The 5-endo-trig-type cyclization has been performed using a Pd-bis(isoxazoline) catalyst. The present cyclization of β,γ-unsaturated carbonyl compounds gave γ-butenolides and 3-pyrrolin-2-ones in good to excellent yields.

The reactions of [2+3] cycloaddition of pyridylnitrile oxides to vinyl- and allylgermanes proceed regioselectively and afford 5-Ge-substituted isoxazolines-2. We have synthesized 9 new pyridyl substituted 5-Si(Ge)-isoxazolines-2 and investigated their biological activity. The vasodilating, anticoagulant and cardioprotective activities of 5-Si(Ge) substituted isoxazolines-2 have been studied in ...

Aromatic and aliphatic oximes have been deoximated in chloroform-water to the corresponding aldehydes with dilute hydrogen peroxide and triscetylpyridinium tetrakis (oxodiperoxotungsto) phosphate as catalyst. The presence of dipolarophiles in the reaction mixtures allows a competitive reaction that converts oximes into isoxazole and isoxazoline derivatives via the intermediate formation of nitr...

Isoxazoline analogues of artemisinin were obtained in low yield and low diastereoselectivity from the 1,3-dipolar cycloaddition of nitrile oxides. Alternatively, starting from the aldehyde 7, a number of transformations--Wittig reaction and reduction, Henry reaction and cyanohydrin formation--were achieved in significantly higher yields. In the cases where a new stereocenter was introduced this...

A rapid and simple procedure was devised for the synthesis of multifunctionalized cyclic β-amino esters and γ-amino alcohols via the 1,3-dipolar cycloaddition of nitrile oxides to β-aminocyclopentenecarboxylates. The opening of the isoxazoline reductive ring to the corresponding highly functionalized 2-aminocyclopentanecarboxylates occurred stereoselectively with good yields.

BACKGROUND Isoxazoles exhibit interesting biological activities, and the 1,3-dipolar cycloaddition(13DC) reactions play an important role in both mechanistic and synthetic organic chemistry. Pyrazoles and annulated pyrazoles exhibit some diverse biological activities. They are used as antipyretic, analgesic drugs, tranquilizing, and herbicidal agents. Pyrazoles are also used extensively as usef...

In this work, it was of interest to synthesize new series of some 2-[(E)-2-furan-2-yl-vinyl]-quinazolin-4(3H)-ones incorporated into pyrazoline, isoxazoline, pyrimidine or pyrimidine-thione ring systems at position-3 of the quinazoline ring. The antimicrobial activity and antiinflammatory effect of some of these compounds were studied.

The asymmetric unit of the title compound, C(43)H(34)Cl(4)N(4)O(3), contains two crystallographically independent mol-ecules. In both mol-ecules, the pyrrolidine ring adopts a twist conformation, the oxindole units are slightly distorted from planarity and the isoxazoline ring adopts an envelope conformation. The crystal structure is stabilized by N-H⋯O hydrogen-bonding inter-actions giving one...

The five membered heterocycles isoxazolines are considered as important class of compounds in bioorganic and medicinal chemistry. They were treated as useful intermediates for transforming to large number of bioactive molecules. These classes of compounds were known to have varied biological activities. In this review, critical discussion has been made on synthetic methodologies developed, util...