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2.
Egyptian Journal of Chemistry. 1993; 36 (6): 497-503
em Inglês | IMEMR | ID: emr-27943

RESUMO

The considerable biological and medicinal activities of quinazoline derivatives as anti-inflammatory[1], antihypertensive[2] hypnotic[3] anti-adrenergic[4] and as fungicides[5] have stimulated the recent interest in the synthesis of derivatives of these ring systems. In continuation of our previous work [6] we have investigated a variety of synthetic routes to a number of quinazoline derivatives. Thus, we have found that the reaction of 4-chloro-2- [a-naphthylmethyl]-quinazoline [1] with aniline, benzylamine, and hydrazine hydrate in boiling butanol gives the corresponding 4-[anilino, benzylamino and hydrazino]-2- [alpha -naphthyl methyl]-quinazolines [2a-c]. However, treatment of [1] with sodium azide in boiling acetic acid gave the corresponding tetrazoloquinazoline derivatives[3]. Refluxing of [1] with acylhdrazines, namely cyanoacetyl hydrazine and benzoylhydrazine in boiling butanol gave the corresponding 3-[cyanomethyl or phenyl]-triazolo [3,4-a]-5 [alpha -naphthyl methyl]-quinazoline [4a and b]. In a recent series of publications [7,8], it has been reported that, the reaction of 4-chloroquinazoline with amino acids gave imidazo quinazoline derivatives. In the present investigation, the reaction of [1] with glycine in boiling butanol and the ring closure by Ac[2]O yielding 5-oxo-imidazo [3,4-a] -2- [[alpha -naphthyl methyl]-quinazoline [5]. Recently [6,9], It has been proved that 4-chloro-quinazoline is a useful precursor in the synthesis of fused nitrogen bridged benzopyrimidinoquinazoline. Similarly, we found that treatment of [1] with anthranilic acid in boiling butanol gave benzopyrimidinoquinazoline [6]


Assuntos
Quinazolinas/análogos & derivados
3.
Egyptian Journal of Pharmaceutical Sciences. 1992; 33 (3-4): 607-614
em Inglês | IMEMR | ID: emr-23713

RESUMO

Reactions of 5-formyl derivatives of uracil, 4-thiouracil and 2', 3',-0-isopropylideneuridine with glucosamine via Schiff base intermediate have been described. The antimicrobial activity of the prepared compounds has been also studied


Assuntos
Bases de Schiff , Farmacocinética
4.
Egyptian Journal of Chemistry. 1992; 35 (2): 243-52
em Inglês | IMEMR | ID: emr-107559
6.
Egyptian Journal of Pharmaceutical Sciences. 1991; 32 (3-4): 565-574
em Inglês | IMEMR | ID: emr-19752

RESUMO

The aminolysis of 2-benzamide [alpha-naphthylidene]-4H-3,1- benzoxazine-4-one 1 gave 2-benzamide, [alpha-naphthylidene]-4-[3H]- quinazolinone 2. The chlorination, benzoylation and Mannich reaction of 2 have been studied. Also, the behavior of 4-chloroquinazoline 4 towards acylhydrazides, sodium azide, alkylating agents, active methylene compounds and amino acid have been described


Assuntos
Estabilidade de Medicamentos , Farmacocinética
7.
Egyptian Journal of Pharmaceutical Sciences. 1991; 32 (3-4): 625-632
em Inglês | IMEMR | ID: emr-19757

RESUMO

The synthesis of 8-tert-butyl-6-hydroxy-4-methyl coumarin 2 was described. The nitration of compound 2 followed by reduction gave the amino coumarin derivative 5. The latter compound condensed with acetic acid in presence of P2O5 to give the benzoxazole derivative 6. Also, the compound 5 reacted with CS2 in presence of KOH/CH3OH to afford the benzoxazole-2-thione derivative 7. It has been found that the coumarin derivative 2 reacted with Grignard reagent by 1, 4 addition to give the products 8a,b


Assuntos
Composição de Medicamentos , Interações Medicamentosas
8.
Egyptian Journal of Pharmaceutical Sciences. 1990; 31 (1-4): 13-8
em Inglês | IMEMR | ID: emr-16021

RESUMO

P-aminoacetophenone was smoothly condensed with semicarbazide to produce the corresponding semicarbazone [1]. The latter compound was oxidized with SeO 2 to give 4-[p-aminophenyl-4-yl]-1, 2, 3- selenadiazole [II]. Compound [II] was allowed to react with aromatic aldehydes to afford the corresponding Schiff bases [III]. Cyclocondensation of mercaptoacetic acid and chloro- acetyl chloride with compound [III] to give thiazolidinones [IV] and azetidinones [V], respectively. The constitution of some of the prepared products is discussed through their microanalysis and infrared spectra. The biological activities of some of these compounds were tested


Assuntos
Química Farmacêutica
9.
Egyptian Journal of Chemistry. 1987; 30 (6): 497-505
em Inglês | IMEMR | ID: emr-107312
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