title: Liquid-phase parallel synthesis of combinatorial libraries of substituted 6-carbamoyl-3,4-dihydro-2H-benzo[1,4]thiazines.
abstract: In this work, we explored several original combinatorial derivatization patterns for the 3,4-dihydro-2H-1,4-benzothiazine scaffold. The synthesis begins with commercially available 4-chloro- and 4-fluoro-3-nitrobenzoates and employs a sequence of moderate and high-yielding reactions that display a relatively high substituent tolerance. Simple manual techniques for parallel reactions were coupled with easy workup and purification procedures to give high-purity final products. The developed approach was easily adaptable for parallel synthesis of more than 2600 novel 2H-benzo[1,4]thiazine-6-carboxylic acid amides, which were efficiently prepared in a semiautomatic fashion using special CombiSyn synthesizers.
authors.affiliation: Chemical Diversity Research Institute, Khimki, Moscow reg. 114401, Russia.
authors.forename: Andrey S
authors.initials: AS
authors.lastname: Trifilenkov
authors.forename: Vladimir V
authors.initials: VV
authors.lastname: Kobak
authors.forename: Marina A
authors.initials: MA
authors.lastname: Salina
authors.forename: Julya A
authors.initials: JA
authors.lastname: Kusovkova
authors.forename: Alexey P
authors.initials: AP
authors.lastname: Ilyin
authors.forename: Alexander V
authors.initials: AV
authors.lastname: Khvat
authors.forename: Sergey E
authors.initials: SE
authors.lastname: Tkachenko
authors.forename: Alexandre V
authors.initials: AV
authors.lastname: Ivachtchenko
mesh_terms: D002853:Chromatography, Liquid / Q000379:methods*; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D015394:Molecular Structure; D013843:Thiazines / Q000138:chemical synthesis*
chemical_list: D013843:Thiazines