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Sonogashira cross-coupling reaction has become one of the most 15 important methods in the synthesis of aryl alkynes from aryl halides or triflates.1 Compounds bearing carbon-carbon triple bonds are often encountered in natural products, pharmaceuticals, biologically important molecules as well as in molecules with materials related applications.2 In a typical Sonogashira 20 procedure, the reaction has been conducted using a phosphaneincluding palladium complex with catalytic amount of copper(I) salt as catalyst in presence of an amine. Although copper would greatly increase the reaction rate, it induces unwanted homocoupled product of the terminal alkynes through a Hay/Glaser25 type reaction.3 Moreover, Cu-acetylide generated in situ is extremely sensitive to air and moisture, so the inert atmospheric conditions are required.4  W)MNPBFROAICJ4`TD]LP$`C.jpg |
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