Reaction of tryptamine 1 with dimethyl -3-methoxyallylidenemalonate 2 afforded N?-[4,4-bis (methoxycarbonyl)-1,3-butadienyl] tryptamine 3 which in combination with acetylchloride and pyridine in dichloromethane gave N?, N?-[acetyl]-[(4,4-dinethoxycarbonyl) 1,3butadienyl] tryptamine 4. Treatment of 3 with sodium hydroxide afforded 2H[N-(3-indolyl) ethyl] 2-oxo-3-methoxycarbonyl-1-pyridine 5. Cy...

a few analogues of atevirdine or 1-[(5-methoxyindol-2-yl) carbonyl]-4-[3- (ethylamino)-2-pyridyl] piperazine – an anti-hiv belonging to non-nucleoside reverse transcriptase inhibitors were synthesized and evaluated for anti-hiv activity. replacement of indolyl moiety with 2-alkylthio-1-benzyl-5-imidazolyl substituent afforded 1-[2-(alkylthio-1-benzyl-5-imidazolyl) carbonyl]-4-[3-(isopropylamino...

An unprecedented technique for the in situ generation of indolyl ortho-quinodimethanes from 2-methylindole-based methylenemalononitriles by amine-mediated remote C(sp(3) )-H deprotonation was developed. These intermediates were efficiently trapped by diverse enals to provide a rapid entry to 2,9-dihydro-1H-carbazole-3-carboxyaldehyde structures through a formal asymmetric [4+2] eliminative cycl...

Triethylborane (TEB) was found to be a mild, efficient, and acid catalyst in electrophilic substitution reaction of indoles with aldehydes compounds to afford the corresponding bis(indolyl)methanes. Vibrindole A (5) and bis(indolyl)methanes derivatives 16 and 18 were synthesized using this methodology. Compound 16 is an intermediary in the synthesis of the natural bisindoles arsindoline B (2) a...

reaction of tryptamine 1 with dimethyl -3-methoxyallylidenemalonate 2 afforded n?-[4,4-bis (methoxycarbonyl)-1,3-butadienyl] tryptamine 3 which in combination with acetylchloride and pyridine in dichloromethane gave n?, n?-[acetyl]-[(4,4-dinethoxycarbonyl) 1,3butadienyl] tryptamine 4. treatment of 3 with sodium hydroxide afforded 2h[n-(3-indolyl) ethyl] 2-oxo-3-methoxycarbonyl-1-pyridine 5. cyc...

the use of quantitative structure–activity relationships, since its advent, has becomeincreasingly helpful in understanding many aspects of biochemical interactions in drug research.this approach was utilized to explain the relationship of structure with biological activity ofantibacterial. for the development of new fungicides against, the quantitative structural–activityrelationship (qsar) an...