Publication Date:
2015-09-15
Description:
A novel strategy for the construction of the phthalazin-1(2 H )-one scaffold has been developed by means of a copper-mediated cascade C–H/C–H coupling and intramolecular annulations and a subsequent facile hydrazinolysis. This C–H activation transformation proceeds smoothly with wide generality, good functional tolerance and high stereo- and regioselectivity under mild conditions. Through the removal of the directing group, the resulting moiety could easily be transformed into the phthalazin-1(2 H )-one scaffold, which is known to be a privileged moiety and a bioactive nucleus in pharmaceuticals. Beilstein J. Org. Chem. 2015, 11, 1624–1631. doi:10.3762/bjoc.11.177
Keywords:
C–H activationcopperphthalazin-1(2H)-one
Electronic ISSN:
1860-5397
Topics:
Chemistry and Pharmacology
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