1-Substitution derivatives of 4-aryl-2,3-dibromo-1-naphthol

1981 ◽  
Vol 46 (9) ◽  
pp. 2116-2122 ◽  
Author(s):  
Jiří Křepelka ◽  
Jiří Roubík ◽  
Jiří Holubek
Keyword(s):  
Aqueous Medium ◽  
Ethyl Esters ◽  
Derivatives Of

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.

scholarly journals Chain Length of Amphipathic-Type Thioesters Dramatically Affects Reactivity in Aqueous Amidation Reactions with Cysteine Esters

SynOpen ◽  
2017 ◽  
Vol 01 (01) ◽  
pp. 0059-0062
Author(s):  
Ikumi Otomo ◽  
Kanna Watanabe ◽  
Chiaki Kuroda ◽  
Kenichi Kobayashi
Keyword(s):  
Amino Acid ◽  
Aqueous Medium ◽  
Chain Length ◽  
Ethyl Esters ◽  
Side Chain ◽  
Amino Acid Side Chain ◽  
Hydrophobic Properties ◽  
M 10 ◽  
Hexyl Ester ◽  
Close Proximity

The reaction of five amphipathic-type thioesters, CH3(CH2) m COS(CH2) n COONa (m + n = 12), with cysteine hexyl, butyl, and ethyl esters were studied in aqueous medium. Compounds with the thioester group in close proximity to the carboxylate moiety (m = 10, n = 2) afforded amides in almost quantitative yield, whereas no reaction proceeded by using compounds with the thioester group distant from the carboxylate. In contrast, no clear difference in yield was observed among the five amphipathic-type thioesters upon reaction with valine hexyl ester. The results indicate that the reaction is affected by both the position of the thioester group and the hydrophilic/hydrophobic properties of the amino acid side chain.

Derivatives of 4-(Aminomethyl)pyrrole-3-carboxylic Acid

1994 ◽  
Vol 47 (5) ◽  
pp. 975 ◽  
Author(s):  
DP Arnold ◽  
RFC Brown ◽  
LJ Nitschinsk ◽  
P Perlmutter ◽  
HK Tope
Keyword(s):  
Carboxylic Acid ◽  
Ethyl Esters ◽  
Tosylmethyl Isocyanide ◽  
Derivatives Of

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.

Derivatives of 5α-androstan-3α- and 3β-ol with acrylate side chain

1990 ◽  
Vol 55 (5) ◽  
pp. 1243-1256 ◽  
Author(s):  
Vladimír Pouzar ◽  
Hana Chodounská ◽  
Dalibor Sameš ◽  
Pavel Drašar ◽  
Miroslav Havel
Keyword(s):  
Ethyl Esters ◽  
Side Chain ◽  
Protecting Group ◽  
Derivatives Of

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.

scholarly journals Effects of Ethyl Ester Derivatives of Valproic Acid Metabolites on Pentylenetetrazol Seizures in Mice

1981 ◽  
Vol 8 (3) ◽  
pp. 259-261 ◽  
Author(s):  
J. Bruni ◽  
E.J. Hammond ◽  
B.J. Wilder
Keyword(s):  
Valproic Acid ◽  
Ethyl Ester ◽  
Adult Male ◽  
Anticonvulsant Activity ◽  
Ethyl Esters ◽  
Icr Mice ◽  
Acid Metabolites ◽  
Pentylenetetrazol Seizures ◽  
Derivatives Of

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.

Synthesis of N-(3-Azido-2-hydroxypropyl), N-(3-Phthalimido-2-hydroxypropyl) and N-(3-Amino-2-hydroxypropyl) Derivatives of Heterocyclic Bases

1994 ◽  
Vol 59 (5) ◽  
pp. 1153-1174 ◽  
Author(s):  
Maria Spassova ◽  
Hana Dvořáková ◽  
Antonín Holý ◽  
Miloš Buděšínský ◽  
Milena Masojídková
Keyword(s):  
Aqueous Medium ◽  
Cesium Carbonate ◽  
Subsequent Reaction ◽  
Weakly Alkaline ◽  
Basic Catalysis ◽  
Palladium On Carbon ◽  
Heterocyclic Bases ◽  
Derivatives Of

Alkylation of heterocyclic bases with azidomethyloxirane (I) under basic catalysis with potassium or cesium carbonate afforded N-(3-azido-2-hydroxypropyl) derivatives II. Hydrogenation of these compounds over palladium on carbon gave the corresponding 3-amino-2-hydroxypropyl derivatives III. The same compounds III were prepared by alkylation of heterocyclic bases with phthalimidomethyloxirane (VII) in the presence of cesium carbonate and subsequent reaction of the formed N-(3-phthalimido-2-hydroxypropyl) derivatives VIII with hydrazine. The phthalimido derivatives VIII are easily hydrolyzed already in weakly alkaline aqueous medium to give 9-[3-(o-carboxybenzoylamino)-2-hydroxypropyl] derivatives IX and X.

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