinal Chemistry , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: David C
authors.initials: DC
authors.lastname: Blakemore