Microwave-assisted synthesis of novel spiro isoxazolidine derivatives

Abstract

α-N-substituted furan derivatives as new dipolarophiles have been employed in 1,3-dipolar cycloaddition reaction with α-chloro nitrones under microwave irradiation and found to afford exclusively novel regioselective 5-spiro cycloadducts with high yield in a very short reaction time.

Synthesis of N,N-diallylanilines by the reaction of anilines and allyl bromide in the presence of Mg–Al hydrotalcites at ambient temperature

Abstract

Anilines react with two equivalents of allyl bromide in aqueous ethanol in the presence of Mg–Al hydrotalcites (Mg/Al = 5, 3, 2) at room temperature to give N,N-diallylanilines in good yield. Hydrotalcites (HTs) are mild and efficient catalysts, which can be easily recovered and reused. In this project, efforts are made to check the activity of the calcined and uncalcined HTs. Also, the methodology can be extended for the synthesis of various N,N-diallylanilines.

An efficient,catalyst free synthesis of 3-(2′'-benzothiazolyl)-2,3-dihydroquinazolin-4(1H)-ones in aqueous medium

Abstract

An efficient and environmentally benign protocol for the synthesis of 3-(2′-benzothiazolyl)-2,3-dihydroquinazolin-4(1H)-ones has been developed. The synthesis of these pharmacologically important compounds can be achieved by the three component condensation of isatoic/5-chloroisatoic anhydride, aldehyde, and 2-aminobenzothiazole in water: ethanol (1:1, v/v) without the aid of any catalyst.

A green synthesis of 3,4-dihydropyrimidin-2-ones and 1,5-benzodiazepines catalyzed by Sn(HPO4)2.H2O nanodisks under solvent-free condition at room temperature

Abstract

Heterogeneous Tin (IV) hydrogen phosphate nanodisks [Sn(HPO4)2.H2O] efficiently catalyzed the one-pot three component condensation of aromatic aldehydes, β-ketoesters and urea to produce 3,4–dihydropyrimidin-2-ones under solvent-free conditions at room temperature. Also, the catalyst is equally applicable for the preparation of 1,5–benzodiazepines under the same reaction conditions. The optimum load of the catalyst required is 10 mole% and reusable. Hence, the process is green.

Deprotection Chemistry Mediated by ZrOCl2 · 8H2O: An Efficient,Mild, and Green Method for the Conversion of Oximes to Carbonyl Compounds in Aqueous Acetone

Abstract

Less-toxic, moisture-stable, inexpensive, and ecofriendly zirconium oxychloride octahydrate (ZrOCl₂ · 8H₂O) in aqueous acetone (1:1) mediates the conversion of oximes to carbonyl compounds in moderate to good yields. This green methodology is applicable to both aldoximes and ketoximes with tolerance to >C?C<, -NO₂, -OH, and -Cl groups. The reaction and workup are simple.

Synthesis of 10-Hydroxycamptothecin: Evaluation of New Moderators for the Chemoselective Reduction of Camptothecin

Abstract

10-Hydroxycamptothecin is prepared by chemoselective catalytic hydrogenation of the B-ring of camptothecin over PtO₂ with sulfur moderators followed by oxidation using iodobenzenediacetate. New moderators (viz. thioanisole, dimethyl sulfide, diphenyl sulfide, 2-mercapto ethanol), which moderate the hydrogenation of the B- ring of camptothecin, are being explored.

Samarium Triflate–Catalyzed Biginelli Condensation: An Improved Method for the Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones

Abstract

A simple and efficient method for multicomponant synthesis of 3,4-dihydropyrimidinones has been reported. All the reactions were carried out using samarium triflate as catalyst (10 mol%) at acetonitrile reflux. This procedure is applicable to a variety of substrates such as aliphatic, aromatic, and heterocyclic aldehydes.

Convenient and Efficient Synthesis of Some Novel Fused Thieno Pyrimidines Using Gewald's Reaction

Abstract

Several functionalized thienopyrimidines were synthesized by a facile synthetic method, which includes Gewald's reaction, and were characterized by spectral and analytical data. These functionalized thienopyrimidines were converted to various new chemical entities of biological importance, such as 2-piperazinymethyl thienopyrimidines (6, 8), 4-dimethylaminoethoxy thienopyrimidines (11), and 3-dimethylaminoethyl thienopyrimidines (12). All the compounds thus synthesized were screened for their invitro biological activities. Some of the compounds displayed promising serotonin 5-HT₆ receptor antagonist activities.