Site-selective Suzuki-Miyaura coupling of heteroaryl halides - understanding the trends for pharmaceutically important classes.

نویسندگان

  • Joshua Almond-Thynne
  • David C Blakemore
  • David C Pryde
  • Alan C Spivey
چکیده

Suzuki-Miyaura cross-coupling reactions of heteroaryl polyhalides with aryl boronates are surveyed. Drawing on data from literature sources as well as bespoke searches of Pfizer's global chemistry RKB and CAS Scifinder® databases, the factors that determine the site-selectivity of these reactions are discussed with a view to rationalising the trends found.

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Site-selective Suzuki–Miyaura coupling of heteroaryl halides – understanding the trends for pharmaceutically important classes† †Electronic supplementary information (ESI) available: Notes on mixed halide–triflate heterocycles and details of the Pfizer RKB and CAS Scifinder® searches. See DOI: 10.1039/c6sc02118b Click here for additional data file.

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Suzuki-Miyaura cross-coupling reaction catalyzed using highly efficient CN-dimeric ortho-palladated complex under microwave irradiation and conventional heating

Suzuki cross-coupling reaction of different aryl halides with arylboronic acids was successfully carried out in methanol using ortho-palladated complex of 2-methoxyphenethylamine. All substrates afforded the corresponding products in good to high yields in the presence of low amounts of this complex as efficient and active catalyst. Application of microwave irradiation improved the yields of th...

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عنوان ژورنال:
  • Chemical science

دوره 8 1  شماره 

صفحات  -

تاریخ انتشار 2017