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A [4+2]‐cycloaddition of para‐quinone methides with hexahydro‐1,3,5‐triazines is reported. The reaction occurs under very mild conditions (catalyst‐, ligand‐, and base‐free), exhibits a broad substrate scope and excellent functional group tolerance, and affords a series of biologically important 1,3‐benzoxazine derivatives in good to excellent yields. Moreover, the successful late‐stage functionalization...
An efficient asymmetric dearomative [3+2] cycloaddition reaction of 2‐nitroindoles and 2‐nitrobenzothiophenes with 3‐isothiocyanato oxindoles was developed by using a chiral Zn(OTf)2/bis(oxazoline) complex as a catalyst. With the developed protocol, a range of enantioenriched complex heterocyclic compounds containing three contiguous stereocenters, one of which is spirocyclic center, could be obtained...
The synthesis of several monomeric and dimeric steroidal [1,2,4]triazolo[1,5-a]pyrimidines (TPs) derived from steroids are described. These derivatives were prepared from α,β-unsaturated carbonyl compounds through a Claisen Schmidt condensation and rearrangement of the spiro moiety followed by a cycloaddition with 3-amino-1,2,4-triazole. The antiproliferative activity of compounds 7, 13–15 was tested...
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