HRP20100031T1 - MEĐUPRODUKTI U DOBIVANJU trans-5-KLOR-2-METIL-2,3,3a,12b-TETRAHIDRO-1H-DIBENZ[2,3:6,7]OKSEPINO[4,5-C]PIROLA - Google Patents
MEĐUPRODUKTI U DOBIVANJU trans-5-KLOR-2-METIL-2,3,3a,12b-TETRAHIDRO-1H-DIBENZ[2,3:6,7]OKSEPINO[4,5-C]PIROLA Download PDFInfo
- Publication number
- HRP20100031T1 HRP20100031T1 HR20100031T HRP20100031T HRP20100031T1 HR P20100031 T1 HRP20100031 T1 HR P20100031T1 HR 20100031 T HR20100031 T HR 20100031T HR P20100031 T HRP20100031 T HR P20100031T HR P20100031 T1 HRP20100031 T1 HR P20100031T1
- Authority
- HR
- Croatia
- Prior art keywords
- formula
- trans
- amino acid
- acid derivative
- image
- Prior art date
Links
- VSWBSWWIRNCQIJ-HUUCEWRRSA-N (S,S)-asenapine Chemical compound O1C2=CC=CC=C2[C@H]2CN(C)C[C@@H]2C2=CC(Cl)=CC=C21 VSWBSWWIRNCQIJ-HUUCEWRRSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 9
- 239000000203 mixture Substances 0.000 claims abstract 4
- 238000000034 method Methods 0.000 claims 14
- VSWBSWWIRNCQIJ-GJZGRUSLSA-N (R,R)-asenapine Chemical compound O1C2=CC=CC=C2[C@@H]2CN(C)C[C@H]2C2=CC(Cl)=CC=C21 VSWBSWWIRNCQIJ-GJZGRUSLSA-N 0.000 claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 6
- 229960005245 asenapine Drugs 0.000 claims 6
- 150000003951 lactams Chemical class 0.000 claims 4
- 238000007363 ring formation reaction Methods 0.000 claims 4
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical group [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims 3
- 150000001732 carboxylic acid derivatives Chemical group 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- CDCWWLYYNIFTQA-CZUORRHYSA-N (5s,6s)-3-chloro-5-(methylaminomethyl)-5,6-dihydrobenzo[b][1]benzoxepine-6-carboxylic acid Chemical class CNC[C@H]1[C@H](C(O)=O)C2=CC=CC=C2OC2=CC=C(Cl)C=C12 CDCWWLYYNIFTQA-CZUORRHYSA-N 0.000 claims 1
- FDEBVKYOGYXKFY-CZUORRHYSA-N (5s,6s)-3-chloro-6-(methylaminomethyl)-5,6-dihydrobenzo[b][1]benzoxepine-5-carboxylic acid Chemical group CNC[C@H]1[C@H](C(O)=O)C2=CC(Cl)=CC=C2OC2=CC=CC=C12 FDEBVKYOGYXKFY-CZUORRHYSA-N 0.000 claims 1
- 239000002841 Lewis acid Substances 0.000 claims 1
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- UORVGPXVDQYIDP-BJUDXGSMSA-N borane Chemical group [10BH3] UORVGPXVDQYIDP-BJUDXGSMSA-N 0.000 claims 1
- 229910000085 borane Inorganic materials 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 239000003638 chemical reducing agent Substances 0.000 claims 1
- 150000007517 lewis acids Chemical class 0.000 claims 1
- 239000012280 lithium aluminium hydride Substances 0.000 claims 1
- -1 lithium aluminum hydride Chemical compound 0.000 claims 1
- 239000001632 sodium acetate Substances 0.000 claims 1
- 235000017281 sodium acetate Nutrition 0.000 claims 1
- UORVGPXVDQYIDP-UHFFFAOYSA-N trihydridoboron Substances B UORVGPXVDQYIDP-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
- C07D313/02—Seven-membered rings
- C07D313/06—Seven-membered rings condensed with carbocyclic rings or ring systems
- C07D313/10—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
- C07D313/14—[b,f]-condensed
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pyrane Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05102742 | 2005-04-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20100031T1 true HRP20100031T1 (hr) | 2010-02-28 |
Family
ID=35511130
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20100031T HRP20100031T1 (hr) | 2005-04-07 | 2010-01-18 | MEĐUPRODUKTI U DOBIVANJU trans-5-KLOR-2-METIL-2,3,3a,12b-TETRAHIDRO-1H-DIBENZ[2,3:6,7]OKSEPINO[4,5-C]PIROLA |
Country Status (28)
| Country | Link |
|---|---|
| EP (2) | EP2154134B1 (zh) |
| JP (1) | JP2008534657A (zh) |
| KR (1) | KR20070116973A (zh) |
| CN (2) | CN101175741B (zh) |
| AR (1) | AR063188A1 (zh) |
| AT (1) | ATE447564T1 (zh) |
| AU (1) | AU2006231281B2 (zh) |
| BR (1) | BRPI0610677A2 (zh) |
| CA (1) | CA2603181A1 (zh) |
| CY (1) | CY1109722T1 (zh) |
| DE (1) | DE602006010132D1 (zh) |
| DK (1) | DK1710241T3 (zh) |
| ES (1) | ES2333980T3 (zh) |
| HK (1) | HK1094800A1 (zh) |
| HR (1) | HRP20100031T1 (zh) |
| IL (1) | IL186354A0 (zh) |
| MX (1) | MX2007012446A (zh) |
| NO (1) | NO20075152L (zh) |
| NZ (1) | NZ562125A (zh) |
| PL (1) | PL1710241T3 (zh) |
| PT (1) | PT1710241E (zh) |
| RS (1) | RS51341B (zh) |
| RU (1) | RU2397164C2 (zh) |
| SI (1) | SI1710241T1 (zh) |
| TW (1) | TW200716589A (zh) |
| UA (2) | UA93043C2 (zh) |
| WO (1) | WO2006106136A1 (zh) |
| ZA (2) | ZA200708493B (zh) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5027477B2 (ja) * | 2005-10-21 | 2012-09-19 | 住友化学株式会社 | ジベンゾオキセピノピロール化合物およびその中間体の製造方法ならびに新規中間体 |
| TW200817414A (en) * | 2006-07-05 | 2008-04-16 | Organon Nv | Process for the preparation of asenapine and intermediate products used in said process |
| CN101563312A (zh) * | 2006-12-22 | 2009-10-21 | 住友化学株式会社 | 阿塞那平合成中间体的制备方法 |
| US7875729B2 (en) | 2007-01-05 | 2011-01-25 | Synthon Bv | Process for making asenapine |
| JP5245428B2 (ja) | 2007-07-06 | 2013-07-24 | 住友化学株式会社 | トランス−ジベンゾオキセノピロール化合物の製造方法およびその中間体 |
| US7964739B2 (en) | 2008-01-04 | 2011-06-21 | N.V. Organon | Process for the preparation of asenapine and intermediate products used in said process |
| EP2453870A2 (en) | 2009-06-24 | 2012-05-23 | MSD Oss B.V. | Injectable formulations containing asenapine and method of treatment using same |
| CN101851242B (zh) * | 2010-05-25 | 2013-07-24 | 上海皓元生物医药科技有限公司 | 阿塞那平中间体的制备方法 |
| CA2805542C (en) | 2010-07-29 | 2017-12-12 | Laboratorios Lesvi, S.L. | Novel process for the preparation of asenapine |
| WO2012038975A2 (en) * | 2010-09-22 | 2012-03-29 | Msn Laboratories Limited | Process for the preparation of (3ars,12brs)-5-chloro-2-methyl-2,3,3a12b-tetrahydro-1hdibenzo[2,3:6,7] oxepino [4,5-c]pyrrole maleate and it's pharmaceutical composition thereof |
| ES2575544T3 (es) | 2010-12-24 | 2016-06-29 | Medichem, S.A. | Procedimientos para la preparación de 5-cloro-2-metil-2,3,3a,12b-tetrahidro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pirrol |
| ITMI20110734A1 (it) * | 2011-05-02 | 2012-11-03 | Olon Spa | Sali cristallini di asenapina |
| WO2013024492A2 (en) * | 2011-07-01 | 2013-02-21 | Megafine Pharma (P) Ltd. | A process for the preparation of asenapine and novel salts thereof |
| CN102952144A (zh) * | 2011-08-29 | 2013-03-06 | 上海华拓医药科技发展股份有限公司 | 阿森纳平马来酸盐的晶型、制备方法及其药物组合物 |
| US20140336391A1 (en) * | 2011-11-28 | 2014-11-13 | Ranbaxy Laboratories Limited | Process for the preparation of asenapine intermediate |
| CN102746209A (zh) * | 2012-06-20 | 2012-10-24 | 盛世泰科生物医药技术(苏州)有限公司 | 一种3-（2-（4-氯苯氧基）苯基）-1-甲基-2,4-二酮的合成方法 |
| CN103965206A (zh) * | 2013-01-29 | 2014-08-06 | 北京京卫燕康药物研究所有限公司 | 一种阿色纳品马来酸盐的新晶型及制备方法 |
| CN103113379A (zh) * | 2013-03-12 | 2013-05-22 | 盛世泰科生物医药技术(苏州)有限公司 | 阿塞那平马来酸盐的合成工艺 |
| CN103254202A (zh) * | 2013-05-19 | 2013-08-21 | 甘肃皓天化学科技有限公司 | 阿塞纳平的制备方法 |
| CN103342707B (zh) * | 2013-06-28 | 2015-09-02 | 甘肃皓天化学科技有限公司 | 用于制备阿塞纳平中间体的制备方法 |
| CN104447771A (zh) * | 2013-09-12 | 2015-03-25 | 天津市汉康医药生物技术有限公司 | 一种稳定的马来酸阿塞那平化合物 |
| CN103864802B (zh) * | 2014-03-31 | 2016-08-17 | 四川科伦药业股份有限公司 | 马来酸阿塞那平的制备方法 |
| CN105693735A (zh) * | 2016-01-15 | 2016-06-22 | 万特制药(海南)有限公司 | 马来酸阿塞那平一种制备方法 |
| MX2019007389A (es) | 2016-12-20 | 2019-08-16 | Lts Lohmann Therapie Systeme Ag | Sistema terapeutico transdermico que contiene asenapina y polisiloxano o poliisobutileno. |
| US20180193283A1 (en) | 2016-12-20 | 2018-07-12 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system containing asenapine |
| JP2020525545A (ja) | 2017-06-26 | 2020-08-27 | エルテーエス ローマン テラピー−ジステーメ アーゲー | アセナピンおよびシリコーンアクリルハイブリッドポリマーを含有する経皮治療システム |
| CN109200025A (zh) * | 2017-06-29 | 2019-01-15 | 哈尔滨莱博通药业有限公司 | 一种阿森纳平马来酸盐舌下片 |
| CA3101420A1 (en) | 2018-06-20 | 2019-12-26 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system containing asenapine |
| CN110183457A (zh) * | 2019-06-27 | 2019-08-30 | 浙江天顺药业有限公司 | 一种阿塞那平及其制备方法 |
| CN112194665A (zh) * | 2020-10-20 | 2021-01-08 | 连云港杰瑞药业有限公司 | 一种合成阿塞那平中间体的方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL7605526A (nl) * | 1976-05-24 | 1977-11-28 | Akzo Nv | Nieuwe tetracyclische derivaten. |
| RU2139051C1 (ru) | 1994-03-02 | 1999-10-10 | Акцо Нобель Н.В. | Сублингвальная или трансбуккальная фармацевтическая композиция |
| WO1999032108A1 (en) | 1997-12-19 | 1999-07-01 | Akzo Nobel N.V. | Org-5222 in the treatment of depression |
-
2006
- 2006-04-06 CN CN2006800167535A patent/CN101175741B/zh not_active Expired - Fee Related
- 2006-04-06 PL PL06112333T patent/PL1710241T3/pl unknown
- 2006-04-06 PT PT06112333T patent/PT1710241E/pt unknown
- 2006-04-06 AU AU2006231281A patent/AU2006231281B2/en not_active Ceased
- 2006-04-06 RU RU2007141161/04A patent/RU2397164C2/ru not_active IP Right Cessation
- 2006-04-06 MX MX2007012446A patent/MX2007012446A/es active IP Right Grant
- 2006-04-06 NZ NZ562125A patent/NZ562125A/en not_active IP Right Cessation
- 2006-04-06 CN CN2006100916992A patent/CN1861604B/zh active Active
- 2006-04-06 DE DE602006010132T patent/DE602006010132D1/de active Active
- 2006-04-06 ES ES06112333T patent/ES2333980T3/es active Active
- 2006-04-06 KR KR1020077025399A patent/KR20070116973A/ko not_active Application Discontinuation
- 2006-04-06 AT AT06112333T patent/ATE447564T1/de not_active IP Right Cessation
- 2006-04-06 TW TW095112190A patent/TW200716589A/zh unknown
- 2006-04-06 SI SI200630526T patent/SI1710241T1/sl unknown
- 2006-04-06 UA UAA200711019A patent/UA93043C2/ru unknown
- 2006-04-06 AR ARP060101357A patent/AR063188A1/es unknown
- 2006-04-06 EP EP09174540A patent/EP2154134B1/en active Active
- 2006-04-06 UA UAA200711020A patent/UA93044C2/ru unknown
- 2006-04-06 BR BRPI0610677-3A patent/BRPI0610677A2/pt not_active IP Right Cessation
- 2006-04-06 CA CA002603181A patent/CA2603181A1/en not_active Abandoned
- 2006-04-06 EP EP06112333A patent/EP1710241B1/en active Active
- 2006-04-06 JP JP2008504777A patent/JP2008534657A/ja not_active Withdrawn
- 2006-04-06 DK DK06112333.7T patent/DK1710241T3/da active
- 2006-04-06 RS RSP-2010/0014A patent/RS51341B/en unknown
- 2006-04-06 WO PCT/EP2006/061409 patent/WO2006106136A1/en not_active Application Discontinuation
-
2007
- 2007-02-26 HK HK07102138.2A patent/HK1094800A1/xx not_active IP Right Cessation
- 2007-10-04 ZA ZA200708493A patent/ZA200708493B/xx unknown
- 2007-10-04 ZA ZA200708490A patent/ZA200708490B/xx unknown
- 2007-10-07 IL IL186354A patent/IL186354A0/en not_active IP Right Cessation
- 2007-10-10 NO NO20075152A patent/NO20075152L/no not_active Application Discontinuation
-
2010
- 2010-01-08 CY CY20101100023T patent/CY1109722T1/el unknown
- 2010-01-18 HR HR20100031T patent/HRP20100031T1/hr unknown
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