Process for preparing indole derivatives containing a 1,2,4-tria

Details Process for preparing indole derivatives containing a 1,2,4-tria Process for preparing indole derivatives containing a 1,2,4-tria

1995-01-20

1996-10-22

Morris, Patricia L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

5482664, C07D40114, C07D40314, C07D40306, C07D40304

Patent

active

055678190

ABSTRACT:
A process for preparing tryptamine derivatives and related compounds having a 1,2,4-triazol-1-yl moiety within the molecule comprises reacting 4-amino-1,2,4-triazol with a nitrobenzene derivative containing a readily displaceable group; deaminating the aminotriazolium salt thereby obtained by treatment with nitrous acid followed by neutralisation; reducing the triazolyl-nitrobenzene derivative thereby obtained by transfer hydrogenation; treating the triazolyl-aniline derivative thereby obtained with nitrous acid and then with an alkali metal sulphate, followed by acidification; and subsequently reacting the triazolyl-hydrazine derivative thereby obtained in situ with a suitable carbonyl compound, to obtain the required triazolyl-indole derivative.

REFERENCES:
Eur. J. Med. Chem, vol. 24 (1989) 537-540, "Synthesis And Antimycotic Activity Of New (1H-1,2,4-Triazol-1-YL-Methyl)Benzeneamine Derivatives" by M. Scalzo et al.

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