AR075436A1 - Produccion y purificacion de 1-[2-(2,4-dimetilfenilsulfanil)fenil] piperazina - Google Patents

Produccion y purificacion de 1-[2-(2,4-dimetilfenilsulfanil)fenil] piperazina

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Publication number
AR075436A1
AR075436A1 ARP100100441A ARP100100441A AR075436A1 AR 075436 A1 AR075436 A1 AR 075436A1 AR P100100441 A ARP100100441 A AR P100100441A AR P100100441 A ARP100100441 A AR P100100441A AR 075436 A1 AR075436 A1 AR 075436A1
Authority
AR
Argentina
Prior art keywords
piperazine
dimethylphenylsulfanyl
phenyl
hbr
solution
Prior art date
Application number
ARP100100441A
Other languages
English (en)
Original Assignee
Lundbeck & Co As H
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 Lundbeck & Co As H filed Critical Lundbeck & Co As H
Publication of AR075436A1 publication Critical patent/AR075436A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/08Heterocyclic 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 bound oxygen or sulfur atoms
    • C07D295/096Heterocyclic 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 bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/02Heterocyclic 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027Heterocyclic 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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/08Heterocyclic 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 bound oxygen or sulfur atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Reivindicacion 1: Un proceso para la produccion de de 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina o su sal aceptable para uso farmacéutico que comprende el paso de obtener una solucion disolviendo la sal 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr en un solvente que comprende más del 65% (v/v) de isopropanol. Reivindicacion 15: El proceso de acuerdo con la reivindicacion 1 que comprende el paso de a) obtener, una solucion disolviendo 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr en un solvente que comprende más del 65% (v/v) de isopropanol; b) precipitar isopropanol solvato de 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr a partir de dicha solucion obtenida; c) disolver isopropanol solvato de 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr en un solvente que no forma solvatos; y d) precipitar 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr a partir de la solucion obtenida en c). Reivindicacion 19: Un proceso para eliminar o reducir una impureza de la sal 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr solida o una solucion de 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr, comprendiendo el proceso los pasos de: a) mezclar un solvente que comprende más del 65% (v/v) de isopropanol con 1-2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr o con una solucion de 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr para obtener una solucion de 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr; y b) enfriar dicha solucion obtenida para precipitar isopropanol solvato de 1-(2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr isopropanol solvato; c) disolver isopropanol solvato de 1-[2-(2,4-dimetilfenilsulfanil) fenil]piperazina-HBr, en un solvente que no forma solvatos; y d) precipitar 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr a partir de la solucion que se obtuvo en el paso c). Reivindicacion 22: Un compuestos que es isopropanol solvato de 1-[2-(2,4-dimetilfenilsulfanil)fenil]piperazina-HBr.
ARP100100441A 2009-02-17 2010-02-16 Produccion y purificacion de 1-[2-(2,4-dimetilfenilsulfanil)fenil] piperazina AR075436A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DKPA200900223 2009-02-17

Publications (1)

Publication Number Publication Date
AR075436A1 true AR075436A1 (es) 2011-03-30

Family

ID=42101395

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100441A AR075436A1 (es) 2009-02-17 2010-02-16 Produccion y purificacion de 1-[2-(2,4-dimetilfenilsulfanil)fenil] piperazina

Country Status (28)

Country Link
US (1) US8598348B2 (es)
EP (1) EP2398785B1 (es)
JP (1) JP5738774B2 (es)
KR (1) KR101639833B1 (es)
CN (1) CN102317272B (es)
AR (1) AR075436A1 (es)
AU (1) AU2010214956B2 (es)
BR (1) BRPI1006975B1 (es)
CA (1) CA2751498C (es)
CL (1) CL2011001992A1 (es)
CO (1) CO6400224A2 (es)
DK (1) DK2398785T3 (es)
EA (1) EA020473B1 (es)
ES (1) ES2441079T3 (es)
HK (1) HK1165955A1 (es)
HR (1) HRP20131236T1 (es)
IL (1) IL214178A (es)
MX (1) MX2011008661A (es)
NZ (1) NZ594658A (es)
PL (1) PL2398785T3 (es)
PT (1) PT2398785E (es)
RS (1) RS53074B (es)
SG (1) SG173735A1 (es)
SI (1) SI2398785T1 (es)
SM (1) SMT201400010B (es)
TW (1) TW201033181A (es)
WO (1) WO2010094285A1 (es)
ZA (1) ZA201105992B (es)

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RU2608307C2 (ru) * 2012-01-03 2017-01-17 Х.Лундбек А/С Способ получения 1-[2-(2,4-диметилфенилсульфанил)фенил]пиперазина
US9499504B2 (en) 2012-09-19 2016-11-22 Sandoz Ag Crystalline form of vortioxetine hydrobromide
CN104853755B (zh) 2012-12-13 2017-08-22 H.隆德贝克有限公司 包含沃替西汀和多奈哌齐的组合物
ME02671B (me) * 2013-02-22 2017-06-20 H Lundbeck As Postupak za proizvodnju vortioksetina
WO2015035802A1 (zh) * 2013-09-12 2015-03-19 杭州普晒医药科技有限公司 沃替西汀盐及其晶体、它们的制备方法、药物组合物和用途
US10414741B2 (en) 2013-09-30 2019-09-17 Cadila Healthcare Limited Amorphous vortioxetine and salts thereof
EP2878596A1 (en) * 2013-11-29 2015-06-03 LEK Pharmaceuticals d.d. Synthesis of vortioxetine via (2-(piperazine-1-yl)phenyl)lithium intermediates
CN103788019B (zh) * 2014-01-22 2015-10-07 苏州明锐医药科技有限公司 沃替西汀的制备方法
CN103788020B (zh) * 2014-01-22 2015-11-04 苏州明锐医药科技有限公司 沃替西汀的制备方法
EA029060B1 (ru) 2014-01-31 2018-02-28 Эгиш Дьёдьсердьяр Зрт. Способ получения солей вортиоксетина
CN104059030B (zh) * 2014-05-30 2016-05-04 镇江圣安医药有限公司 [(苯硫烷基)-苯基]哌嗪的衍生物及其药物组合物和用途
CN105218482B (zh) * 2014-06-24 2018-04-06 杭州和泽医药科技有限公司 沃替西汀氢溴酸盐β晶型的制备方法
US9687484B2 (en) 2014-07-18 2017-06-27 Dipharma Francis S.R.L. Crystalline forms of an antidepressant compound
WO2016079751A2 (en) 2014-11-17 2016-05-26 Megafine Pharma (P) Ltd. A process for preparation of vortioxetine and polymorphs thereof
CN105669594A (zh) * 2014-11-19 2016-06-15 康普药业股份有限公司 抗抑郁症药1-[2-(2,4-二甲基苯基硫基)苯基]哌嗪的制备方法
CN105801517A (zh) * 2014-12-30 2016-07-27 上海奥博生物医药技术有限公司 一种沃替西汀氢溴酸盐新晶型及其制备方法
WO2016125190A2 (en) 2015-02-04 2016-08-11 Mylan Laboratories Limited Novel crystalline forms of vortioxetine, premixes, and processes for the preparation thereof
EP3274330A1 (en) 2015-03-26 2018-01-31 Cipla Limited Method for making serotonin reuptake inhibitors
CN105439980B (zh) * 2015-05-08 2017-10-24 北京北陆药业股份有限公司 一种氢溴酸沃替西汀一仲丁醇合物及其制备方法
CN105367515B (zh) * 2015-05-08 2017-10-27 北京北陆药业股份有限公司 一种氢溴酸沃替西汀α晶型的制备方法
CN106316985B (zh) * 2015-06-18 2021-11-09 郑州深蓝海生物医药科技有限公司 一种β型高效氢溴酸沃替西汀转晶方法
US20190194154A1 (en) * 2016-01-20 2019-06-27 Amneal Pharmaceuticals Company Gmbh Polymorphic Forms Of Vortioxetine Hydrobromide Tert-Butanolate
MX2018015759A (es) 2016-07-01 2019-03-21 H Lundbeck As Regimenes de dosificacion de vortioxetina para el rapido inicio del efecto antidepresivo.
US10519121B2 (en) 2016-12-30 2019-12-31 Apicore Us Llc Process and novel polymorphic form of vortioxetine and its pharmaceutically acceptable salts
ES2905962T3 (es) * 2017-04-25 2022-04-12 H Lundbeck As Procedimiento para la fabricación de la forma alfa de vortioxetina HBr
CN108017595A (zh) * 2017-12-20 2018-05-11 安徽源久源科技有限公司 一种1-[2-(2,5-二甲基苯硫基)苯基]哌嗪的制备方法
CN112125868B (zh) * 2020-09-25 2021-08-03 中山万远新药研发有限公司 一种氢溴酸伏硫西汀晶型及其制备方法、组合物与用途

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Also Published As

Publication number Publication date
CA2751498C (en) 2017-09-12
JP2012517961A (ja) 2012-08-09
ES2441079T3 (es) 2014-01-31
JP5738774B2 (ja) 2015-06-24
IL214178A0 (en) 2011-08-31
EP2398785B1 (en) 2013-11-27
SMT201400010B (it) 2014-03-07
CA2751498A1 (en) 2010-08-26
CN102317272B (zh) 2014-11-12
CN102317272A (zh) 2012-01-11
DK2398785T3 (da) 2013-12-16
MX2011008661A (es) 2011-09-06
RS53074B (en) 2014-04-30
SI2398785T1 (sl) 2014-01-31
BRPI1006975A2 (pt) 2020-08-18
PT2398785E (pt) 2013-12-26
IL214178A (en) 2014-09-30
EA201171065A1 (ru) 2012-02-28
AU2010214956B2 (en) 2012-08-23
AU2010214956A1 (en) 2011-09-22
HK1165955A1 (en) 2012-10-12
US8598348B2 (en) 2013-12-03
KR101639833B1 (ko) 2016-07-14
TW201033181A (en) 2010-09-16
HRP20131236T1 (hr) 2014-02-14
ZA201105992B (en) 2012-10-31
WO2010094285A1 (en) 2010-08-26
PL2398785T3 (pl) 2014-07-31
US20120004409A1 (en) 2012-01-05
CL2011001992A1 (es) 2012-04-09
KR20110126625A (ko) 2011-11-23
CO6400224A2 (es) 2012-03-15
EA020473B1 (ru) 2014-11-28
BRPI1006975B1 (pt) 2022-11-22
EP2398785A1 (en) 2011-12-28
NZ594658A (en) 2013-02-22
SG173735A1 (en) 2011-09-29

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