# US 5,708,172 A · Intermediates for synthetic use and processes for producing aminopiperazine derivatives

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- Number: US 5,708,172 A
- Document ID: US5708172A
- Status: Granted
- Kind: A
- Application number: 08/553,551
- Filed: 1996-01-18
- Granted: 1998-01-13
- Earliest claimed: 1993-06-18
- Assignees: Fujisawa Pharmaceutical Co., Ltd.
- Inventors: Teruo Oku; Hiroshi Kayakiri; Hirokazu Tanaka
- Web page: https://patentgrep.com/patent/US5708172A

## CPC

- C07D 295/32: acylated with carboxylic or carbonic acids, or their nitrogen or sulfur analogues
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

A novel industrial process excellent in yield and purity for preparing a compound of the formula: ##STR1## or a salt thereof, which comprises reacting a compound of the formula: ##STR2## or a salt thereof with a compound of the formula: R.sup.3 --A--OH or its reactive derivative or a salt thereof, wherein R.sup.2 is cyclo(lower)alkyl, aryl or ar(lower)alkyl, each of which may be substituted with halogen, R.sup.3 is lower alkyl, aryl, ar(lower)alkoxy or heterocyclic group, each of which may be substituted with halogen, A is ##STR3## or lower alkylene and ##STR4##

## Claims

### Claim 1

A compound of the formula: ##STR10## 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 and ##STR11## or a pharmaceutically acceptable salt thereof.

### Claim 2

N-(4-benzyloxycarbonyl-1-piperazinyl)-4-fluorobenzamide.

### Claim 3

A process for the preparation of a compound of the formula: ##STR12## or a pharmaceutically acceptable salt thereof which comprises reacting a compound of the formula: ##STR13## or a pharmaceutically acceptable salt thereof with a compound of the formula:
R.sup.3 --A--OH
or its reactive derivative or a pharmaceutically acceptable salt thereof,
wherein R.sup.2 is cyclo(lower)alkyl, aryl or ar(lower)alkyl, each of which may be substituted with halogen,
R.sup.3 is lower alkyl, aryl, ar(lower)alkoxy or heterocyclic group, each of which may be substituted with halogen, ##STR14##

### Claim 4

A process for the preparation of a compound of the formula: ##STR15## or a pharmaceutically acceptable salt thereof, which comprises i) subjecting a compound of the formula: ##STR16## to elimination reaction of the benzyloxycarbonyl group to give a compound of the formula: ##STR17## or a pharmaceutically acceptable salt thereof and then ii) reacting the compound obtained or the pharmaceutically acceptable salt thereof with a compound of the formula:
R.sup.3 --A--OH
or its reactive derivative or a pharmaceutically acceptable salt thereof,
wherein R.sup.2 is cyclo(lower)alkyl, aryl or ar(lower)alkyl, each of which may be substituted with halogen,
R.sup.3 is lower alkyl, aryl, ar(lower)alkoxy or heterocyclic group, each of which may be substituted with halogen,
A is ##STR18## or lower alkylene and Y is ##STR19##

### Claim 5 (depends on 1)

The compound as claimed in claim 1 wherein R.sup.2 is cyclo(lower)alkyl, or phenyl, each of which may be substituted with halogen.

### Claim 6 (depends on 3)

The process as claimed in claim 3 wherein R.sup.2 is cyclo(lower)alkyl, or phenyl, each of which may be substituted with halogen and R.sup.3 is lower alkyl, phenyl, naphthyl, tolyl, xylyl, mesityl, cumenyl or thienyl.

### Claim 7 (depends on 4)

The process as claimed in claim 4 wherein R.sup.2 is cyclo(lower)alkyl, or phenyl, each of which may be substituted with halogen and R.sup.3 is lower alkyl, phenyl, naphthyl, tolyl, xylyl, mesityl, cumenyl or thienyl.