title: Rapid, Microwave-Assisted Organic Synthesis of Selective (V600E)BRAF Inhibitors for Preclinical Cancer Research.
abstract: We report a dramatically improved total synthesis of two highly selective (V600E)BRAF inhibitors, PLX4720 and PLX4032, that leverages microwave-assisted organic synthesis (MAOS). Compared with previously reported approaches, our novel MAOS method significantly reduces overall reaction time without compromising yield. In addition to providing a gram-scale route to these compounds for preclinical oncology research, we anticipate this approach could accelerate the synthesis of azaindoles in high-throughput, library-based formats.
authors.affiliation: Vanderbilt University Institute of Imaging Science (VUIIS), Nashville, TN 37232, USA ; Department of Radiology & Radiological Sciences, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
authors.forename: Jason R
authors.initials: JR
authors.lastname: Buck
authors.forename: Sam
authors.initials: S
authors.lastname: Saleh
authors.forename: Md Imam
authors.initials: MI
authors.lastname: Uddin
authors.forename: H Charles
authors.initials: HC
authors.lastname: Manning