title: Direct amidation of unprotected amino acids using B(OCH2CF3)3.
abstract: A commercially available borate ester, B(OCH2CF3)3, can be used to achieve protecting-group free direct amidation of α-amino acids with a range of amines in cyclopentyl methyl ether. The method can be applied to the synthesis of medicinally relevant compounds, and can be scaled up to obtain gram quantities of products.
authors.affiliation: Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk.
authors.forename: Rachel M
authors.initials: RM
authors.lastname: Lanigan
authors.affiliation: Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk.
authors.forename: Valerija
authors.initials: V
authors.lastname: Karaluka
authors.affiliation: Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk.
authors.forename: Marco T
authors.initials: MT
authors.lastname: Sabatini
authors.affiliation: Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk.
authors.forename: Pavel
authors.initials: P
authors.lastname: Starkov
authors.affiliation: Pfizer Global Pharmaceutical Sciences, Discovery Park, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
authors.forename: Matthew
authors.initials: M
authors.lastname: Badland
authors.affiliation: GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK.
authors.forename: Lee
authors.initials: L
authors.lastname: Boulton
authors.affiliation: Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk.
authors.forename: Tom D
authors.initials: TD
authors.lastname: Sheppard