Ethyl 3-aminobut-2-enoates MeC(NHR)=CHCO2Et (R = H, Me, Bn) whose reaction site is C(2) atom add to 2-R-3-nitro-2H-chromenes at their C(4) atom to give the corresponding trans,trans-2,3,4-trisubstituted chromanes. Analogous substrates MeC(NR2)=CHCO2Et (NR2 is piperidin-1-yl or morpholin-4-yl) re...

Reactions of 1,3-di(tert-butyl)acetylacetone (2,2,6,6-tetramethyl-3,5-heptanedione), (tBu2acac)H, with tri(tert-butyl)aluminum, -gallium and -indium afforded selectively the corresponding di(tert-butyl)metal derivatives (tBu2acac)MtBu2 [M = Al (1), Ga (2), In (3)] by release of isobutane. Likewi...

As a continuation of our search for novel histamine H3 receptor ligands, a series of twenty four new tert-butyl and tert-pentyl phenoxyalkylamine derivatives (2−25) was synthesized. Compounds with three to four carbon atoms alkyl chain spacer were evaluated for their binding properties at human ...

The redox-active bis-chelate hexacoordinate ruthenium complex 2 Ru(ONO)2 comprising two redox-active 2,4,6,8-tetrakis(tert.-butyl)-9-hydroxyphenoxazin-1-one ligands 1 was synthesized by coupling ruthenium trichloride with 1 or its thallium salt. Reduction of 2 with zinc amalgam produces its radi...

A novel triamine (1) with tert-butyl side group, N1,N1-bis(4-aminophenyl)-4-(tert-butyl)benzene-1,3-diamine, is synthesized and then polymerized with the dianhydride 6FDA (A2) at the different feed molar ratio. Monitoring by 1H NMR spectrum, the reactivity of 3-amino group with ortho-tert-butyl ...

The compounds 5-(4-hydroxy-3-methoxy-phenyl)-3,7-dimethyl-5H-thiazolo[3,2-a]pyrimidine-2,6-dicarboxylic acid 2-ethyl ester 6-methyl ester (2a) and 3,7-dimethyl-5-naphthalen-1-yl-5H-thiazolo[3,2-a]pyrimidine-2,6-dicarboxylic acid diethyl ester (2b) were synthesized by the base catalyzed cyclocond...

N-(α-Ketoacyl)anthranilic acids were prepared by oxidative ring opening of 3-hydroxyquinoline-2,4(1H,3H)-diones by using paraperiodic acid (H5IO6) or sodium periodate (NaIO4). The optimisation of the reaction conditions is described as well as the utilisation of N-(α-ketoacyl)anthranilic acids...

A large laboratory scale synthesis of (S)-α-methylphenylalanine from benzaldehyde and methyl cyanoacetate has been developed. The synthesis is based on the following sequence: (i) preparation of racemic 2-cyano-2-methyl-3-phenylpropanoic acid, (ii) resolution of the enantiomers by crystallisati...

An efficient synthesis of (S)-α-benzyl-α-methyl-β-alanine in 59% overall yield from benzaldehyde and methyl cyanoacetate has been developed. Enantioconvergent approaches to the synthesis of the target α,α-disubstituted β-amino acid from both enantiomers of previously resolved 2-cyano-2-met...

The synthesis of some substituted arylamines is described. These substances were tested as antioxidants, both in liquid hydrocarbons and in polymers. Their effectiveness was compared with common additives and some conclusions about possibility of their use is made.

Chiroptical properties and X-ray diffraction were studied for both diastereomers of N-[(R)-1-phenylethyl]-2-(3,5-di-tert-butyl-4-hydroxyphenyl)propanamide, whose acid moiety is a chiral antioxidant.

3-(1H-benzo[d][1,2,3]triazol-1-yl)-1-(4-ethylphenyl)-1-oxopropan-2-yl-4-ethyl-benzoate (BEOE) has been synthesized and characterized by elemental analysis, IR, UV–vis and fluorescence spectroscopy. Its crystal structure has also been determined by X-ray single crystal diffraction. For the title...

The present paper describes the synthesis of novel ligand, N′-[(4-ethylphenyl)methylidene]-4-hydroxy benzohydrazide (HL) and its Co(II), Ni(II), Cu(II) and Cd(II) complexes. The ligand (HL) crystallizes in orthorhombic lattice in P212121 space group with a = 7.9941 (7) Å, b = 11.6154 (10) Å, c ...

Carbon nucleophiles generated by a non-nucleophilic base (LDA) were effectively trapped with di-tert-butyl dicarbonate (Boc-anhydride) to provide the corresponding tert-butyl aryl acetates, di-tert-butyl aryl malonates, unsymmetrical aryl malonates and tert-butyl benzoates in high yields. This r...

A novel, environmentally benign and single-step synthesis of 8-chloro-2-arylbenzo[b]furo[2,3-e]oxepin-10(4H)-ones by the photochemical irradiation of 2-{5-chloro-2-(prop-2-ynyloxy)benzoyl}-3-aryloxiranes has been developed. Some of these substrates also furnished hydroxyalkenones alongside. The ...

The vinylogues of furfurylamines, easily available in two steps from furylacroleins (3-(furyl)allylamines), were studied in a tandem N-acylation/intramolecular [4+2] cycloaddition with maleic, pyrocinchonic, and citraconic anhydrides, as well as furylacryloyl and cinnamoyl chlorides. By using a ...

Previous investigations have demonstrated metabolism of leukotriene (LT) C4in vivo involving transformations of the tripeptide, but not the fatty acid part, yielding N-acetyl LTE4 as a main biliary metabolite in the rat. In addition, several polar metabolites were detected in the same studies. T...

N-Acetyl-leukotriene E4, the end product of leukotriene C4 metabolism in the mercapturic acid pathway, was rapidly eliminated from the blood circulation into the bile of rats. Part of the N-acethyl-leukotriene E4 secreted from bile into the intestine undewent enterohepatic circulation. Leukotrie...

The in vitro antifungal activity of a novel series of cis- and trans-5-{[aryl or aryloxy (or thio)]methyl}-3-(1 H-imidazol-1-ylmethyl)-3-(2-thienyl)-2-methylisoxazolidines (13–24) was evaluated and compared with ketoconazole. The title series of compounds was prepared via a 1,3-dipolar cycloadd...

The synthesis of a novel class of antifungal agents, the 3-(2-furanyl)-3-(1H-imidazol-1-ylmethyl)-2-methyl-5-phenyl(or phenyloxymethyl)isoxazolidines (10–15) is described. When tested in vitro, derivatives 10–15 exerted a potent antifungal activity against dermatophytes, but were less effectiv...