Palladium-catalyzed highly meta-selective C—H iodination of phenylacetic acid,benzylphosphonate and benzylsulfonate scaffolds with molecular I2 is developed using a pyridine-type template.The practical ester linkages...Palladium-catalyzed highly meta-selective C—H iodination of phenylacetic acid,benzylphosphonate and benzylsulfonate scaffolds with molecular I2 is developed using a pyridine-type template.The practical ester linkages enable the directing template easily installed and readily removed.The substrate scope is broad,and alkyl,methoxyl,trifluomethyl,and halo substituents are compatible with this reaction.Further transformations of ibuprofen iodide intermediates by Pd-catalyzed C—C and C-heteroatom bond formation illustrate the broad utility of this method.展开更多
基金Shanghai Institute of Materia Medica,Chinese Academy of Sciences,National Natural Science Foundation of China(No.21772211)Youth Innovation Promotion Association CAS(Nos.2014229 and 2018293)+4 种基金Institutes for Drug Discovery and Development,Chinese Academy of Sciences(No.CASIMM0120163006)Science and Technology Commission of Shanghai Municipality(No.17JC1405000)Program of Shanghai Academic Research Leader(No.19XD1424600)National Science&Technology Major Project“Key New Drug Creation and Manufacturing Program”,China(No.2018ZX09711002-006)the State Key Laboratory of Natural and Biomimetic Drugs for financial support。
文摘Palladium-catalyzed highly meta-selective C—H iodination of phenylacetic acid,benzylphosphonate and benzylsulfonate scaffolds with molecular I2 is developed using a pyridine-type template.The practical ester linkages enable the directing template easily installed and readily removed.The substrate scope is broad,and alkyl,methoxyl,trifluomethyl,and halo substituents are compatible with this reaction.Further transformations of ibuprofen iodide intermediates by Pd-catalyzed C—C and C-heteroatom bond formation illustrate the broad utility of this method.
