Phthalazinone moiety

Wang J, Wang M, Liu C, Zhou H, Jian X. Synthesis of poly(arylene ether nitrile ketone)s bearing phthalazinone moiety and their properties. Poiym Bull 2013 70(5) 1467-81. 

Y. Song, J. Wang, G. Li, Q. Sun, X. Jian, J. Teng, H. Zhang, Synthesis, characterization and optical properties of fluorinated poly(aryl ether)s containing phthalazinone moieties. Polymer 49 (23) (2008) 4995-5001. 

YE. Liang, Study on Sulfonated Poly(Aryl Ether)s Containing Phthalazinone Moieties as Proton Exchange Membranes (Doctoral degree paper), Dalian University of Technology, China, 2007. 

Condensation of these substrates with hydrazine derivatives normally occurs with ehmination of the alkyhmino moiety of the substrate to afford l,4(2//,3f0-phthalazinediones. However, abnormal cases have been reported in which the said moiety is retained to afford 4-alkylamino-l(2f/)-phthalazinones. The following examples illustrate both outcomes. 

Encouraged by the results obtained with DRF-2189 and PATS A, we modified the heterocycle further with insertion of heteroatoms as well as an oxo group on the heterocycle (Scheme 19.10). The novel compounds generated are the subject matter of several patents. The activities of the compounds when the Het moiety is phthalazinone and benzoxa-zinone are compiled in Table 19.5. PHT46 (entry 1, Table 19.5) was found to be a better PPARy activator than pioglitazone and was found to normalize the PG levels at a dose of 10 mg/kg per day and to reduce TG levels by 51% in db/db mice treated for 10 days. 

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