Microwave-Assisted Regioselective Synthesis of 3-Functionalized Indole Derivatives via Three-Component Domino Reaction.

A microwave-assisted regioselective synthesis of 3-functionalized indole derivatives via a three-component domino reaction of anilines, arylglyoxal monohydrates, and cyclic 1,3-dicarbonyl compounds is described. The main advantages of this protocol are short reaction times, practical simplicity, its metal-free nature, the availability of starting materials, green solvents, and high regioselectivity.

An efficient one-pot synthesis of functionalized chromeno[4,3-b]pyridine derivatives under catalyst-free conditions.

A concise, efficient one-pot synthesis of functionalized chromeno[4,3-b]pyridine derivatives via a three-component reaction of 4-oxo-4H-chromene-3-carbaldehydes, malononitrile or cyanoacetates, and aromatic amines under catalyst-free conditions in an environmentally friendly medium (ethanol-water, 3:1 v/v) is described. This synthesis involves a group-assisted purification process, which avoids traditional recrystallization and chromatographic purification methods.

Multicomponent Strategy to Pyrazolo[3,4-e]indolizine Derivatives under Microwave Irradiation.

A simple and efficient one-pot construction of pyrazolo[3,4-e]indolizine derivatives via a diethylamine-catalyzed three-component domino reaction of arylglyoxals, cyclic 1,3-diones, and 5-aminopyrazoles under microwave irradiation is described. In this one-pot transformation, seven bonds and two new rings are efficiently formed. This synthesis was confirmed to follow the group-assisted-purification (GAP) chemistry process, which can avoid traditional recrystallization or chromatography purification methods.

Multicomponent strategy to indeno[2,1-c]pyridine and hydroisoquinoline derivatives through cleavage of carbon­carbon bond.

A concise and efficient three-component domino reaction has been developed for the synthesis of polyfunctionalized indenopyridine and hydroisoquinoline derivatives via the cleavage of a C­C bond under transition-metal-free conditions. This reaction provides facile access to complex nitrogen-containing heterocycles by simply mixing three common starting materials in EtOH in the presence of 20 mol % NaOH under microwave irradiation conditions.

Efficient synthesis and evaluation of antitumor activities of novel functionalized 1,8-naphthyridine derivatives.

An efficient synthesis of novel functionalized 1,8-naphthyridine and chromeno[2,3-b]quinoline derivatives via cascade reaction of 2-chloroquinoline-3-carbaldehyde and enaminones or cyclic 1,3-dicarbonyl compounds was developed. All of the 1,8-naphthyridine derivatives synthesized were evaluated for their antiproliferative properties in vitro against cancer cells and several compounds were found to have high activities.

Highly selective synthesis of functionalized polyhydroisoquinoline derivatives via a three-component domino reaction.

Two series of novel functionalized polyhydroisoquinoline derivatives have been synthesized via the three-component domino reaction of glutaraldehyde and malononitrile with a series of ß-ketoamides under microwave irradiation conditions in the presence of a catalytic amount of Et3N (10 mol%). This reaction represents the first reported process for the facile conversion of a ß-ketoamide to a hydroisoquinoline via a C-N bond cleavage reaction without the need for a multistep reaction process.

Microbial transformation of sinenxan A, a rich constituent in callus cultures of Taxus / 药学学报

<p><b>AIM</b>To study the microbial transformation of sinenxan A.</p><p><b>METHODS</b>Choose two strains of Fungi (Mucor spinosus AS 3.3450 and Cunninghamella echinulata AS 3.3400) and a strain of bacterium (Proteus vulgaris AS 1.1208) to transform the substrate.</p><p><b>RESULTS</b>Three products were obtained and identified as 10-deacetylsinenxan A1, 6 alpha-hydroxy-10-deacetylsinenxan A2 and 9 alpha-hydroxy-10-deacetylsinenxan A3 respectively.</p><p><b>CONCLUSION</b>Sinenxan A is facile to be transformed by microorganisms, the 10-acetyl group of which is an active group.</p>