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Copper/6-methylpicolinic acid catalyzed coupling reaction of substituted 5-bromopyrimidin-4-amines with alkynes and subsequent cyclization took place in DMSO at 100–110°C to afford 2-chloro-pyrrolo[2,3-d]pyrimidines in moderate to excellent yields. Variable functional groups, including aromatic and aliphatic groups, could be introduced at the 6 and 7 positions using this method.
CuI/sodium picolinate-catalyzed direct arylation of α-substituted cyanoacetates takes place at 60°C in the presence of Cs 2 CO 3 and 4Å molecular sieve, affording 2-alkyl-2-arylcyanoacetates in good to excellent yields. Both electron-rich and electronic-deficient aryl iodides, and some functionalized α-substituted cyanoacetates are compatible with the reaction conditions, thereby allowing...
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