A series of new 3-amino-N-phenyl-1H-indazole-1-carboxamides 10 have been prepared from commercially available phenyl isocyanate precursors 8 and 3-aminoindazole 9. Some of the synthesized compounds were evaluated for their in vitro antineoplastic activity against 60 human cell lines derived from...

Several new ethyl 1-methyl-5-(substituted 3,4-dihydro-4-oxoquinazolin-3-yl)-1H-pyrazole-4-acetates 2, substituted at 2 and, alternatively at, 6, 7 or 8 positions of the quinazolinone nucleus, were synthesised. The compounds were screened for their analgesic and antiinflammatory activities, acute...

Polyfluorinated arylhydrazones were synthesized starting from 1-(4-amino-tetrafluorophenyl)ethanone and polyfluorinated arylhydrazines by action of p-toluenesulfonic acid in good yields. The resulting mixtures of E- and Z-isomers were next treated with K2CO3 in MeCN at room temperature. Under th...

Styrene oligomers with perfluoro[1-(2-fluorosulfonyl)ethoxy]ethyl end-groups have been synthesized with moderate to high yields (52–97%) via radical oligomerization by using perfluoro[2-(2-fluorosulfonyl)ethoxy]propyonyl peroxide (PPP) at various reactant ratios of styrene over PPP (80, 160, 24...

We evaluated the effect of combining 2′-O-[2-[2-(N,N-dimethylamino)ethoxy]ethyl] (2′-O-DMAEOE), a 2′-cationic modification, with a 2′,4′-constrained 2′-O-ethyl nucleic acid (cEt BNA) on the activity of an antisense oligonucleotide (ASO) using PTEN as a model target. Our results suggest tha...

The highly versatile 1-[(2-trimethylsilyl)ethoxy]ethyl (SEE) group, readily obtainable from an alcohol and 2-(trimethylsilyl)ethyl vinyl ether in the presence of a catalytic amount of PPTS, has been developed for the protection of hydroxyl groups. Its deprotection can be achieved under virtually...

The one-step preparation of diethyl 2-ethoxy-6-CF3-2H-pyran-3,5-dicarboxylate via the condensation of ethyl 4,4,4-trifluoroacetoacetate with CH(OEt)3 has been reported and a plausible mechanism for this transformation is discussed. To demonstrate the synthetic potential of the obtained pyran, th...

In this communication, synthesis of mesoporous nickel oxalate and its catalytic activity in ozonation of 2-ethoxy ethyl acetate (2-EEA) was reported. The mesoporous nickel oxalate was synthesized by simple method without using any template. The XRD and HR-TEM analyses indicated the formation of ...

A series of thirty N-(phenoxy)alkyl or N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols has been designed, synthesized and evaluated for anticonvulsant activity in MES, 6 Hz test, and pilocarpine-induced status epilepticus. Among the title compounds, the most promising seems R-(−)-2N-{2-[2-(2,6-dimet...

Aim of the study was evaluation of anxiolytic, antidepressant, anticonvulsant and analgesic activity in a series of a consistent group of compounds. A series of eleven new N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives has been obtained. Their affinity towards 5-HT1A, ...

The aim of this study was to design and synthesize COX-1/COX-2 balanced inhibitors incorporating the structural motifs of anti-inflammatory ascidian metabolites. We designed a series of substituted indole analogs that incorporate the key structures of the ascidian metabolites, herdmanines C and ...

Various derivatives and analogs of isocoumarins, including benzo-fused isocoumarins, thiaisocoumarins, telluroisocoumarins, hydrazinoisocoumarins, in addition to the α-pyranone fused with heteroaryl ring are known. The strategies and approaches used for the synthesis of isocoumarins were also e...

This review presents a systematic survey of the literature (through the end of 2017) that reports on the reactivity of 3-pyrrolin-2-ones. The discussion starts with site-specific reactivity (N, C2, C3, C4, and C5), followed by reactions across the C3–C4 π-bond, and then transformations of 3-py...

CoCl2 catalyzes effectively the chemoselective reduction of phenyl carboxylic esters to the corresponding saturated alcohols in high yields using NaBH4 at ambient conditions. By employing this methodology, the synthesis of (R)-tolterodine, a muscarinic receptor antagonist, has been achieved in h...

Tetrahydroquinoline A is a potent inhibitor of the cholesterol ester transfer protein (CETP), a target for the treatment of low HDL-C and atherosclerosis. Low HDL-C has been identified as a key risk factor for cardiovascular disease in addition to high LDL-C, the target of the statin drugs. Tetr...

Annulation of 3-nuclofugal phthalides, also known Hauser annulation is a unique reaction for the synthesis of quinonoids embodying the peri‑oxygenated naphthalenes and their higher homologs. It involves the reaction between a C3-nucleofugal phthalide and an acceptor molecule with polarized multi...

Reactions of ethyl 2-acyl-3-ferrocenylacrylates (acyl = acetyl, benzoyl, p-nitrobenzoyl) with guanidine and 1,1-dimethylguanidine furnish ethyl 2-amino-6-ferrocenyl-4-methyl(aryl)-1,6-dihydropyrimidine-5-carboxylates. Their oxidative dehydrogenation with PhI(OAc)2 results in the corresponding et...

This chapter principally describes the chemical literature of epoxides, aziridines, and azirines for the year 2016, while other three-membered heterocycles, such as oxaziridines and diazirines, receive limited coverage. As in previous years, this account does not provide an exhaustive list but i...

In this chapter the chemistry and structural aspects of three-membered saturated and unsaturated nitrogen, oxygen, and sulfur heterocycles with monoheteroatoms such as aziridine, 1H-azirine, 2H-azirine, oxirane, oxirene, thiirane, thiirane-1,1-dioxide, thiirene, thiirene-1-oxide, and thirene-1,1...

A comprehensive overview on methods applied for syntheses of β-amino-α-trifluoromethyl alcohols, including stereocontrolled variants, is presented. In addition, reported cases of the exploration of β-amino-α-trifluoromethyl alcohols for the preparation of trifluoromethylated peptidomimetics ...