HUE028806T2 - Eljárás egy gyógyszerhatóanyag elõállítására - Google Patents

Eljárás egy gyógyszerhatóanyag elõállítására Download PDF

Info

Publication number
HUE028806T2
HUE028806T2 HUE10803222A HUE10803222A HUE028806T2 HU E028806 T2 HUE028806 T2 HU E028806T2 HU E10803222 A HUE10803222 A HU E10803222A HU E10803222 A HUE10803222 A HU E10803222A HU E028806 T2 HUE028806 T2 HU E028806T2
Authority
HU
Hungary
Prior art keywords
formula
compound
alcoholic solvent
reactor
fluoro
Prior art date
Application number
HUE10803222A
Other languages
English (en)
Inventor
Frans Therkelsen
Michael Harold Rock
Svend Treppendahl
Original Assignee
H Lundbeck As
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 H Lundbeck As filed Critical H Lundbeck As
Publication of HUE028806T2 publication Critical patent/HUE028806T2/hu

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D209/16—Tryptamines

Claims (8)

  1. Szabadalmi igénypontok Î, Eljárás IV képletö vegyület előállítására.
    Formula IV amely az alábbi lépéseket fogai ja magában: (a) (b-fluor-iH-indol-S-iljacetonltni, vizes :MH3 ás egy átmenetifém katalizátor osszekeve-rése alkoholos oldószerben; és (b) a keverék hl drogé nézésé Bx-nel.
  2. 2. Az i. igénypont szerintii eljárás,, ahol az átmenetifém katalizátor Rahfl,
  3. 3, Az 1, igénypont szerinti eljárás, ahol az alkoholos oldószer metanol.
  4. 4. Az t~3, igénypontok bármelyike szerinti eljárás., aboi a bidrogénezést 2SÜ00D pascal (2,3 par) nyomáson végezzük 16 órán keresztül,
  5. 5, Az 1*4V igénypontok bármelyike szerinti eljárás, ahol a hidrogénezést 55 és SS ®C közötti hőmérsékleten végezzük. S, A 2. igénypont szerinti eljárás, ahol az alkalmazott RaNl szivacs típusé fém·· katalizátor, 7. A 2. vagy 6,. igénypont szerinti eljárás, ahol a RaM-öen a nominális alumínium keverék S% és a RaNi átlagos részecske mérete 33 mikron,
  6. 8. Az 1-7. Igénypontok bármelyike szerinti eljárás, ahol vizes oldatban az !MH3 koncentrációja 23%,
  7. 9. Az előző igénypontok bármeiyike szerinti eljárás, amely továbbá tartalmazza a W képletű vegyület tisztifását, ahoi a Uszdtás az alábbiakat foglalja magában : (a.) a IV képletű vegyület feloldását egy alkoholos oldószerben; (b) L{-borkősav oldat hozzáadását; és (c) a borkősavas só csapadék formájú kinyerését. m A 3. igénypont szerinti eljárás, ahol az alkoholos oldószer metanol 11- A 9, vagy 10. igénypont szerinti eljárás, ahol az alkoholos oldószerrel stll-- a ceti tot alkalmazunk,
  8. 12. Az előző igénypontok bármelyike szerinti eljárás, amely továbbá tartalmazza a IV képletű vegyület reakcióját í képletű vegyület előállítására az amin 3-(2,2,3,3-tetraflyor*propexl}benzaldehlddel egy oldószerben végzett kapcsolásával, amelyet az Imin kötés egy redukáló szerrel történd redukciója követ
    Formula L 13, A 12, igénypont szerinti eljárás, ahol a redukáló szar náttíum-bérhldnd, 14. A 12, vagy 13. igénypontok szerinti eljárás, amely továbbá: tartalmazza az I képtető vegyület HO-sójává történő alakítását HO addídóval, amelyet adott esetben a kapott só 'tisztítása követ.
HUE10803222A 2009-12-23 2010-12-20 Eljárás egy gyógyszerhatóanyag elõállítására HUE028806T2 (hu)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US28953009P 2009-12-23 2009-12-23

Publications (1)

Publication Number Publication Date
HUE028806T2 true HUE028806T2 (hu) 2017-01-30

Family

ID=43567689

Family Applications (1)

Application Number Title Priority Date Filing Date
HUE10803222A HUE028806T2 (hu) 2009-12-23 2010-12-20 Eljárás egy gyógyszerhatóanyag elõállítására

Country Status (37)

Country Link
US (3) US8461353B2 (hu)
EP (1) EP2516394B1 (hu)
JP (2) JP5864435B2 (hu)
KR (2) KR101873182B1 (hu)
CN (2) CN102656146B (hu)
AR (1) AR079580A1 (hu)
AU (1) AU2010335659B2 (hu)
BR (1) BR112012015749A2 (hu)
CA (1) CA2785440C (hu)
CL (1) CL2012001725A1 (hu)
CR (1) CR20120316A (hu)
CY (1) CY1118032T1 (hu)
DK (1) DK2516394T3 (hu)
DO (1) DOP2012000170A (hu)
EA (1) EA021440B1 (hu)
ES (1) ES2575666T3 (hu)
GE (1) GEP20146078B (hu)
HK (2) HK1174921A1 (hu)
HR (1) HRP20160518T1 (hu)
HU (1) HUE028806T2 (hu)
IL (2) IL220329A (hu)
MA (1) MA33945B1 (hu)
ME (1) ME02401B (hu)
MX (1) MX2012007078A (hu)
MY (1) MY159251A (hu)
NZ (2) NZ600639A (hu)
PL (1) PL2516394T3 (hu)
PT (1) PT2516394E (hu)
RS (1) RS54820B1 (hu)
SG (1) SG181910A1 (hu)
SI (1) SI2516394T1 (hu)
SM (1) SMT201600166B (hu)
TN (1) TN2012000279A1 (hu)
TW (1) TW201139370A (hu)
UA (1) UA111584C2 (hu)
WO (1) WO2011076212A2 (hu)
ZA (1) ZA201305936B (hu)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201139370A (en) 2009-12-23 2011-11-16 Lundbeck & Co As H Processes for the manufacture of a pharmaceutically active agent
JO3459B1 (ar) 2012-09-09 2020-07-05 H Lundbeck As تركيبات صيدلانية لعلاج مرض الزهايمر
JO3639B1 (ar) * 2014-07-04 2020-08-27 H Lundbeck As صورة متعددة الشكل جديدة لـ n-[2-(6-فلورو-1h-إندول-3-يل)إيثيل]-3-(2،2،3،3-تترا فلورو بروبوكسي)بنزيل أمين هيدروكلوريد
CN104130174A (zh) * 2014-07-30 2014-11-05 天津市斯芬克司药物研发有限公司 一种吲唑衍生物及其制备方法
CN105175307A (zh) * 2014-11-18 2015-12-23 苏州晶云药物科技有限公司 Lu AE58054的盐酸盐晶型A及其制备方法和用途
TW201630881A (zh) 2014-12-12 2016-09-01 Ｈ 朗德貝克公司 用於生產艾達魯吡啶之方法
CN104529865B (zh) * 2014-12-12 2017-02-01 广东东阳光药业有限公司 苄胺类衍生物及其在药物上的应用
MA41148A (fr) * 2014-12-12 2017-10-17 H Lundbeck As Procédé de fabrication d'idalopirdine
CN108271369A (zh) * 2015-10-23 2018-07-10 法尔玛赞公司 用于制备色胺及其衍生物的新工艺
JP2019513742A (ja) 2016-04-08 2019-05-30 ハー・ルンドベック・アクチエゼルスカベット イミンの水素化によるイダロピルジンの製造方法
EP3333154A1 (en) * 2016-12-07 2018-06-13 Sandoz Ag Crystalline form of a selective 5-ht6 receptor antagonist

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3042685A (en) 1962-07-03 Process of making g-fluoro tryptamine
GB846675A (en) 1958-04-18 1960-08-31 Lab Francais Chimiotherapie Process for the production of a tryptamine derivative
US4803218A (en) * 1982-09-29 1989-02-07 Mcneilab, Inc. 3-aminoalkyl-1H-indole-5-urea and amide derivatives
DE69416697T2 (de) 1993-12-28 1999-09-09 Rhone Poulenc Fibres Verfahren zur katalytischer hydrogenierung von nitrilen zu aminen in anwesenheit eines dosierten raney nickel katalysators
EP0737101B1 (fr) 1993-12-28 1998-09-23 RHODIA FIBER & RESIN INTERMEDIATES Procede de preparation d'un catalyseur d'hydrogenation de nitriles en amines et application de ce catalyseur en hydrogenation
US5869653A (en) 1997-10-30 1999-02-09 Air Products And Chemicals, Inc. Hydrogenation of nitriles to produce amines
KR20000069831A (ko) 1997-10-31 2000-11-25 요트.게.아. 롤페즈 구성 신호에 대한 잡음 추가를 통한 엘피씨 원칙에 따라 인코딩된 음성의 오디오 표현을 위한 방법 및 장치
US6156694A (en) 1998-11-05 2000-12-05 E. I. Dupont De Nemours & Company Raney cobalt catalyst and a process for hydrogenating organic compounds using said catalyst
AU2002303094B2 (en) 2001-03-29 2006-11-23 Eli Lilly And Company N-(2-arylethyl)benzylamines as antagonists of the 5-HT6 receptor
US7084154B2 (en) * 2003-02-11 2006-08-01 Pharmacopeia Drug Disclovery, Inc. 2-(aminomethyl) arylamide analgesics
FR2866335B1 (fr) 2004-02-13 2006-05-26 Servier Lab Nouveau procede de synthese de l'agomelatine
JP2006169113A (ja) * 2004-12-10 2006-06-29 Dainippon Sumitomo Pharma Co Ltd インドール類の合成方法および合成中間体
WO2007070796A1 (en) * 2005-12-15 2007-06-21 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
EP2002834A1 (de) * 2007-06-13 2008-12-17 Bayer Schering Pharma Aktiengesellschaft Aryl/Hetarylamide als Modulatoren des EP2-Rezeptors
JO2704B1 (en) * 2007-09-21 2013-03-03 جانسين فارماسوتيكا ان في Interference inhibition factors between MD2 and B53
EP2219646A4 (en) 2007-12-21 2010-12-22 Univ Rochester METHOD FOR MODIFYING THE LIFETIME OF EUKARYOTIC ORGANISMS
WO2010036362A1 (en) * 2008-09-26 2010-04-01 Wyeth 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors
CN101531624A (zh) 2009-04-08 2009-09-16 大连凯飞精细化工有限公司 6-氟吲哚-3-乙腈的合成方法
TW201139370A (en) 2009-12-23 2011-11-16 Lundbeck & Co As H Processes for the manufacture of a pharmaceutically active agent

Also Published As

Publication number Publication date
MY159251A (en) 2016-12-30
DK2516394T3 (en) 2016-06-13
US20150080584A1 (en) 2015-03-19
KR101796330B1 (ko) 2017-11-09
EP2516394B1 (en) 2016-03-16
ME02401B (me) 2016-09-20
TW201139370A (en) 2011-11-16
US20110152539A1 (en) 2011-06-23
NZ600639A (en) 2014-07-25
SI2516394T1 (sl) 2016-07-29
IL220329A (en) 2016-03-31
KR20170125417A (ko) 2017-11-14
PL2516394T3 (pl) 2016-09-30
CN103694161A (zh) 2014-04-02
GEP20146078B (en) 2014-04-10
CA2785440C (en) 2018-05-01
JP6195605B2 (ja) 2017-09-13
CY1118032T1 (el) 2017-05-17
DOP2012000170A (es) 2012-08-31
RS54820B1 (sr) 2016-10-31
US20130245281A1 (en) 2013-09-19
AU2010335659B2 (en) 2015-05-21
PT2516394E (pt) 2016-06-07
CA2785440A1 (en) 2011-06-30
CL2012001725A1 (es) 2012-11-30
EA201290552A1 (ru) 2012-12-28
WO2011076212A3 (en) 2011-08-11
US8461353B2 (en) 2013-06-11
HK1174921A1 (en) 2013-06-21
EA021440B1 (ru) 2015-06-30
SG181910A1 (en) 2012-08-30
JP5864435B2 (ja) 2016-02-17
CN102656146B (zh) 2014-12-17
AU2010335659A1 (en) 2012-07-05
KR101873182B1 (ko) 2018-06-29
KR20120112480A (ko) 2012-10-11
HRP20160518T1 (hr) 2016-06-03
IL231141A (en) 2016-03-31
ES2575666T3 (es) 2016-06-30
MA33945B1 (fr) 2013-01-02
IL231141A0 (en) 2014-03-31
WO2011076212A2 (en) 2011-06-30
CN103694161B (zh) 2015-09-09
CN102656146A (zh) 2012-09-05
TN2012000279A1 (en) 2013-12-12
US9382205B2 (en) 2016-07-05
JP2016117734A (ja) 2016-06-30
ZA201305936B (en) 2015-09-30
UA111584C2 (uk) 2016-05-25
BR112012015749A2 (pt) 2015-09-15
IL220329A0 (en) 2012-08-30
CR20120316A (es) 2012-08-16
SMT201600166B (it) 2016-07-01
US8901318B2 (en) 2014-12-02
NZ625798A (en) 2014-10-31
JP2013515683A (ja) 2013-05-09
EP2516394A2 (en) 2012-10-31
MX2012007078A (es) 2012-07-20
HK1196352A1 (en) 2014-12-12
AR079580A1 (es) 2012-02-01

Similar Documents

Publication Publication Date Title
DK2516394T3 (en) PROCEDURE FOR THE PREPARATION OF A PHARMACEUTICAL ACTIVE AGENT
CA2160966C (fr) Derives de piperidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP3356726B2 (ja) ５ＨＴ１Ａリガンドとしてのピロロ［１，２−ａ］ピラジン誘導体
EP2852572B1 (en) Carboline and carbazole based imaging agents for detecting neurological dysfunction
EP2167083B1 (en) 1- heteroaryl-3-azabicyclo[3.1.0]hexanes, methods for their preparation and their use as medicaments
SK382004A3 (en) 5-halo-tryptamine derivatives used as ligands of the 5-HT6 and/or 5-HT7 serotonin receptors
WO2008044656A1 (fr) Dérivé d'imidazolidinone
AU2004228760A1 (en) Azabicyclo derivatives as muscarinic receptor antagonists
TW470745B (en) Hexahydro-pyrido[4,3-b]indole derivatives
HRP940960A2 (en) N-substituted azabicycloheptane derivatives, the preparation and use thereof
JP3886829B2 (ja) 新規インデノインドロン化合物、それらの調製方法およびそれらを含む医薬組成物
JP4499208B2 (ja) 新規な光学活性アミノペンタン誘導体
US6410787B2 (en) Process to prepare 2-aminoindan derivatives
EP1241169A1 (fr) Dérivés d'isoindoloindolone, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
CA2756876A1 (en) A process for the preparation of frovatriptan and frovatriptan succinate and their synthetic intermediates
JP2019513742A (ja) イミンの水素化によるイダロピルジンの製造方法
NZ299232A (en) (+)-6-carboxamido-3-n-ethylamino-1,2,3,4- tetrahydrocarbazoles; medicaments thereof
KR20060014373A (ko) 무스카린 수용체 길항제로서의 치환된 아자비시클로 헥산유도체
JP2003081960A (ja) トリフルオロプロピルアミノペンタン誘導体及びその製造方法