Rhodium-catalyzed asymmetric conjugate addition to R,âunsaturated ketones and related compounds is now well-recognized to be one of the most efficient methods of introducing aryl and alkenyl groups with high enantioselectivity.1 On the other hand, asymmetric conjugate addition of alkynyl groups has not been welldeveloped in spite of its high synthetic utility.2 A most straightforward and conven...

Reaction of ethyl (Z)-3-(heteroaryl/aryl)-2-((triphenyl-λ5-phosphaneylidene) amino) acrylates intermediates with 2,3-thiophenedicarboxaldehyde was used in novel Tandem three consecutive reactions: aza-Wittig, imine condensation and electrophilic heteroaromatic cyclization to obtain a series indolizines. A tentative mechanism this reaction is proposed.

Aberrant epigenetic changes are known to contribute to various phases of tumor development. The gene function loss caused by aberrant methylation is analogous to genetic mutations. Unlike genetic mutations, epigenetic alterations can be reversed. 5-Aza-2'-deoxycytidine (5-aza-CdR) has been approved by the Food and Drug Administration for the treatment of certain types of cancer, such as MDS and...

New chiral bifunctional thiourea-phosphonium salts have been developed based on natural amino acids as highly efficient phase-transfer catalysts in the enantioselective aza-Henry reaction.

BACKGROUND Dietary polyphenols, such as those found in green tea and red wine, are linked to antitumor activity. They are known to influence many signaling pathways epigenetically within the human body. In this regard, CPUK02 (15-Oxosteviol benzyl ester) is a new ent-kaurenoid derivative of stevioside and exhibits strong anti-cancer activity in vitro and in vivo. Nowadays, the role of epigeneti...

We have presented a near-infrared fluorescent probe Lyso-JN for the detection of nitroxyl (HNO) in cells and in vivo. Lyso-JN is comprised of three moieties: an Aza-BODIPY fluorophore, a HNO-response modulator, diphenylphosphino-benzoyl, and a lysosomal locator, alkylmorpholine. The detection mechanism is based on aza-ylide intramolecular ester aminolysis reaction with HNO. The probe holds the ...

The title compound, C(24)H(21)N(3)O, was prepared by the reaction of (Z)-2-(1H-indol-3-ylmethyl-ene)-1-aza-bicyclo-[2.2.2]octan-3-one with α-bromo-p-toluonitrile, under phase-transfer catalytic (PTC) conditions using triethyl-benzyl-ammonium chloride and 50% w/v aqueous NaOH solution in dichloro-methane. The crystal structure indicates the presence of a double bond with Z geometry connecting th...