Highly Efficient Coupling of Unstable Bicyclic Pyrimidines and Pyrazoles under Basic Conditions, and its Application to the Synthesis of Pharmaceutical Compounds

The efficient Pd-catalyzed coupling of unstable bicyclic pyrimidines and pyrazoles under basic conditions was established for the first time. The reactions proceeded with excellent yields without hydrolysis using Pd2( dba) 3, tBuXPhos, and K3PO4.

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Bibliographic Details
Published inSynlett Vol. 29; no. 14; pp. 1867 - 1870
Main Authors Goi, Takashi, Fukase, Koichi
Format Journal Article
LanguageEnglish
Published STUTTGART Thieme Medical Publishers 01.09.2018
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
bicyclic pyrimidine
bicyclic pyridine
Pd-catalyzed coupling
ARYL HALIDES
pyrazole
(t)BuXPhos
INHIBITORS
DERIVATIVES
PALLADIUM-CATALYZED AMINATION
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Summary:The efficient Pd-catalyzed coupling of unstable bicyclic pyrimidines and pyrazoles under basic conditions was established for the first time. The reactions proceeded with excellent yields without hydrolysis using Pd2( dba) 3, tBuXPhos, and K3PO4.
ISSN:0936-5214
1437-2096
DOI:10.1055/s-0037-1609906