In(OTf)3-mediated synthesis of substituted pyridazines
2015
Zhang, Mengyang | Lu, Yi-Ju | Cheng, Yu-Chieh
In(OTf)3 (4c)-mediated one-pot (4+2) cyclocondensation of γ-alkynones 3 with N2H4(aq) in dioxane affords substituted pyridazines 5 in good yields via a sequential desulfonative or dehydrogenative aromatization. The facile transformation proceeds by a facile synthetic sequence starting with an α-propargylation of β-ketosulfones 1 and a cyclocondensation of γ-alkynones 3 with N2H4(aq). The method provides a mild and efficient condition. Moreover, this route can be enlarged to multigram scale.
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