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The known DNMT inhibitor SGI-1027 4 has been synthesized using as key steps Pd-catalyzed Ar–N bond formation reactions performed in a sequential or convergent manner. In the former approach, a by-product, which corresponds to the incorporation of two units of 4-chloroquinoline, was also isolated. The biological effects of compound 4 in the U937 human leukemia cell line are also described.
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