Simple and Efficient Synthesis of Belinostat

A novel synthesis of belinostat (1) starting from 3-nitrobenzaldehyde has been developed. The key step in this sequence involves the conversion of (2E)-3-(3-aminophenyl)acrylic acid methyl ester to (2E)-3-(3-chlorosulfonylphenyl)acrylic acid methyl ester via diazotization and sulfonylation.     

Asymmetric Inductive Synthesis of α-Aminoaryl-Acetic Acids in Chiral Micellar System

In the micellar solution of chiral surfactant N-hexadecyl-N-methylephedrine bromide, seven α-amino-arylacetic acids were synthesized from corresponding aldehydes, the e.e.% being about 28%.     

Carbon-Carbon Bond Formation Reaction Promoted by Cadmium In Aqueous Media

Promoted by metallic cadmium allylilic and propargyl bromides react smoothly with aldehydes in aqueous DMF to give homoallylic and homopropargyl alcohols in moderate to good yields. It can also promote pinacol coupling of aromatic aldehydes. The metallic cadmium is produced in situ by the reduction of CdCl₂ H₂O with samarium metal.     

Wang Resin Bound Addition Reactions Under Microwave Irradiation

The addition reaction process of Wang resin bound amines with isocyanates was monitored directly using a FTIR method. It showed that the reaction process was greatly enhanced under microwave irradiation.     

Cleavage of S-S Bond by Sm/cat. CoCl2 or Sm/cat. CoCl2 • 6H2O System: A Novel Method for the Synthesis of Thiolesters

Abstract

The Sm/cat. CoCl₂ or Sm/cat. &;Cl₂ ? 6H₂O system promoted disulfides to react with anhydrides or acyl chlorides to afford thiolesters in good yields under mild and neutral conditions.     

Organic Reactions in Ionic Liquids: Ionic Liquid Ethylammonium Nitrate–Promoted Knoevenagel Condensation of Meldrum's Acid With Aromatic Aldehydes

The Knoevenagel condensation of Meldrum's acid with aromatic aldehydes proceeded efficiently in a reusable ionic liquid, ethylammonium nitrate, at room temperature in the absence of any catalyst with high yields.     

Total Synthesis of α-Elvucitabine

Total synthesis of α-elvucitabine was achieved in 26% overall yield by a concise nine-step procedure starting from L-lyxose, with trimethylsilyl trifluoromethaneoulfonate (TMSOTf)–mediated stereocontrolled α-N-glycosidation and olefination through Barton–McCombie deoxygenation being the key steps, and the stereochemistry of the product was determined by nuclear Overhauser effect spectroscopy.     

Novel Route to Functionalized Indans via Formal [3 + 2] Cycloadditions of 1-Benzylbenzotriazoles with Alkenes

α-Functionalized 1-benzylbenzotriazoles (3, 4 and 12), derived from the lithiation of 1-(2,3-dimethoxybenzyl)benzotriazole 2 followed by reactions with electrophiles, or from the condensation of benzyl alcohol 11 with benzotriazole, undergo formal [3 + 2] cycloadditions with styrenes upon treatment with ZnBr₂ to give functionalized indans (9, 10, 13 and 14).     

Efficient Friedländer Synthesis of Quinoline Derivatives from 2-Aminoarylketones and Carbonyl Compounds Mediated by Recyclable PEG-Supported Sulfonic Acid

2-Aminoarylketones undergo smooth condensation with α-methylene ketones in the presence of 10 mol% of poly(ethylene glycol) (PEG)–supported sulfonic acid under mild reaction conditions to afford the corresponding poly-substituted quinolines in excellent yields. The catalyst can be recovered by simple filtration and can be recycled in subsequent reactions. The method is simple, cost-effective, and environmentally benign.     

Green Method for the Synthesis of Benzo[f]pyrimido[4,5-b]quinoline Derivatives Catalyzed by Iodine in Aqueous Media

A convenient one-pot synthesis of benzo[f]pyrimido[4,5-b]quinoline derivatives is described via three-component reaction of benzaldehydes, naphthalen-2-amine, and barbituric acid at room temperature in aqueous media catalyzed by iodine. Compared with other methods, this three-component reaction used a green solvent, gave good yields, and was operationally simple.