AR061811A1 - Procedimiento para la preparacion de asenapina y productos intermedios usados en dicho procedimiento - Google Patents

Procedimiento para la preparacion de asenapina y productos intermedios usados en dicho procedimiento

Info

Publication number
AR061811A1
AR061811A1 ARP070102980A ARP070102980A AR061811A1 AR 061811 A1 AR061811 A1 AR 061811A1 AR P070102980 A ARP070102980 A AR P070102980A AR P070102980 A ARP070102980 A AR P070102980A AR 061811 A1 AR061811 A1 AR 061811A1
Authority
AR
Argentina
Prior art keywords
formula
procedure
asenapine
preparation
intermediate products
Prior art date
Application number
ARP070102980A
Other languages
English (en)
Inventor
Timothy Lee Stuk
Der Linden Jacobus Johannes Maria Van
Gerardus Johannes Kemperman
Original Assignee
Organon Nv
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 Organon Nv filed Critical Organon Nv
Publication of AR061811A1 publication Critical patent/AR061811A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C39/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
    • C07C39/24—Halogenated derivatives
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/017—Esters of hydroxy compounds having the esterified hydroxy group bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te

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)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Se refiere a un procedimiento para la preparacion de asenapina, es decir, trans-5-cloro-2-metil-2,3,3a,12b-tetrahidro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pirrol, así como también a productos intermedios para usar en dicho procedimiento. Reivindicacion 1: Un procedimiento para preparar asenapina de Formula (1) o una sal farmacéuticamente aceptable de la misma, caracterizado porque se hace reaccionar un derivado de E-estilbeno de Formula (2) con iluro de azometina para proveer un deirvado de trans- pirrolidina de Formula (3) del cual se retira el grupo protector, si está presente, y que es tratado subsiguientemente bajo condiciones que producen una reaccion de cierre del anillo intramolecular para dar el compuesto de Formula 1, y convertir opcionalmente el compuesto de Formula 1 en una sal farmacéuticamente aceptable del mismo, en donde: R1 es F, Br o I; R2 es R3 son diferentes y cada uno es seleccionado entre H y Cl; y R4 es H o un grupo protector hidroxilo.
ARP070102980A 2006-07-05 2007-07-04 Procedimiento para la preparacion de asenapina y productos intermedios usados en dicho procedimiento AR061811A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP06116660 2006-07-05

Publications (1)

Publication Number Publication Date
AR061811A1 true AR061811A1 (es) 2008-09-24

Family

ID=37685865

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070102980A AR061811A1 (es) 2006-07-05 2007-07-04 Procedimiento para la preparacion de asenapina y productos intermedios usados en dicho procedimiento

Country Status (18)

Country Link
EP (1) EP2044076B1 (es)
JP (1) JP2010503611A (es)
CN (1) CN101484456B (es)
AR (1) AR061811A1 (es)
AT (1) ATE445620T1 (es)
CA (1) CA2655670A1 (es)
CY (1) CY1109707T1 (es)
DE (1) DE602007002826D1 (es)
DK (1) DK2044076T3 (es)
ES (1) ES2333488T3 (es)
HK (1) HK1127044A1 (es)
MX (1) MX2008016490A (es)
PL (1) PL2044076T3 (es)
PT (1) PT2044076E (es)
SI (1) SI2044076T1 (es)
TW (1) TW200817414A (es)
WO (1) WO2008003460A1 (es)
ZA (1) ZA200810859B (es)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7875729B2 (en) * 2007-01-05 2011-01-25 Synthon Bv Process for making asenapine
JP2011508751A (ja) * 2008-01-04 2011-03-17 ナームローゼ・フエンノートチヤツプ・オルガノン アセナピンの調製方法および前記方法において使用される中間生成物
JP5801295B2 (ja) * 2009-06-24 2015-10-28 メルク・シャープ・エンド・ドーム・ベー・フェー アセナピンを含有する注射可能な配合物およびそれを用いた処置方法
WO2012123325A1 (en) 2011-03-11 2012-09-20 Medichem S.A. NEW CRYSTAL FORMS OF THE SALT OF TRANS-5-CHLORO-2-METHYL-2,3,3A,12b-TETRAHYDRO-1H-DIBENZO[2,3:6,7]OXEPINO[4,5-c]PYRROLE WITH MALEIC ACID
CN102229613B (zh) * 2011-04-27 2013-08-07 上海华升生物科技有限公司 阿森纳平的合成工艺
ITMI20110734A1 (it) * 2011-05-02 2012-11-03 Olon Spa Sali cristallini di asenapina
EP2524919A1 (en) * 2011-05-17 2012-11-21 Sandoz AG Novel crystalline salts of Asenapine with organic Di-acids and Tri-acids
EP2524921A1 (en) * 2011-05-17 2012-11-21 Sandoz AG Novel Crystalline Salts of Asenapine
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
WO2013041604A1 (en) 2011-09-21 2013-03-28 Sandoz Ag Crystal form of asenapine maleate
EP2572703A1 (en) 2011-09-21 2013-03-27 Hexal AG Compressed oral dosage form for asenapine maleate
GB201121124D0 (en) * 2011-12-08 2012-01-18 Dow Corning Hydrolysable silanes
GB201121128D0 (en) * 2011-12-08 2012-01-18 Dow Corning Treatment of filler with silane
CN103183680A (zh) * 2011-12-27 2013-07-03 上海华拓医药科技发展股份有限公司 阿森那平的制备方法
WO2013190481A1 (en) * 2012-06-21 2013-12-27 Alembic Pharmaceuticals Limited Process for preparing asenapine and salts of intermediates thereof
CN103772402A (zh) * 2014-01-07 2014-05-07 万特制药(海南)有限公司 一种新的阿塞那平马来酸盐粗品精制方法
CN104974167B (zh) * 2014-04-02 2019-01-04 洋浦慧谷医药有限公司 阿塞那平的制备方法以及用于制备阿塞那平的中间体
US10056563B2 (en) * 2016-04-08 2018-08-21 Samsung Electronics Co., Ltd. Synthetic method of fused heteroaromatic compound and fused heteroaromatic compound, and intermediate thereof
KR102677490B1 (ko) 2016-11-08 2024-06-20 삼성전자주식회사 축합 헤테로방향족 화합물의 합성 방법, 축합 헤테로방향족 화합물 및 그 중간체 및 합성 방법
KR102614709B1 (ko) 2016-12-20 2023-12-18 에르테에스 로만 테라피-시스테메 아게 아세나핀 및 폴리실록산 또는 폴리이소부틸렌을 함유하는 경피흡수 치료 시스템
CN110087640A (zh) 2016-12-20 2019-08-02 罗曼治疗系统股份公司 包含阿塞那平的透皮治疗系统
US11033512B2 (en) 2017-06-26 2021-06-15 Lts Lohmann Therapie-Systeme Ag Transdermal therapeutic system containing asenapine and silicone acrylic hybrid polymer
KR20210022656A (ko) 2018-06-20 2021-03-03 에르테에스 로만 테라피-시스테메 아게 아세나핀을 함유하는 경피 치료 시스템
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
CN110606852B (zh) 2019-08-13 2021-02-05 浙江奥翔药业股份有限公司 制备阿塞那平的方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7605526A (nl) * 1976-05-24 1977-11-28 Akzo Nv Nieuwe tetracyclische derivaten.
RS51341B (en) * 2005-04-07 2011-02-28 N.V. Organon INTERMEDIATE COMPOUNDS FOR THE TRANS-5-CHLOR-2-METHYL-2,3A, 12B-TETRAHYDRO-1H-DIBENZE [2,3; 6,7] OXEPINO [4,5-C] Pyrrole

Also Published As

Publication number Publication date
ZA200810859B (en) 2009-09-30
DK2044076T3 (da) 2010-02-01
CN101484456A (zh) 2009-07-15
DE602007002826D1 (de) 2009-11-26
EP2044076B1 (en) 2009-10-14
CY1109707T1 (el) 2014-04-09
HK1127044A1 (en) 2009-09-18
CA2655670A1 (en) 2008-01-10
ATE445620T1 (de) 2009-10-15
EP2044076A1 (en) 2009-04-08
ES2333488T3 (es) 2010-02-22
SI2044076T1 (sl) 2010-01-29
WO2008003460A1 (en) 2008-01-10
MX2008016490A (es) 2009-01-22
PL2044076T3 (pl) 2010-03-31
JP2010503611A (ja) 2010-02-04
TW200817414A (en) 2008-04-16
PT2044076E (pt) 2010-01-20
CN101484456B (zh) 2011-09-07

Similar Documents

Publication Publication Date Title
AR061811A1 (es) Procedimiento para la preparacion de asenapina y productos intermedios usados en dicho procedimiento
DOP2009000232A (es) Metanoisoindoles y dionas de éstos como agentes anti-psicóticos.
UY35641A (es) PROCEDIMIENTO DE SÍNTESIS PARA PREPARAR ANÁLOGOS MACROCÍCLICOS C1-CETO DE HALICONDRINA B, E INTERMEDIARIOS ÚTILES INCLUYENDO INTERMEDIARIOS CONTENIENDO GRUPOS ?SO2-(p-TOLILO)
PE20161251A1 (es) Compuestos heteroarilo o arilo biciclicos fusionados y su uso como inhibidores de irak4
MX358149B (es) Derivado de pirazoloquinolina.
PE20061033A1 (es) Sintesis asimetrica de derivados de dihidrobenzofurano
PE20142335A1 (es) Sintesis de compuestos heterociclicos
AR079226A1 (es) Espiroindolinona- pirrolidinas, procesos de preparacion y uso de los mismos para el tratamiento y profilaxis del cancer
GT200500183A (es) Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
ECSP15012804A (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
GT200300296A (es) Derivados de pirimidina para el tratamiento del crecimiento celular anormal
AR047523A1 (es) Procedimiento para la preparacion de 1-(2s,3s)-2-bencidril-n-(5-terc-butil-2-metoxibencil)quinuclidin-3-amina
IL192253A0 (en) Substituted cyclohexylmethyl derivatives
CO6410299A2 (es) Derivados de triazolo [4,3-b] pridazina y sus usos para el cáncer de próstata
CU24177B1 (es) Derivados de heteroarilo como moduladores de nachr alfa 7
AR061580A1 (es) Profarmacos de 5- amino-3-(3'- desoxi- beta-d - ribofuronosil)-tiazolo [4 ,5- d] pirimidin-2,7- diona
AR059905A1 (es) Pirrolidina-3-ilaminas n-substituidas como antagonistas del receptor histamina-3, composicion farmaceutica y proceso para preparar el compuesto
AR073248A1 (es) Proceso para la preparacion de (1s, 2r)-3- ((4-aminofenil) sulfonil) ( isobutil) amino)-1- bencil-2- hidroxipropilcarbamato de (3r, 3as,6ar)- hexahidrofuro-(2,3-b) furan-3- ilo (darunavir) y compuestos intermediarios utiles en dicho proceso.
GT200500317A (es) Proceso para preparar compuestos de quinolina y productos obtenidos de los mismos
PE20091359A1 (es) Proceso de preparacion de compuestos organicos intermediarios de inhibidores de renina
PE20221732A1 (es) Derivados de 3-((hetero)aril)-8-amino-2-oxo-1,3-diaza-espiro-[4.5]-decano
EA201300647A1 (ru) Оптимизированный синтез чистых неполиморфных кристаллических жёлчных кислот с заданным размером частиц
CO6460764A2 (es) [1,2,4] triazolo [4,3-b] piridazinas como ligandos del receptor de andrógenos
DOP2012000078A (es) Derivados de espirolactama y usos de los mismos
PE20090101A1 (es) Compuestos derivados de azabicicloalcano, preparacion y composicion farmaceutica

Legal Events

Date Code Title Description
FB Suspension of granting procedure