The front cover illustrates the diastereoselective formation of condensed heterocyclic ring systems by domino reaction sequences. dominoes toppling each other represent steps sequences, transformation initiating next one. mechanism cyclization is tunable choice reagent, affording four different systems. A novel mild nitroarenes to N-hydroxyindoles, in which deoxygenation carried out an intramol...

An efficient stereocontrolled route to ( )-cylindricine C is described. Reaction of 9-hydroxynon-1-en-5one oxime with 2,3-bis(phenylsulfonyl)-1,3-butadiene affords a 7-oxa-1-azanorbornane cycloadduct in high yield. The formation of the bicyclic isoxazolidine arises from conjugate addition of the oxime onto the diene to give a transient nitrone that spontaneously undergoes an intramolecular dipo...

A new intramolecular Lewis acid catalyzed hetero-Diels-Alder reaction of N-arylimines 5 with nonactivated olefins tethered to the 2-azadiene system was developed in order to prepare 1,2,3,4,4a,9,9a,lO-octahydroacridine derivatives 6. Both reactivity and cis/ trans selectivity of 6 were mainly dependent on the substitution pattern in the 3-position of the cyclization precursor 5. The type of Lew...

Oxoisoaporphine alkaloids are conveniently prepared via direct ring metalation of alkoxy-substituted isoquinolines at C-1, followed by reaction with iodine. Subsequent Suzuki cross-coupling of the resulting 1-iodoisoquinolines to methyl 2-(isoquinolin-1-yl)benzoates and intramolecular acylation of the corresponding carboxylic acids with Eaton's reagent afforded five alkaloids of the oxoisoaporp...

We have described an efficient gold-catalyzed double cyclization of 1,5-enynes to afford a range of heterobicyclic compounds, including oxabicylclo[3.2.1]octenes, azabicyclo[3.2.1]octenes, oxaspiro[5.4]decene, azaspiro[5.4]decene, oxaspiro[5.5]undecene, oxabicyclo[4.3.0]nonene, azabicyclo[4.3.0]nonene, and oxabicyclo[4.4.0]decene. The mechanism of this reaction is proposed to involve a chemosel...

A useful aminohalogenation reaction for the cyclization of O-alkynyl carbamates under copper catalysis has been developed. N-Halosuccinimides have used as a halogen source. The intramolecular C−N bond formation occurs selectively affording haloalkylidene substituted heterocycles. Just in case α,α-cyclohexyl-substituted propargyl carbamate, alkoxyhalogenation pathway was operative. mechanism two...

A method was proposed for the synthesis of substituted 2-(2-(furan-2-carbonyl)hydrazono)-4-oxobutanoic acids by reaction 2,4-dioxobut-2-enoic with furan-2-carbohydrazide. It found that undergo intramolecular cyclization in presence propionic anhydride to form corresponding N'-(2-oxofuran-3(2H)-ylidene)furan-2-carbohydrazides. The anti-inflammatory activity obtained compounds studied. have prono...