Synthesis and reactivity of 2-formylindole and 5-formylpyrrole derivatives

The methylation of 2-formyl-3-hydroxyindole was studied, and the sequence of introduction the methyl groups was traced by¹H NMR spectroscopy. The O-methyl, N-methyl, and N,O-methyl derivatives of 2-formylindole, and also the O-methyl and N-methyl derivatives of 2-methyl-3-ethoxycarbonyl-4-hydroxypyrrole were synthesized. Novel derivatives of indolyl- and pyrrolylacrylic acids were obtained on the basis of some O- and N,O-substituted aldehydes of the indole and pyrrole series.     

Synthesis and anti-fungal activity of 5-aminopyrazole derivatives]

4-Thiocyanato-5-amino or acylaminopyrazoles were prepared and their antifungal activity was tested against Candida albicans and Trichophyton mentagrophytes: the 4-thiocyanato-5-aminopyrazoles were the most effective in both tests.     

β-锗代-α-氨基酸衍生物的合成及抗肿瘤活性

自六十年代初期发现羧乙基锗倍半氧化物(Ge—132)广泛的生物活性以来,已有许多相应的有机锗化合物被发现,在抗肿瘤活性方面,因有毒性较低、抗瘤谱广等一系列优点而引起人们广泛的兴趣,但由于活性较低影响了应用及发展,据文献报道,有机锗倍半氧     

Synthesis of perhydropyrazino [1,2-c] pyrimidine derivatives

The reaction of 1-benzoyl-2-oxo-4,6-dihydroxyazetino-[3,2-d] pyrimidine (III) with diethanolamine affords the amide (IV). Heating of the last with SOCl2 yields 2-beta-chloroethyl-8-hydroxy-9-benzoylamino-perhydropyrazino [1,2-c] pyrimidine-1,6-dione (VI). Reaction of compound (VI) with different amines gives the respective 2-beta-aminosubstituted derivatives (VII-XIII). Some of the obtained compounds showed central activity.     

Synthesis of pyrazolo [4,5]pyridazine and isoxazolo [3,4d]pyridazine derivatives

Arylhydrazones of diethylacetondicarboxylate3 was treated with formaldehyde to give 1-aryl-4,5,6-trihydropyridaine derivatives4a-f Cyclization of compound4a-f by hydroxylamine afforded [3,4d] 1,3,4,5-tetrahydropyridazine derivatives5a-f. Also cyclization of compound4c with semicarbazide gave 1-amidopyrazolo-5-one-1-aryl-3-carboxypyridazine6. On the other hand compound3 reacted with ethylorthoformate to give diethyl-1,4-dihydro-1-arylpyridazine-4-one-2,5 dicarboxylate7, which on treatment with hydrazine, semicarbazide and thiosemicarbazide gave pyridazine, amido and thioamido derivatives. The spectral and antimicrobial data of these compounds1–8 were studied.     

Synthesis and analytical characterization of the dansyl derivatives of 6,14-ethenomorphinans]

The synthesis of the dansyl derivatives of the pharmacologically important 6,14-ethenomorphinans has not been reported. The authors realized the preparation of the dansyl derivatives (2a-i) of some 20-alkyl(aralkyl)-orvinols (1a-i). The authors unequivocally proved the structure of the parent compounds, and their dansyl derivatives. The authors also investigated certain analitical characteristics (thin-layer chromatography, UV-spectral data and reversed-phase HPLC purity tests) for the detection if necessary of these compound in biological fluid. Namely, due to the fluorescent properties of the dansyl derivatives, the sensitivity and selectivity of the analytical determinations of the parent compounds are significantly enhanced.     

Synthesis and antitumor properties of pyrazolo [3,4-D] pyrimidine derivatives

Several new 5-substituted 1-phenylpyrazole [3,4-d] pyrimidine derivatives were synthesized and tested for antitumor activity. Compound 17, which has 3,4-dichlorophenyl moiety at N5 of the pyrazole pyrimidine ring, shows a strong activity against L-1210 leukemia (152%). On the other hand, compounds 15, 17 and 21 were the most active against sarcoma Sa-180. It was observed that many derivatives of pyrazole [3,4-d] pyrimidine possess different biological, especially antitumor properties [1-6, 9, 10].