YU64403A - Postupak za pripremanje mezilata piperazin derivata - Google Patents
Postupak za pripremanje mezilata piperazin derivataInfo
- Publication number
- YU64403A YU64403A YU64403A YUP64403A YU64403A YU 64403 A YU64403 A YU 64403A YU 64403 A YU64403 A YU 64403A YU P64403 A YUP64403 A YU P64403A YU 64403 A YU64403 A YU 64403A
- Authority
- YU
- Yugoslavia
- Prior art keywords
- mesylates
- preparation
- piperazine derivatives
- methyl
- benzyl
- Prior art date
Links
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 title abstract 5
- 238000000034 method Methods 0.000 title abstract 3
- 150000004885 piperazines Chemical class 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 229940066771 systemic antihistamines piperazine derivative Drugs 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- -1 m-phenyl benzyl Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Pronalazak se odnosi na mezilate grupe piperazin derivata i na postupak za pripremanje ovih mezilata na ekonomičan način u visokom prinosu i visoke čistoće. Prema postupku pronalaska sinteza piperazin prstena i obrazovanja mezilata se kombinuju u jednom reakcionom koraku. Pronalazak se odnosi na mezilate jedinjenja sa formulom (1) gde je X biciklična heterociklična fenil grupa a Y je metil, etil (opciono supstituisan sa fluorom), cikloalkil (3-7C).[The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step. The invention relates to the mesylate of compounds of the formula (I) wherein X is a bicyclic heterocyclic phenyl group and Y is methyl, ethyl (optionally substituted with fluorine), cycloalkyl (3-7C) methyl, benzyl or m-phenyl benzyl.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01200534 | 2001-02-16 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| YU64403A true YU64403A (sh) | 2006-05-25 |
| RS51126B RS51126B (sr) | 2010-10-31 |
Family
ID=8179894
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US7030241B2 (sh) |
| EP (1) | EP1362040B1 (sh) |
| JP (1) | JP4328528B2 (sh) |
| KR (2) | KR100859106B1 (sh) |
| CN (1) | CN1176079C (sh) |
| AR (1) | AR034206A1 (sh) |
| AT (1) | ATE284875T1 (sh) |
| AU (1) | AU2002250962B2 (sh) |
| BG (1) | BG66101B1 (sh) |
| BR (1) | BR0205683A (sh) |
| CA (1) | CA2422703C (sh) |
| CZ (1) | CZ301780B6 (sh) |
| DE (1) | DE60202261T2 (sh) |
| DK (1) | DK1362040T3 (sh) |
| DZ (1) | DZ3489A1 (sh) |
| ES (1) | ES2230481T3 (sh) |
| HK (1) | HK1059934A1 (sh) |
| HR (1) | HRP20030610B1 (sh) |
| HU (1) | HUP0400772A3 (sh) |
| IL (1) | IL153509A (sh) |
| IS (1) | IS2417B (sh) |
| ME (1) | MEP37508A (sh) |
| MX (1) | MXPA03002359A (sh) |
| MY (1) | MY130687A (sh) |
| NO (1) | NO324460B1 (sh) |
| NZ (1) | NZ524632A (sh) |
| PL (1) | PL208363B1 (sh) |
| PT (1) | PT1362040E (sh) |
| RS (1) | RS51126B (sh) |
| RU (1) | RU2272036C2 (sh) |
| SI (1) | SI1362040T1 (sh) |
| SK (1) | SK286143B6 (sh) |
| UA (1) | UA75390C2 (sh) |
| WO (1) | WO2002066449A2 (sh) |
| ZA (1) | ZA200301590B (sh) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7435738B2 (en) | 2003-08-18 | 2008-10-14 | Solvay Pharmaceuticals, Inc. | Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate) |
| AR045362A1 (es) * | 2003-08-18 | 2005-10-26 | Solvay Pharm Bv | Forma cristalina estable de mesilato de bifeprunox (monometansulfonato de 7-[4-([1,1- bifenil] -3- ilmetil) -1- piperazinil] - 2-(3h) -benzoxazolona |
| US7405216B2 (en) * | 2004-08-18 | 2008-07-29 | Solvay Pharmaceuticals, B.V. | Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate) |
| US7964604B2 (en) * | 2005-02-18 | 2011-06-21 | Solvay Pharmaceuticals B.V. | Bifeprunox mesylate maintenance dose compositions and methods for using the same |
| US7423040B2 (en) * | 2005-02-18 | 2008-09-09 | Irene Eijgendaal | Stable crystalline form of bifeprunox mesylate, dosage forms thereof and methods for using same |
| US20070275977A1 (en) * | 2006-05-02 | 2007-11-29 | Van Aar Marcel P | N-oxides of pyridylmethyl -piperazine and -piperidine derivatives |
| US7786126B2 (en) * | 2006-06-16 | 2010-08-31 | Solvay Pharmaceuticals B.V. | Combination preparations comprising SLV308 and a dopamine agonist |
| US8106056B2 (en) | 2006-06-16 | 2012-01-31 | Solvay Pharmaceuticals B.V. | Combination preparations comprising bifeprunox and a dopamine agonist |
| US20080132520A1 (en) * | 2006-08-31 | 2008-06-05 | Winsemius Antje A | Compositions, kits and methods for administering a titration schedule comprising bifeprunox compounds |
| BRPI0715445A2 (pt) | 2006-08-31 | 2014-05-13 | Solvay Pharm Bv | Uso de um composto de bifeprunox, e, kit de titulação |
| US20090068290A1 (en) * | 2006-08-31 | 2009-03-12 | Michel Bourin | Bifeprunox doses for treating schizophrenia |
| CN103467554A (zh) | 2008-02-05 | 2013-12-25 | 哈博生物科学公司 | 药学固体形式 |
| WO2011023796A1 (en) | 2009-08-31 | 2011-03-03 | Abbott Healthcare Products B.V. | Bifeprunox for treating addiction |
| UY32935A (es) | 2009-10-12 | 2011-05-31 | Abbott Healthcare Products Bv | Polimorfos de pardoprunox |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3586794T2 (de) * | 1984-12-21 | 1993-05-27 | Duphar Int Res | Arzneimittel mit psychotroper wirkung. |
| EP0185429A1 (en) * | 1984-12-21 | 1986-06-25 | Duphar International Research B.V | New bicyclic heteroaryl piperazines |
| JPH0344383A (ja) * | 1989-07-12 | 1991-02-26 | Ihara Chem Ind Co Ltd | ５―トリフルオロメチル―２―ハロメチルベンゾチアゾール類の製造法 |
| JP3044383B2 (ja) * | 1990-05-22 | 2000-05-22 | コニカ株式会社 | 含窒素６員環化合物の製造方法 |
| TR199801942T2 (xx) * | 1996-03-29 | 2000-08-21 | Duphar International Research B.V. | Piperazin ve piperidin bile�ikleri. |
| SE9702799D0 (sv) * | 1997-07-25 | 1997-07-25 | Astra Ab | New compounds |
| UA71590C2 (en) * | 1998-11-13 | 2004-12-15 | Duphar Int Res | Piperazine and piperidine derivatives |
| US7435738B2 (en) * | 2003-08-18 | 2008-10-14 | Solvay Pharmaceuticals, Inc. | Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate) |
-
2002
- 2002-02-12 AR ARP020100460A patent/AR034206A1/es active IP Right Grant
- 2002-02-14 RU RU2003105902/04A patent/RU2272036C2/ru not_active IP Right Cessation
- 2002-02-14 IL IL153509A patent/IL153509A/en not_active IP Right Cessation
- 2002-02-14 CA CA2422703A patent/CA2422703C/en not_active Expired - Fee Related
- 2002-02-14 HU HU0400772A patent/HUP0400772A3/hu unknown
- 2002-02-14 CZ CZ20030697A patent/CZ301780B6/cs not_active IP Right Cessation
- 2002-02-14 CN CNB028016858A patent/CN1176079C/zh not_active Expired - Fee Related
- 2002-02-14 UA UA2003098528A patent/UA75390C2/uk unknown
- 2002-02-14 WO PCT/EP2002/001666 patent/WO2002066449A2/en active IP Right Grant
- 2002-02-14 SI SI200230061T patent/SI1362040T1/xx unknown
- 2002-02-14 KR KR1020037000026A patent/KR100859106B1/ko not_active IP Right Cessation
- 2002-02-14 AT AT02719858T patent/ATE284875T1/de active
- 2002-02-14 NZ NZ524632A patent/NZ524632A/en not_active IP Right Cessation
- 2002-02-14 ES ES02719858T patent/ES2230481T3/es not_active Expired - Lifetime
- 2002-02-14 RS YUP-644/03A patent/RS51126B/sr unknown
- 2002-02-14 EP EP02719858A patent/EP1362040B1/en not_active Expired - Lifetime
- 2002-02-14 JP JP2002565965A patent/JP4328528B2/ja not_active Expired - Fee Related
- 2002-02-14 DE DE60202261T patent/DE60202261T2/de not_active Expired - Lifetime
- 2002-02-14 PT PT02719858T patent/PT1362040E/pt unknown
- 2002-02-14 DK DK02719858T patent/DK1362040T3/da active
- 2002-02-14 ME MEP-375/08A patent/MEP37508A/xx unknown
- 2002-02-14 AU AU2002250962A patent/AU2002250962B2/en not_active Ceased
- 2002-02-14 US US10/468,098 patent/US7030241B2/en not_active Expired - Fee Related
- 2002-02-14 PL PL369330A patent/PL208363B1/pl unknown
- 2002-02-14 SK SK309-2003A patent/SK286143B6/sk not_active IP Right Cessation
- 2002-02-14 KR KR1020087015071A patent/KR101000733B1/ko not_active IP Right Cessation
- 2002-02-14 MY MYPI20020505A patent/MY130687A/en unknown
- 2002-02-14 MX MXPA03002359A patent/MXPA03002359A/es active IP Right Grant
- 2002-02-14 DZ DZ023489A patent/DZ3489A1/fr active
- 2002-02-14 BR BR0205683-6A patent/BR0205683A/pt not_active Application Discontinuation
-
2003
- 2003-02-26 ZA ZA200301590A patent/ZA200301590B/en unknown
- 2003-04-15 NO NO20031754A patent/NO324460B1/no not_active IP Right Cessation
- 2003-07-17 IS IS6876A patent/IS2417B/is unknown
- 2003-07-28 HR HR20030610A patent/HRP20030610B1/xx not_active IP Right Cessation
- 2003-08-13 BG BG108090A patent/BG66101B1/bg unknown
-
2004
- 2004-04-22 HK HK04102835A patent/HK1059934A1/xx not_active IP Right Cessation
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