title: Synthesis of Tetrazolo-Fused Benzodiazepines and Benzodiazepinones by a Two-Step Protocol Using an Ugi-Azide Reaction for Initial Diversity Generation.
abstract: A two-step strategy for the synthesis of arrays of tricyclic tetrazolo-fused benzodiazepines and benzodiazepinones has been investigated. The protocol uses ortho-N-Boc phenylisocyanides and phenylglyoxaldehydes or ethyl glyoxylate in the 4-component Ugi-Azide reaction to afford MCR (Multi Component Reactions) derived adducts equipped with the desired diversity inputs. A subsequent acidic treatment (TFA/DCE) allows a simultaneous deprotection-cyclization leading to the final products.
authors.affiliation: Department of Pharmacology and Toxicology, College of Pharmacy, BIO5 Oro Valley, The University of Arizona, 1580 E. Hanley Blvd., Oro Valley, AZ 85737 USA.
authors.forename: Steven
authors.initials: S
authors.lastname: Gunawan
authors.forename: Muhammad
authors.initials: M
authors.lastname: Ayaz
authors.forename: Fabio
authors.initials: F
authors.lastname: De Moliner
authors.forename: Brendan
authors.initials: B
authors.lastname: Frett
authors.forename: Christine
authors.initials: C
authors.lastname: Kaiser
authors.forename: Nina
authors.initials: N
authors.lastname: Patrick
authors.forename: Zhigang
authors.initials: Z
authors.lastname: Xu
authors.forename: Christopher
authors.initials: C
authors.lastname: Hulme