Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1996-05-20
1998-02-10
Morris, Patricia L.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C07D24912
Patent
active
057171041
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-ni-trobenzene 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:
Cram a Hammond, "Organic Chemistry"; 2nd Ed, pp. 565-567, (1964).
Eur. J. Med. Chem., vol. 24 (1989) 537-540, "Synthesis and Antimycotic Activty of New (1H-1,2,4-triazol-1-yl-methyl) benezeneamine derivatives" by M. Scalzo et al.
Merck Sharp & Dohme Ltd.
Morris Patricia L.
North Robert J.
Winokur Melvin
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