Synthesis of novel spin-labeled crown ethers

Diazonium salts obtained from aminophenyl-substituted crown ethers react with paramagnetic imidazolinium salt to yield arylazoenamines, containing spin-labeled crown ethers. An alternative approach to the synthesis of related compounds, spin-labeled ureas, consists of the reaction of aminophenyl-substituted crown ethers with paramagnetic isocyanates.     

Synthesis of some spin-labeled inhibitors and a cholinesterase substrate

Conclusions Some new spin-labeled inhibitors and a cholinesterase substrate were synthesized.The data on the biological activity of the synthesized compounds will be published separately.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 10, pp. 2334–2336, October, 1971.     

Synthesis of ethophenprox analogs

The synthesis of ethophenprox analogs was performed by condensation of alcohols with benzyl halides under conditions of the phase transfer catalysis. The ultrasonic irradiation was shown to accelerate the reaction and to increase the yield of ethers. The trends in fragmentation of new generation pyrethroids under the electron impact were established. Insecticidal activity of the compounds obtained was evaluated.     

Synthesis of phthalascidin analogs

We report a new approach to obtain phthalascidin analogs. 6-Phthalimidomethylpyrazino[1,2-b]isoquinoline-1,4-dione (5a) was obtained in a one-pot N-alkylation/cyclization of the corresponding 1-acetyl-3-arylmethyl-2,5-piperazinedione with N-phthalylacetaldehyde dimethyl acetal. Chemoselective reduction of the C(1)-carbonyl group in the 3-arylmethyl-11,11a-dehydroderivative 9a was followed by cyclization of an acyliminium intermediate, to give the 6,15-imino-7-oxo-14,14a-dehydroisoquino[3,2-b]3-benzazocin 11a. Alternatively, the octacyclic compound 13a was obtained through a novel double cyclization of a precursor in which the C(1)-carbonyl and one phthalimide carbonyl group were reduced.     

Synthesis of melatonin analogs

Conclusions A number of melatonin analogs, containing dichloroacetic acid and various amino acid residues instead of an acetic acid residue, were synthesized.     

Synthesis of methaprogerol analogs

Novel synthetic approaches towards analogs of methaprogerol, the efficient wound healing drug, were developed. Several hitherto unknown compounds obtained exhibited in vivo activity similar to methaprogerol. 2-(3-Dimethylaminopropyl)-5-methylhex-4-enoic acid enhanced the efficacy of the treatment of diseases of various etiologies and different organ injuries by transplantation of mesenchymal stem cells (MSC) and MSC-derived cardiomyoblasts.     

Synthesis of analogs of juvenoids

Conclusions Structural analogs of juvenile hormone, viz., derivatives of C₁₀-C₁₄ aliphatic unsaturated acids, were synthesized on the basis of telomers of butadiene and isoprene with -sulfono esters and -keto sulfones.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 4, pp. 816–820, April, 1984.     

Synthesis of analogs of actinomycin

D, L-Valine derivatives of actinomycin and its chlorine analog have been synthesized. The replacement of the methyl groups in positions 4 and 6 of the chromophore of actinomycin by chlorine has practically no effect on the absorption spectrum of compounds of this class.For part I, see [5].     

Synthesis of analogs of actinomycin

Chlorine-containing analogs of the actinomycin chromophore-2-amino-4, 6-dichloro-3-phenoxazone-1,9-dicarboxylic acid and its methyl ester-have been synthesized.     

Synthesis of aza steroid analogs

Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 854–855, June, 1991.     

Synthesis of alkylated iridolactone analogs

Bicyclic δ-lactones, iridolactones analogs with an alkyl group at the bicyclic junction, are obtained from α-alkyl-α-hydroxymethylcyclopentanones via an intramolecular Horner-Wadsworth-Emmons reaction.     

Synthesis of diastereomeric ketoconazole analogs

Syntheses of trans-isomers of ketoconazole, and the corresponding des-acetyl, 1-methyl-, 1-formyl and 1-methanesulfonyl analogs were investigated. These isomers, along with the corresponding cis-diastereomers were characterized by their carbon-13 nmr spectra.     

Synthesis of indole analogs of tolan

A method for the preparation of indole analogs of tolan, viz., indolylphenylacetylene and di-indolylacetylene, from indolyl benzyl ketone and indolyl skatyl ketone, respectively, by reaction with a Vilsmeier—Haack reagent was developed. The synthesis of indolyl skatyl ketone and 3-(3-indolyl)-3-chloro-2-phenyl-2-propen-1-al was realized.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 956–958, July, 1980.     

Synthesis of ketomethylene analogs of dipeptides

A convenient method of synthesizing ketomethylene dipeptides by using homoallylic Grignard reagents as amino acid analog synthons is described.