title: Construction of a 2,6-difunctionalized 2-methyl-2H-1-benzopyran library by using a solid-phase synthesis protocol.
abstract: [reaction: see text] A library containing 1200 analogues of 2,6-difunctionalized 2-methyl-2H-1-benzopyran was constructed by using a solid-phase synthesis protocol. Polymer-bound 6-amido-, 6-sulfonamido-, and 6-uredo-functionalized 2-hydroxymethyl-2-methylbenzopyrans 10 were prepared as part of a first-generation diversification step by employing reactions of respective acid halides, sulfonyl chlorides, and isocyanates with the amine precursor 7. Transformations of the resin-bound intermediates 10 by reactions with alkyl and acid halides were then used to produce a diverse series of 2,6-difunctionalized 2-methyl-2H-1-benzopyran analogues 12 and 14.
authors.affiliation: Medicinal Science Division, Korea Research Institute of Chemical Technology, P.O. Box 107, Yusung-gu, Daejeon 305-600, Korea.
authors.forename: Jong Yeon
authors.initials: JY
authors.lastname: Hwang
authors.forename: Hyung-Sub
authors.initials: HS
authors.lastname: Choi
authors.forename: Jin-soo
authors.initials: JS
authors.lastname: Seo
authors.forename: Hyun Ju
authors.initials: HJ
authors.lastname: La
authors.forename: Dong-Soo
authors.initials: DS
authors.lastname: Kim
authors.forename: Hyun Suk
authors.initials: HS
authors.lastname: Jeon
authors.forename: Moon-Kook
authors.initials: MK
authors.lastname: Jeon
authors.forename: Duck-Hyung
authors.initials: DH
authors.lastname: Lee
authors.forename: Young-Dae
authors.initials: YD
authors.lastname: Gong
mesh_terms: D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure
chemical_list: C511507:2-methyl-2H-1-benzopyran; D001578:Benzopyrans