EP0364091A1
Expired / Lapsed
EP
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Antipsychotic 4-(4-(3-benzisothiazolyl)-1-piperazinyl)butyl bridged bicyclic imides
Assignee: Pfizer Inc
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Filing: 1989-08-22
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Granted: —
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Expires: 2009-08-22
Abstract
Abstract Antipsychotic compounds of the formula (I):- or a pharmaceutically-acceptable acid addition salt thereof, wherein each of R¹ and R², which may be the same or different, is hydrogen, methyl or ethyl; X is -CH₂-, -CH₂CH₂- or -CH₂CH₂CH₂-; and Y is CR³R⁴ wherein each of R³ and R⁴, which may be the same or different, is hydrogen or methyl.
Inventors
- 👤 Gene Michael Bright
- 👤 John Adams Lowe Iii
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-08 23:40
CPC Classifications
C; C07; C07D; C07D417/00; C07D417/14; C07D417/02; C07D417/12; A; A61; A61P; A61P25/00; A61P25/18
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
101 words
A process for making a compound of formula wherein each of R¹ and R², which may be the same or different, is hydrogen, methyl or ethyl; X is -CH₂-, -CH₂CH₂ or -CH₂CH₂CH₂-; and Y is CR³R⁴ wherein each of R³ and R⁴, which may be the same or different, is hydrogen or methyl; which comprises reacting N-(3-benzisothiazolyl)piperazine with a compound of formula (II) wherein Z is halo, mesyloxy or tosyloxy and each of R¹, R², X and Y are as previously defined, in a reaction-inert solvent at a temperature of from 50°C. to 200°C. in the presence of an acid acceptor.
Claim 2
Dependent Claim
101 words
A process for making a compound of formula wherein each of R¹ and R², which may be the same or different, is hydrogen, methyl or ethyl; X is -CH₂-, -CH₂CH₂ or -CH₂CH₂CH₂-; and Y is CR³R⁴ wherein each of R³ and R⁴, which may be the same or different, is hydrogen or methyl; which comprises reacting N-(3-benzisothiazolyl)piperazine with a compound of formula (II) wherein Z is halo, mesyloxy or tosyloxy and each of R¹, R², X and Y are as previously defined, in a reaction-inert solvent at a temperature of from 50°C. to 200°C. in the presence of an acid acceptor.
Claim 3
Dependent Claim
30 words
A process according to claim 1 wherein Z is tosyloxy; the solvent is methylisobutylketone and the temperature is 50°C. to 150°C. and the acid acceptor is an alkali metal carbonate.
Claim 4
Dependent Claim
23 words
A process according to claim 1 or 2 wherein each of R¹ and R² is hydrogen; Y is CH₂ and X is -CH₂-.
Claim 5
Dependent Claim
22 words
A process according to claim 1 or 2 wherein R¹ is methyl; R² is hydrogen; Y is CH₂; and X is -CH₂CH₂-.
Claim 6
Dependent Claim
22 words
A process according to claim 1 or 2 wherein R¹ is methyl; R² is hydrogen; Y is C(CH₃)₂ and X is -CH₂CH₂-.
References Cited (Backward Citations)
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