Intermediates for synthetic use and processes for producing amin

Details Intermediates for synthetic use and processes for producing amin Intermediates for synthetic use and processes for producing amin

1996-01-18

1998-01-13

Shah, Mukund J.

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

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544 61, C07D29528, C07D29532

Patent

active

057081727

DESCRIPTION:

BRIEF SUMMARY
DESCRIPTION

1. Technical Field
The present invention relates to novel industrial processes excellent in yield and purity for preparing aminopiperazine derivatives and pharmaceutically acceptable salts thereof and to novel synthetic intermediates thereof and is useful in a pharmaceutical field.
2. Background Technology
The processes for preparing aminopiperazine derivatives of the present invention are described in an international patent application (international publication number W091/01979) published based on the Patent Cooperation Treaty. By the said processes, however, isolation and purification of intermediate products are not necessarily easy owing to water-solubility thereof or the like and mass production of the aminopiperazine derivatives was difficult.


DISCLOSURE OF INVENTION

One object of the present invention is to provide novel processes for preparing the aminopiperazine derivatives and pharmaceutically acceptable salts thereof which possess the potentiation of the cholinergic activity and are useful for treating disorders in the central nervous system, especially for treating amnesia, dementia, senile dementia, and the like in human being.
Another object of the present invention is to provide novel synthetic intermediates useful for the processes for preparing the aforesaid aminopiperazine derivatives and pharmaceutically acceptable salts thereof.
The synthetic intermediates of the present invention are novel and can be represented by the following general formula: ##STR5## wherein R.sup.1 is hydrogen or benzyloxycarbonyl, R.sup.2 is cyclo(lower)alkyl, aryl or ar(lower)alkyl, each of which may be substituted with halogen, ##STR6##
According to the present invention, the aminopiperazine derivatives of the object compound (I) and pharmaceutically acceptable salts thereof can be prepared by the following processes. ##STR7## wherein R.sup.2 and Y are each as defined above, R.sup.3 is lower alkyl, aryl, ar(lower)alkoxy or heterocyclic group, each of which may be substituted with halogen, ##STR8## or lower alkylene and R.sup.1.sub.a is benzyloxycarbonyl. ##STR9## wherein R.sup.2, R.sup.3, A and Y are each as defined above.
In the above and subsequent descriptions of the present specification, suitable examples of the various definitions to be included within the scope of the invention are explained in detail as follows.
The term "lower" is intended to mean 1 to 6 carbon atom(s),unless otherwise indicated.
Suitable "lower alkyl" may include a straight or branched one such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, t-butyl, pentyl, hexyl, and the like, in which the preferable one is methyl.
Suitable "aryl" may include phenyl, naphthyl, tolyl, xylyl, mesityl, cumenyl, and the like, in which the preferable one is phenyl or naphthyl.
Suitable "ar(lower)alkoxy" may include benzyloxy, phenethyloxy, phenylpropoxy, benzhydryloxy, trityloxy, and the like.
Suitable "heterocyclic group" may include saturated or unsaturated monocyclic group containing at least one hetero-atom such as nitrogen, oxygen and sulfur atom.
Preferable "heterocyclic group" thus defined may be unsaturated 3 to 8-membered (more preferably 5 or 6-membered) heteromonocyclic group containing 1 to 4 nitrogen atom(s), for example, pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyridyl N-oxide, dihydropyridyl, tetrahydropyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl, triazolyl, tetrazinyl, tetrazolyl, etc.; (s), for example, indolyl, isoindolyl, indolizinyl, benzimidazolyl, quinolyl, isoquinolyl, indazolyl, benzotriazolyl, etc.; atom(s) and 1 to 3 nitrogen atom(s), for example, oxazolyl, isoxazolyl, oxadiazolyl, etc.; atom(s) and 1 to 3 nitrogen atom(s), for example, morpholino, sydnonyl, etc.; and 1 to 3 nitrogen atom(s), for example, benzoxazolyl, benzoxadiazolyl, etc.; atom(s) and 1 to 3 nitrogen atom(s), for example, thiazolyl, isothiazolyl, thiadiazolyl, etc.; atom(s), for example, thienyl, etc.; and 1 to 3 nitrogen atom(s), for example, benzothiazolyl, benzothiadiazolyl, etc.; atom, for example, furyl, etc.; for exampl

REFERENCES:
patent: 3200120 (1965-08-01), Lovell
patent: 3200121 (1965-08-01), Lovell
patent: 4983606 (1991-01-01), Casagrande et al.
patent: 5250528 (1993-10-01), Oku et al.

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