• Archives of Pharmacal Research
• /
• v.13 no.3
• /
• pp.274-277
• /
• 1990

It has been found that $\alpha, \beta$-unsaturated nitrile derivatives 1-3 reached with S- methylisothiourea to give the prpone derivatives 4-6 respectively. Cyclisation of 4-6 using ethanolic hydrochloric acid afforded the pyridine derivatives 7-9 in good yields. On the other hand, the reactions of hydrazine hydrate and of phenylhydrazine with each of 7-9 gave the corresponding pyrazolopyridine derivatives 10-15. The structures of the newly synthesised derivatives were assigned on the basis of elemental analyses, IR and $^1H$-NMR spectral data studies.

• YAKHAK HOEJI
• /
• v.35 no.2
• /
• pp.73-84
• /
• 1991

Quinoline, pyrazolo-[5, 4-b]-pyridine, isoxazolo-[5, 4-b]-pyridine, pyrazolo-[4, 3-c]-quinoline, isoxazolo-[5, 4-e]-thiazine, and isothiazolo-[5, 4-e]-thiazine derivatives were prepared as possible antiinflammatory agents. Some of the synthesized compounds showed antiinflammatory activities comparable to Aspirin and Naproxen.

• Archives of Pharmacal Research
• /
• v.17 no.6
• /
• pp.411-414
• /
• 1994

Phenylazocyanothioacetamide 1 reacts with malononitrile to afford the pyridinethione 4 which reacts with phenacylbromide to yield the pyridine-S-phenacyl derivative 6, 1 reacts with ethyl cyanoacetate to yield the pyridazine derivative, 8, and with phenacyl bromide to afford the N-phenacyl derivative 11, instead of the thiazole 10. Compound 11 afforded the pyrazolopyridine 13 on reaction with malononitrile while 10 was obtained on coupling of the thiazole 14 with diazotised aniline. Compound 10 reacts with malononitrile to afford the thizaolyl pyridazine 15. Compound 1 reacts with malononitrile dimer to afford the pyriodopyridazine derivative 17a. 1 reacts also with active methylene heterocycies to afford the pyrazolo and thiazolo-fused phridazines 20 and 23 respectively.