期刊
ORGANIC LETTERS
卷 18, 期 13, 页码 3282-3285出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b01552
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资金
- MESR (Ministere de l'Enseignement Superieur et de la Recherche)
- LABEX SynOrg [ANR-11-LABX-0029]
A selective functionalization of thiazolo[5,4-f]quinazolin-9(8H)-one has been developed through sequential activation of C-H bonds to furnish diarylated compounds. This strategy allows the regioselective C2 and C7 arylation by a judicious choice of coupling partners and bases, requiring no additional ligands or directing groups. Differently substituted N-8-benzylated-2,7-diaryl-thiazoloquinazolin-9(8H),ones were thereby obtained in a facile manner. A one-pot procedure was also performed. These protocols provide a synthetically useful route for late-stage functionalization of this highly valuable scaffold, required in drug discovery.
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