title: Straightforward protocol for the efficient synthesis of varied N(1)-acylated (aza)indole 2-/3-alkanoic acids and esters: optimization and scale-up.
abstract: A library of approximately 40 N(1)-acylated (aza)indole alkanoic esters and acids was prepared employing a microwave-assisted approach. The optimized synthetic route allows for parallel synthesis, variation of the indole substitution pattern and high overall yield. Additionally, the procedure has been scaled up to yield multi-gram amounts of preferred indole compounds, e.g.: 2'-des-methyl indomethacin 2. The reported compounds were designed as biomedical tools for primary and secondary in vitro and in vivo studies at relevant molecular targets.
authors.affiliation: A.B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology and Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
authors.forename: Andy J
authors.initials: AJ
authors.lastname: Liedtke
authors.forename: Kwangho
authors.initials: K
authors.lastname: Kim
authors.forename: Donald F
authors.initials: DF
authors.lastname: Stec
authors.forename: Gary A
authors.initials: GA
authors.lastname: Sulikowski
authors.forename: Lawrence J
authors.initials: LJ
authors.lastname: Marnett