Letters in Organic Chemistry - Volume 16, Issue 10, 2019

Biscarbonylmethylenetriphenylphosphoranes are versatile compounds derived from stabilized α-carbonylmethylenetriphenylphosphoranes, mainly prepared by transylidation or by analogue methodologies; other procedures include electrochemical oxidation, palladium-catalized insertions and displacements reactions with tellurol esters, as well as the use of Bestmann’s ylide with different reagents and reaction conditions. Thes Read More

The selective functionalization of unactivated C(sp3)-H bonds has been regarded as an efficient and atom-economical approach for the formation of carbon-carbon or carbon-heteroatom bonds in modern organic synthesis. Especially, the oxidative activation of C(sp3)–H bonds adjacent to a heteroatom exhibits quite significant features in synthetic chemistry. For example, the direct functionalizations of amines, amides and et Read More

4-Methylenepiperidine hydrochloride 1 is a key intermediate for synthesis of the novel antifungal drug efinaconazole 2. In this work, a simple and robust process has been developed to synthesize 4-methylenepiperidine hydrochloride 1, with a high overall yield of 99.1% at a high purity of 99.7% in a large-scale. Moreover, this synthetic process avoided the uses of organolithium reagent and column chromatography process which Read More

The synthesis of a novel series of 1,3,5-trisubstitiuted pyrazoline was achieved by refluxing chalcone derivative with different heteroaryl hydrazines. The newly synthesized compounds were characterized by 1H NMR, 13CNMR, mass spectral and elemental analysis data. The synthetic series of novel pyrazoline hybrids was screened for in vitro schizont maturation assay against chloroquine sensitive 3D7 strain of Plasmodium falc Read More

A series of new bisarylidene Meldrum’s acid derivatives (3a-i) were prepared in high yield by a condensation reaction between Meldrum's acid and ether functionalized dibenzaldehyde, without any catalyst. Regardless of the nature of the substitution, all the reactions were completed within 2-3 hours in ethanol at reflux condition. In the reactions, the column purification of the products was not needed. The FT-IR, 1H-NMR, 13C-N Read More

Some new 1,3,4-thiadiazole compounds derived from 3,4-(methylenedioxy)cinnamic acid were synthesized in this study. Their structures were determined using UV-Vis, IR, 1H-NMR, and 13C-NMR spectroscopy. Moreover, the antibacterial activities of the new 1,3,4-thiadiazole derivatives were tested against Gram positive (Enterococcus durans, Bacillus subtilis, and Staphylococcus aureus) and gram negative (Salmonella ty Read More

A class of 1-((benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol derivatives (4a-t) has been synthesized in good yields through a three component coupling reaction. The newly synthesized compounds were evaluated for their in vitro antiproliferative activity against five cell lines such as DU145 (human prostate cancer), MDA-MB-B231 (human breast cancer), SKOV3 (human ovarian cancer), B16-F10 (mouse skin Read More

A multicomponent one-pot atom-economic reaction is performed for an efficient synthesis of 1-amidoalkyl-2-naphthol from aromatic aldehydes, β-naphthol and amide/urea promoted by hexachlorocyclotriphosphazene (HCCP). Various techniques such as stirring, microwave irradiation and thermal technique (hot plate and oil bath) were used in different solvents for the synthesis of 1- amidoalkyl-2-naphthol derivatives with Read More