Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1986-07-23
1988-04-19
Jiles, Henry R.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C07D40300
Patent
active
047390727
ABSTRACT:
The invention relates to a process for the preparation of a compound of general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group, and one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represent a hydrogen atom or a C.sub.1-6 alkyl group;
or a salt or protected derivative thereof, by cyclization of a compound of general formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.
The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.
REFERENCES:
patent: 3592824 (1971-07-01), Schut
patent: 3892766 (1975-07-01), Zinnes
patent: 4259345 (1981-03-01), Cross et al.
J. Chem. Soc., J. A. Ballantine, et al., 1957, 2227-2231, "Bacteria. V. Some Acylindoles".
Bell James A.
Coates Ian H.
Eldred Colin D.
Ewan George B.
Humber David C.
Jiles Henry R.
Sanofi
Whittenbaugh Robert C.
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