GB1075156A - Substituted piperazines - Google Patents

Substituted piperazines

Info

Publication number
GB1075156A
GB1075156A GB4699363A GB4699363A GB1075156A GB 1075156 A GB1075156 A GB 1075156A GB 4699363 A GB4699363 A GB 4699363A GB 4699363 A GB4699363 A GB 4699363A GB 1075156 A GB1075156 A GB 1075156A
Authority
GB
United Kingdom
Prior art keywords
hydrogen
lower alkyl
phenyl
hydroxyalkyl
formula
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
GB4699363A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Istituto Luso Farmaco dItalia SpA
Original Assignee
Istituto Luso Farmaco dItalia SpA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Istituto Luso Farmaco dItalia SpA filed Critical Istituto Luso Farmaco dItalia SpA
Publication of GB1075156A publication Critical patent/GB1075156A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical

Abstract

A new method for preparing compounds of formula <FORM:1075156/C2/1> or salts thereof with mineral or carboxylic acids, wherein R is hydrogen, lower (i.e. 1-4C) alkyl or a mononuclear aralkyl radical, R1 is hydrogen, lower alkyl or a mononuclear aryl radical, R11 and R111 are each hydrogen, halogen, hydroxy, lower alkyl, lower alkyloxy or benzyloxy, or jointly represent a methylenedioxy group, n is 1, 2 or 3, A is hydrogen, lower alkyl, free or esterified lower hydroxyalkyl or substituted or unsubstituted mononuclear aryl or aralkyl radical, comprises subjecting to an indole ring closure by treatment with a mineral acid a phenyl hydrazone of formula <FORM:1075156/C2/2> wherein m is n + 1; also methods as exemplified, including reaction of products wherein A is hydroxyalkyl with an acid chloride or phenyl isocyanate. Subsequent introduction of groups R and modification of A generally are mentioned. Substituted piperazine starting materials prepared are: 1 - (33 - acetylpropyl)- and (31 - p - fluorobenzoylpropyl) - 4 - phenyl - piperazine. Reference has been directed by the Comptroller to Specification 944,443.
GB4699363A 1963-08-27 1963-11-28 Substituted piperazines Expired GB1075156A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT1772863 1963-08-27

Publications (1)

Publication Number Publication Date
GB1075156A true GB1075156A (en) 1967-07-12

Family

ID=11150904

Family Applications (1)

Application Number Title Priority Date Filing Date
GB4699363A Expired GB1075156A (en) 1963-08-27 1963-11-28 Substituted piperazines

Country Status (1)

Country Link
GB (1) GB1075156A (en)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0038298A1 (en) * 1980-04-10 1981-10-21 Sandoz Ag Isoxazolyl indolamines
US4302589A (en) * 1980-05-08 1981-11-24 American Cyanamid Company Cis-mono and disubstituted-2-methyl-3-[(piperazinyl) and (piperidino)ethyl]indolines, intermediates for their preparation and methods of preparation
EP0083565A1 (en) * 1980-04-10 1983-07-13 Sandoz Ag Isoxazolyl indolamines
US4734416A (en) * 1978-03-30 1988-03-29 Otsuka Pharmaceutical Co., Ltd. Pharmaceutically useful carbostyril derivatives
US5002948A (en) * 1988-12-28 1991-03-26 H. Lundbeck A/S 3-[4-[4-substituted-1-piperazinyl]-1-butyl]-1H-2,3-dihydroindoles
EP0496222A1 (en) 1991-01-22 1992-07-29 MERCK PATENT GmbH Indole derivatives
EP0529462A1 (en) * 1991-08-22 1993-03-03 MERCK PATENT GmbH Benzodioxan derivatives
EP0648767A1 (en) * 1993-09-30 1995-04-19 MERCK PATENT GmbH Piperdine and piperazine derivatives which affect the C.N.S.
WO1997016446A1 (en) * 1995-11-02 1997-05-09 Merck Sharp & Dohme Limited Bicyclic heteroaryl-alkylene-(homo)piperazinones and thione analogues thereof, their preparation and their use as selective agonists of 5-ht1-like receptors
US6310068B1 (en) 1995-04-05 2001-10-30 Merck Patent Gesellschaft Mit Beschrankter Haftung Benzonitriles and benzofluorides
WO2002066473A1 (en) * 2001-02-21 2002-08-29 Solvay Pharmaceuticals B.V. 8’4-’3-(5-fluoro-1h-indol-3yl) propyl!-1-piperazynyl!-2-methyl-2h-1,4-benzoxazin -3 (4h)- one methanesulfonate with high affinity for the dopamine d 2 receptor and the serotonin reuptake site
US7067513B1 (en) 1999-08-23 2006-06-27 Solvay Pharmaceuticals B.V. Phenylpiperazines

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4734416A (en) * 1978-03-30 1988-03-29 Otsuka Pharmaceutical Co., Ltd. Pharmaceutically useful carbostyril derivatives
US4824840A (en) * 1978-03-30 1989-04-25 Otsuka Pharmaceutical Co., Ltd. Carbostyril derivatives and pharmaceutical preparations containing same
EP0083566A1 (en) * 1980-04-10 1983-07-13 Sandoz Ag Isoxazolyl indoles
EP0083565A1 (en) * 1980-04-10 1983-07-13 Sandoz Ag Isoxazolyl indolamines
EP0038298A1 (en) * 1980-04-10 1981-10-21 Sandoz Ag Isoxazolyl indolamines
US4302589A (en) * 1980-05-08 1981-11-24 American Cyanamid Company Cis-mono and disubstituted-2-methyl-3-[(piperazinyl) and (piperidino)ethyl]indolines, intermediates for their preparation and methods of preparation
US5002948A (en) * 1988-12-28 1991-03-26 H. Lundbeck A/S 3-[4-[4-substituted-1-piperazinyl]-1-butyl]-1H-2,3-dihydroindoles
US5418237A (en) * 1991-01-22 1995-05-23 Merck Patent Gesellschaft Mit Beschrankter Haftung Indole derivatives
EP0496222A1 (en) 1991-01-22 1992-07-29 MERCK PATENT GmbH Indole derivatives
AU655623B2 (en) * 1991-01-22 1995-01-05 Merck Patent Gesellschaft Mit Beschrankter Haftung Indole piperazine derivatives and pharmaceutical preparations containing such derivatives
EP0529462A1 (en) * 1991-08-22 1993-03-03 MERCK PATENT GmbH Benzodioxan derivatives
EP0648767A1 (en) * 1993-09-30 1995-04-19 MERCK PATENT GmbH Piperdine and piperazine derivatives which affect the C.N.S.
US6310068B1 (en) 1995-04-05 2001-10-30 Merck Patent Gesellschaft Mit Beschrankter Haftung Benzonitriles and benzofluorides
WO1997016446A1 (en) * 1995-11-02 1997-05-09 Merck Sharp & Dohme Limited Bicyclic heteroaryl-alkylene-(homo)piperazinones and thione analogues thereof, their preparation and their use as selective agonists of 5-ht1-like receptors
US5998415A (en) * 1995-11-02 1999-12-07 Merck Sharp & Dohme Ltd. Bicyclic heteroaryl-alkylene-(homo)piperazinones and thione analogues thereof, their preparation, and their use of as selective agonists of 5-HT1 -like receptors
US7067513B1 (en) 1999-08-23 2006-06-27 Solvay Pharmaceuticals B.V. Phenylpiperazines
WO2002066473A1 (en) * 2001-02-21 2002-08-29 Solvay Pharmaceuticals B.V. 8’4-’3-(5-fluoro-1h-indol-3yl) propyl!-1-piperazynyl!-2-methyl-2h-1,4-benzoxazin -3 (4h)- one methanesulfonate with high affinity for the dopamine d 2 receptor and the serotonin reuptake site
US6958396B2 (en) 2001-02-21 2005-10-25 Solvay Pharmaceuticals B.V. 8-{4-[3-(5-fluoro-1H-indol-3-YL)-Propyl]-Piperazin-1-YL}-2-methyl-4H-Benzo[1,4]oxazin-3-one mesylate with high affinity for the dopamine D2 receptor and the serotonin reuptake site
US8106044B2 (en) 2001-02-21 2012-01-31 Solvay Pharmaceuticals B.V. 8-{4-[3-(5-fluoro-1H-indol-3-yl)-propyl]-piperazin-1-yl}-2-methyl-4H-benzo[1,4]oxazin-3-one mesylate with high affinity for the dopamine D2 receptor and the serotonin reuptake site

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