Intermediates for the preparation of pharmaceutical thiophene co

Details Intermediates for the preparation of pharmaceutical thiophene co Intermediates for the preparation of pharmaceutical thiophene co

1992-07-30

1994-07-12

Raymond, Richard L.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546270, 549 9, C07D40904

Patent

active

053290160

ABSTRACT:
Thiophene compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, nitro, amino, halogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, nitro, amino, halogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, acyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, aryloxy-C.sub.1-4 alkyl, acyloxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl, acyloxy-C.sub.2-5 alkanoyl, C.sub.1-4 alkoxy-C.sub.2-5 alkanoyl, hydroxy-C.sub.2-5 alkanoyl, aryloxy-C.sub.2-5 alkanoyl or C.sub.2-5 haloalkanoyl; R.sup.3 is hydrogen, C.sub.1-8 alkyl, hydroxy-C.sub.1-4 alkyl, C.sub.2-5 alkanoyloxy-C.sub.1-4 alkyl, aryl, aryl-C.sub.1-4 alkyl, heteroaryl, heteroaryl-C.sub.1-4 alkyl or aryl, aryl-C.sub.1-4 alkyl, heteroaryl or heteroaryl-C.sub.1-4 alkyl substituted by at least one substituent selected from the group consisting of halogen, hydroxy, amino, nitro, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 alkanoylamino, C.sub.1-4 haloalkyl, acyloxy, C.sub.2-5 alkoxycarbonyl and carboxyl on the aromatic ring; m is 0, 1 or 2; n is 1 or 2; the bond represented by is a single bond or a double bond. Thiophene compounds (I) are useful as antianxiety drugs, hypnotics, antiepileptic drugs or nootropics. Thiophene compounds (II) are useful as intermediates for said thiophene compounds (I).

REFERENCES:
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patent: 4782057 (1988-11-01), Tahara et al.
patent: 4843075 (1989-06-01), Nakao et al.
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T. Yakushiji et al., Br. J. Pharmacol., 98, pp. 735-640, (1989).

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