Letters in Organic Chemistry - Volume 16, Issue 6, 2019

Cu-Fe spinels promoted the Ferrier rearrangement of 2-nitroglycals with several O-nucleophiles. 2,3-Unsaturated carbohydrate derivatives were prepared by the reaction of 3,4,6-tri-Oacetyl- 2-nitroglucal and alcohols in the presence of 5 % of CuFe2O4. After separation of the catalyst with an external magnet, the reaction products were obtained in good yields and high stereo and regioselectivity. Also, S- and heterocyclic C-3 s Read More

A series of novel hydroxy-pyran–chalcone hybrid compounds 4(a-b), 5(a-f), 7(a-b) & 8(a-f) has been synthesized by employing simple methods in various approaches through convergent synthetic strategies. 4-hydroxy-3-acetylcoumarin and 3-acetyl-4-hydroxy-6-methyl-2H-pyran-2-one have been used as starting materials and were condensed with indole aldehyde, pyrrole aldehydes independently to give the corresponding c Read More

A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, Read More

4-Aryl-2-amino-4H-chromenes possessing N,N-dimethylamino group have been reported as potential anticancer drugs. Despite few synthetic methods reported in the literature for their synthesis, there appear to be no reports on the direct use of N,N-dimethyl-3-aminophenol for the synthesis of 4- aryl-2-methylamino-3-nitro-4H-chromenes. One-pot condensation of N,N-dimethyl-3-aminophenol, aromatic aldehydes a Read More

In this report, two new steroidal glycosides were isolated and determined from n-butanol fraction of A.asphodeloides. The structures were confirmed in comparison with the spectral data of known compounds by using different spectroscopic analysis approaches including 1D & 2D-NMR techniques and HRMS. The anti-proliferation screening against cancer cell lines A549 and HeLa indicated that compound 1 exhibited goo Read More

Two ether and one ester derivatives of the 4-nitro-3-hydroxybenzoic acid were synthesized and characterized. The in vitro antimicrobial and cytotoxic activities of the three novel compounds were also evaluated. The aromatic derivatives showed antibacterial activity against one of the four microorganisms tested and two compounds (C8 and NOBA) had a lower IC50 in HeLa cells.

A method for the synthesis of aryl trifluoroethyl ethers from fluoroalcohols and diaryliodonium salts in the presence of NaH and warm 1,2-dichloroethane has been developed. This transition metal free reaction is mild and facile. Various functional group including electron-withdrawing and electron-donating substrates in the diaryliodonium salts were tolerated in this transformation to afford the products in moderate to high yields.

A proficient, microwave mediated methodology using CuFe2O4 nanoparticle as the catalyst for S-arylation of substituted benzene boronic acids with thiophenol has been developed. In this method, the substituted thioethers were easily obtained through a C-S bond formation using microwave irradiation technique as well as conventional heating in the presence of CuFe2O4 nanoparticles with modest to excellent yields with the l Read More

An efficient and rapid synthesis of a new class of chiral oxime ethers has been achieved via two-step reaction in which the first step is the reaction of oximes 1a-f with ethyl bromoacetate in the presence of sodium hydride to give oxime ethers 2a-f which are subsequently, in the second step, reacted with different commercially available chiral amines under microwave irradiation conditions to give compounds 3a-l in good to ex Read More

The 3+2 cycloaddition reactions are important to generate five-membered heterocyclic compounds as well as altering biological activity effects based on structure. In the study, we synthesized new isoxazoline derivatives of different monoterpenoids and examined the structure analysis using spectroscopical analysis methods, reveal changes in the theoretical analysis related to the biological activity. These new compounds exh Read More

Efficient steps towards the synthesis of novel (phenyl)(1'-aryl-1,5,5'-triphenyl[3,3'-bi-1Hpyrazol]- 4-yl)methanones 4a-e were developed. The procedure starts from 1-(4-benzoyl-1,5-diphenyl- 1H-3-pyrazolyl)-3-phenyl-2-propyn-1-one (2) which was synthesized by a palladium catalyzed crosscoupling reaction. Compound 2 reacted with various hydrazines to give (E)-(phenyl)[1,5-diphenyl-3- [3-phenyl-1-(2-arylhydrazono)- Read More

A series of 3-arylspiro[oxirane-2,3'-thiochroman]-4'-one derivatives were synthesized and characterized by spectroscopy like 1H NMR, 13C NMR, mass spectrometry and elemental analysis. They were evaluated for their anti-lung cancer activity on human lung cancer cell line A-549 in DMSO. Compounds under study were found to be potent anti-lung cancer agents with GI50 values less than 10 with respect to positive control adriamycin.