In the aza-Morita–Baylis–Hillman reaction of N-sulfonated imines with methyl vinyl ketone (MVK) promoted by chiral phosphine Lewis base: (R)-2'-diphenylphosphanyl[1,1']binaphthalenyl-2-ol (LB1) (10 mol %), the aza-Morita–Baylis–Hillman adducts were obtained in good yields with high ee (70–94 % ee) at –30 °C in THF. The scope and limitations of this reaction have been disclosed.

The development of a stereoselective aza-Piancatelli reaction to access 4-aminocyclopentenones is reported. This transformation relies on the use chiral o-sulfinyl anilines as inductors afford targeted products in good excellent yields. Remarkably, high value-added cyclopentenones could be obtained drs up >95:5, depending upon furan substitution pattern.

A Cu-catalyzed new sequence involving the Ullmann type intermolecular C-C followed by an intramolecular C-N coupling and then intramolecular aza-Michael type addition (and oxidation) in a single pot afforded various fused N-heterocyclic acetic acid derivatives as inhibitors of PDE4.

Highly efficient silicone surfactants are typically based on polyether hydrophiles. As part of a program to increase the natural content silicones, we describe synthesis with amino acid hydrophiles (cysteine, arginine, and lysine). The compounds were prepared using radial thiol–ene reaction vinylsilicones for cysteine derivatives catalyst-free aza-Michael arginine lysine. Short chain monomer:hy...

Initially, lasubin II was synthesized diastereoselectively in racemic form [3]. Asymmetric syntheses of lasubin II were achieved based on stereoselective transformations of enantiomerically pure substrates [4] or, for example, via a diastereoselective aza-Diels-Alder reaction using a resolved chiral arylaldehyde tricarbonylchromium complex [5]. Recently, an enantioselectively catalyzed aza-Diel...

The title compound, C(31)H(34)N(2)O(9), is a product of the Michael addition of the cyclic secondary amine subunit of the (bis-pidino)aza-14-crown-4 ether to dimethyl acetyl-ene-dicarboxyl-ate. The mol-ecule comprises a tricyclic system containing the aza-14-crown-3 ether macrocycle and two six-membered piperidinone rings. The aza-14-crown-3-ether ring adopts a bowl conformation with a dihedral...

Novel β-aminocyclobutanecarboxylic acid derivatives were prepared via a sequential solvent-free aza-Michael addition of benzophenone imine across 3-halopropylidenemalonates and base-induced ring closure. These highly substituted cyclobutanedicarboxylic acid derivatives were subjected to a reactivity study which demonstrated the tendency of these donor-acceptor substituted four-membered rings to...

A highly enantioselective intramolecular 6-exo-trig aza-Michael addition was developed to afford chiral 3-substituted 1,2-oxazinanes in high yields (up to 99% yield) and good enantioselectivities (up to 98/2 er). These reactions were enabled by a quinine-derived primary-tertiary diamine as a catalyst and pentafluoropropionic acid (PFP) as a co-catalyst.

Various tetrasubstituted pyrroles/pyrazoles have been prepared from nitro-substituted 1,3-enynes with aromatic amines/hydrazines via a copper-catalyzed cascade aza-Michael addition, cyclization and aromatization at room temperature. This protocol is also effective for the synthesis of tetrasubstituted pyrazoles in high yields.