ChemInform Abstract: Synthesis and Cytostatic Properties of 5-Substituted Derivatives of 3- Methylisoxazolo(5,4-d)1,2,3-triazine-4-ones and 3-Methyl-5-triazene-4- isoxazolecarboxylic Acid Ethyl Esters.

ChemInform ◽  
2010 ◽  
Vol 28 (36) ◽  
pp. no-no
Author(s):  
S. RYNG ◽  
W. MALINKA ◽  
D. DUS
Keyword(s):  
1981 ◽  
Vol 46 (9) ◽  
pp. 2116-2122 ◽  
Author(s):  
Jiří Křepelka ◽  
Jiří Roubík ◽  
Jiří Holubek

Alkylation of 7-ethyl-4-(4-ethylphenyl)-2,3-dibromo-1-naphthol (I) with ethyl esters of ω-bromoalkanoic acids XX-XXIII in a non-aqueous medium gave the 1-substitution derivatives II, IV, VI and VIII which were hydrolyzed to the acids III, V, VII and IX. The acid III was used for syntheses of the esters X-XIII and amides XIV-XVIII. Compounds II-XVIII exhibited moderate antineoplastic effects in animals with transplanted tumours; best results were observed with the compound II.


1994 ◽  
Vol 47 (5) ◽  
pp. 975 ◽  
Author(s):  
DP Arnold ◽  
RFC Brown ◽  
LJ Nitschinsk ◽  
P Perlmutter ◽  
HK Tope

Methyl and ethyl esters of 4-( aminomethyl )pyrrole-3-carboxylic acid were made through pyrrole synthesis with tosylmethyl isocyanide , but cyclization to a bicyclic lactam (1) was not achieved.


1990 ◽  
Vol 55 (5) ◽  
pp. 1243-1256 ◽  
Author(s):  
Vladimír Pouzar ◽  
Hana Chodounská ◽  
Dalibor Sameš ◽  
Pavel Drašar ◽  
Miroslav Havel

Hydroxy derivatives I, II, III, XVII and XX were oxidized to give the respective aldehydes IV, V, VI, XVIII and XXI which were further converted by Wittig-Horner reaction into unsaturated methyl and ethyl esters. Removal of the acetal protecting group in position 3 afforded methylesters X, XXIV and XXXVI and ethyl esters XIV, XXV and XXXVII. Compounds XXIV, XXV, XXXVI and XXXVII were converted into the corresponding hemisuccinates XXVIII, XXIX, XL and XLI and β-D-glucosides XXXII, XXXIII, XLIV and XLV.


Author(s):  
J. Bruni ◽  
E.J. Hammond ◽  
B.J. Wilder

SUMMARY:The anticonvulsant activity of the ethyl esters of the major valproic acid metabolites was assessed against minimal pentylenetetrazol seizures in adult male ICR mice. The ethyl ester 3-hydroxy-propylpentanoic acid was found to possess significant anticonvulsant activity.


1991 ◽  
Vol 56 (2) ◽  
pp. 439-448 ◽  
Author(s):  
Stanislav Rádl ◽  
Lenka Kovářová ◽  
Jiří Holoubek

N-Alkylation of IIIa, IIIb, IIId - IIIf and 9-acridanone with 3-bromopropyne in dimethyl sulfoxide in the presence of potassium carbonate yielded N-(2-propynyl) derivatives IVa - IVe and VIa, respectively. Ethyl esters IVa, IVb, and IVe were hydrolyzed to IVf - IVh, respectively. Compounds IVf, IVg, IVctreated with bases yielded N-propadienyl derivatives Va - Vc. On the other hand 2-substituted compounds IVd and IVh did not change under the same conditions. Compound VIa treated with powdered potassium hydroxide in dimethyl sulfoxide at room temperature yielded N-(1-propynyl) derivative VII.


1982 ◽  
Vol 47 (6) ◽  
pp. 1636-1640 ◽  
Author(s):  
Jan Beneš ◽  
Jiří Holubek

Using the Horner-Wittig reaction, aldehydes I and II were converted, with high E-selectivity, into ethyl esters of substituted acrylic acids, VI and VII. The N-anions generated by deprotonation of derivative I-V with sodium hydride in tetrahydrofuran reacted with vinyltriphenylphosphonium bromide with the formation of derivatives of pyrrolo[1,2-a]ergoline-I, XI-XV.


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