“…Recently, the intramolecular variant of the aza-Michael reaction has been reported. 65 The (E)-1-(3,5-dimethyl-1H-pyrazol-1-yl)-7-(tosylamino)hept-2-en-1-one derivatives (3) have an NH group, whose acidity is increased by the tosyl substituent, suitable to give addition to the β-position of the α,β-unsaturated carbonyl moiety. The organocatalyst of choice is the squaramide incorporating cinchona alkaloid (S,S,R)-XXIVa (R′ = ethyl) that, in cylopentyl methyl ether (CPME) at 50−90°C, activates the approach to the β-Si face of the substrate to afford several derivatives with the (S)-1-(3,5-dimethyl-1H-pyrazol-1-yl)]-2-(1-tosylpiperidin-2-yl)-1-ethanone scaffold (S)-131.…”