The reaction of N-aryl-substituted ketenimines with N,N-disubstituted cyanamides or (MeS)2C=N-CN under high pressure afforded 4-(N,N-disubstituted amino) or 4-(MeS)2C=N-substituted quinazoline derivatives, respectively. These products were formed by [4+2] cycloaddition between the aza-diene moieties of the N-arylsubstituted ketenimines and cyano groups. A 4-(unsubstituted amino)quinazoline deri...

The rhodium-catalyzed regio- and enantioselective amination of racemic tertiary allylic trichloroacetimidates with a variety of aniline nucleophiles is a direct and efficient route to chiral α,α-disubstituted allylic N-arylamines. We describe the first dynamic kinetic asymmetric transformations of racemic tertiary allylic electrophiles with anilines utilizing a chiral diene-ligated rhodium cata...

The cycloisomerization reactions of allenes bearing cyclic acetal, thioacetal and dithioacetal subunits, when triggered either by the catalytic action of AgSbF6 or by one equiv. of CF3COOH, gave rise to four different classes of indeno-fused 1,4-dioxa, oxathia and dithia heterocycles, in most cases as a single diastereomer. Acyclic acetals and dithioacetals are also suitable starting materials ...

2,10-Disubstituted phenothiazines are the best drugs in psychiatry. Several methods for their analysis have been reported in the literature. The official methods are based on non-aqueous titration or spectrophotometry. Various oxidizing agents have been used for the spectrophotometric determination of 2,10-disubstituted phenothiazines, e.g. Ce(SO4)2, NH4VO3, K2S208, KIO4, KIO3, KBrO3, FeCl3, Na...

The convenient, high yielding and diastereoselective synthesis of α-amino-β-substituted-γ,γ-disubstituted butyric acid derivatives was carried out by a three-component tandem reaction of a chiral equivalent of nucleophilic glycine. The reaction was performed smoothly under mild conditions and enabled the construction of two or three adjacent chiral centers in one step, thus affording a novel an...

The stereocontrolled synthesis of trans-disubstituted cyclopropylketones has been achieved from beta-alkyl, gamma-benzoyl phosphine oxides via a three-step cascade reaction incorporating an acyl transfer, phosphinoyl transfer and cyclisation to form the cyclopropane. Using Evans' chiral oxazolidinone auxiliary and by masking the phosphine oxide moiety as a phosphine borane we have extended the ...

Ethyl diazoacetate (EDA), which is easily prepared from ethyl glycinate and NaNO2, reacts in situ with alkynes a water micelle environment without organic solvent to form pyrazoles. The reaction pH dependent, as the presence of protic catalysis (H2SO4 4 %, 3.5) mixture 3,5- 4,5-disubstituted pyrazoles was obtained, while, at 5.5, only 3,5-disubstituted isomer obtained. surfactant TPGS-750-M cru...

3,5-disubstituted-2,6-dicyanoaniline derivatives have been synthesized via the reaction of aryl methylene- and 1-arylethylidenemalonodinitriles using 1,8-diazabicyclo[5.4.0] undec-7-ene (DBU) as ...

An efficient method for the synthesis of 1,2-disubstituted benzimidazoles has been developed from 1,2‐diaminobenzenes and aldehydes using 1-butyl-3-methylimidazolium ([Bmim]BF4) as a catalyst under solvent-free conditions. Various products were obtained in good to excellent yields microwave irradiation. The features some advantages such short reaction time, environmentally benign conditions, si...

A straightforward and reliable method for the regioselective synthesis of steroidal 1,4-disubstituted triazoles and 1,5-disubstituted tetrazoles via copper(I)-catalyzed cycloadditions is reported. Heterocycle moieties were efficiently introduced onto the starting azide compound 3β-acetoxy-16β-azidomethylandrost-5-en-17β-ol through use of the "click" chemistry approach. The antiproliferative act...