Process for preparing pyrrolo(1,2-A)azepinone derivatives

Details Process for preparing pyrrolo(1,2-A)azepinone derivatives Process for preparing pyrrolo(1,2-A)azepinone derivatives

1987-11-04

1989-05-02

Daus, Donald G.

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

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

548408, 544143, 544373, C07D48706, C07D41314, C07D40314

Patent

active

048269743

ABSTRACT:
Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, or (B) R is phenyl optionally substituted with one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals and R.sub.1 and R.sub.2 together form a piperazine or homopiperazine ring substituted by hydroxyalkyl (2 to 4 C), alkenyl (2 to 4 C), alkynyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CN, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, the said alkyls containing, except where otherwise stated, 1 to 4 C in a straight or branched chain, and the pharmaceutically acceptable salts thereof, are useful as antipsychotics.

REFERENCES:
patent: 3239528 (1966-03-01), Bebenburg et al.
patent: 4148895 (1979-04-01), Lattrell et al.
Jones et al., CA97-23610r, "Azonia-azulene Salts", Part 5, Synthesis of 5H-pyrrolo[1,2-a]azepine and of 7H-pyrrolo-[1,2-a]azepine-7-one.
Jones et al., J. C. S. Perkin I, 1982, (4), pp. 1123-1130.

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