- 3H-Indolium Salts Efficiently Prepared from N-Substituted Anilines and α-Branched Ketones by an One-pot Synthesis
-
Starting with the N-substituted anilines 4/12 and the α-branched ketones 3 the 3H-indolium salts 1 and their fused derivatives 13 are prepared by combining a sodium nitrite nitrosation, a zinc dust reduction, a hydrazone formation and a Fischer indolization to a reaction sequence in which the isolation and purification of intermediates is not necessary. The scope and limitations of this effective one-pot synthesis are discussed.
- Zimmermann, Thomas,Brede, Ortwin
-
-
Read Online
- AMIDRAZONES 9. CONVENIENT SYNTHESIS OF 1-ALKYL-1-PHENYLHYDRAZINES AND α,β-UNSATURATED AMIDRAZONES VIA BASE-PROMOTED REACTIONS OF 1,1-DISUBSTITUTED-3-AMNIO-4,5-DIHYDRO-1H-PYRAZOLIUM SALTS.
-
A simple, efficient procedure for the conversion of phenylhydrazine to 1-alkyl-1-phenylhydrazines via base-promoted hydrolysis of 1-alkyl-3-amino-4,5-dihydro-1-phenyl-1H-pyrazolium iodides (2) is described.N',N'-disubstituted hydrazones of trans-cinnamamide and acrylamide are obtained by Hofmann-type ring openings of 1,1-disubstituted-3-amino-4,5-dihydro-5-phenyl (or 5-unsubstituted) -1H-pyrazolium halides (5,7).
- Smith, Richard F.,Olson, Laurie A.,Ryan, William J.,Coffman, Karen J.,Galante, Julienne M.,et al.
-
p. 585 - 596
(2007/10/02)
-
- Pharmaceutical formulations
-
Heterocyclic compounds of formula (I) STR1 and their acid addition salts, when administered topically, exhibit anti-inflammatory activity and do not produce the side-effects associated with the administration of certain other anti-inflammatories. The compounds of formula (I) may be administered topically as the compound alone or in a suitable topical pharmaceutical formulation.
- -
-
-
- Therapeutically active 3-amino-1-phenyl(and substituted phenyl)-2-pyrazolines
-
This disclosure describes certain 3-amino-1-phenyl-2-pyrazolines and 3-amino-1-substituted phenyl-2-pyrazolines and their C4 and C5 analogs useful for meliorating the inflammation and/or the progressive joint deterioration characteristic of arthritic disease, preventing the onset of asthmatic symptoms and allergic diseases, or as analgesic, antibacterial or antifungal agents.
- -
-
-
- 3-Trifluoroacetylamino-1-aryl-2-pyrazolines
-
This disclosure describes novel 3-substituted amino-1-phenyl-2-pyrazolines and 3-substituted amino-1-mono and disubstituted phenyl-2-pyrazolines and their C4 and C5 analogs, useful for meliorating the inflammation and/or the progressive joint deterioration characteristic of arthritic disease, preventing the onset of asthmatic symptoms and allergic diseases, or as analgesic, antibacterial or antifungal agents.
- -
-
-
