ZA200308697B - Process for the production of the piperidine derivative fexofenadine. - Google Patents

Process for the production of the piperidine derivative fexofenadine. Download PDF

Info

Publication number: ZA200308697B
Authority: ZA; South Africa
Prior art keywords: alkyl; formula; compound; carbon atoms; process according
Prior art date: 2001-06-15

Application number

ZA200308697A

Other languages

English (en)

Inventor

Collin Schroeder

Ryan Huddleston

Richard Charles

Original Assignee

Aventis Pharma Gmbh

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.)

2001-06-15

Filing date

2003-11-07

Publication date

2004-09-03

2003-11-07 Application filed by Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh

2004-09-03 Publication of ZA200308697B publication Critical patent/ZA200308697B/en

Links

238000000034 method Methods 0.000 title claims description 35
150000003053 piperidines Chemical class 0.000 title claims description 13
238000004519 manufacturing process Methods 0.000 title claims description 7
RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 title description 13
229960003592 fexofenadine Drugs 0.000 title description 9
125000000217 alkyl group Chemical group 0.000 claims description 57
125000004432 carbon atom Chemical group C* 0.000 claims description 39
150000001875 compounds Chemical class 0.000 claims description 37
-1 piperidine derivative compound Chemical class 0.000 claims description 20
239000000203 mixture Substances 0.000 claims description 11
229910052739 hydrogen Inorganic materials 0.000 claims description 10
150000003839 salts Chemical class 0.000 claims description 10
239000002841 Lewis acid Substances 0.000 claims description 8
150000007517 lewis acids Chemical class 0.000 claims description 8
239000007858 starting material Substances 0.000 claims description 7
NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 7
125000000896 monocarboxylic acid group Chemical group 0.000 claims description 3
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 7
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
MCQRPQCQMGVWIQ-UHFFFAOYSA-N boron;methylsulfanylmethane Chemical compound [B].CSC MCQRPQCQMGVWIQ-UHFFFAOYSA-N 0.000 claims 2
238000011084 recovery Methods 0.000 claims 2
UCKMPCXJQFINFW-UHFFFAOYSA-N Sulphide Chemical compound [S-2] UCKMPCXJQFINFW-UHFFFAOYSA-N 0.000 claims 1
125000002887 hydroxy group Chemical group [H]O* 0.000 description 9
239000001257 hydrogen Substances 0.000 description 5
125000004435 hydrogen atom Chemical group [H]* 0.000 description 5
239000000543 intermediate Substances 0.000 description 5
GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 4
239000004480 active ingredient Substances 0.000 description 4
229940008201 allegra Drugs 0.000 description 4
230000001387 anti-histamine Effects 0.000 description 4
239000000739 antihistaminic agent Substances 0.000 description 4
230000001624 sedative effect Effects 0.000 description 4
229910052799 carbon Inorganic materials 0.000 description 3
125000001424 substituent group Chemical group 0.000 description 3
125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 2
125000004093 cyano group Chemical group *C#N 0.000 description 2
229910052736 halogen Inorganic materials 0.000 description 2
150000002367 halogens Chemical class 0.000 description 2
241001442234 Cosa Species 0.000 description 1
239000002253 acid Substances 0.000 description 1
125000003545 alkoxy group Chemical group 0.000 description 1
CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
- C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
- C07C69/738—Esters of keto-carboxylic acids or aldehydo-carboxylic acids
- 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
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Life Sciences & Earth Sciences (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmacology & Pharmacy (AREA)
Engineering & Computer Science (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Hydrogenated Pyridines (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

ZA200308697A 2001-06-15 2003-11-07 Process for the production of the piperidine derivative fexofenadine. ZA200308697B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US29839701P	2001-06-15	2001-06-15

Publications (1)

Publication Number	Publication Date
ZA200308697B true ZA200308697B (en)	2004-09-03

Family

ID=23150325

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200308697A ZA200308697B (en)	2001-06-15	2003-11-07	Process for the production of the piperidine derivative fexofenadine.

Country Status (23)

Country	Link
US (2)	US6743941B2 (de)
EP (1)	EP1401816B1 (de)
JP (1)	JP4344230B2 (de)
KR (1)	KR100903285B1 (de)
CN (1)	CN1229347C (de)
AR (1)	AR037005A1 (de)
AT (1)	ATE386021T1 (de)
AU (1)	AU2002320847B2 (de)
BR (1)	BR0210410A (de)
CA (1)	CA2450313C (de)
DE (1)	DE60225008T2 (de)
DK (1)	DK1401816T3 (de)
ES (1)	ES2298384T3 (de)
HK (1)	HK1063795A1 (de)
HU (1)	HUP0401125A2 (de)
IL (2)	IL159304A0 (de)
MX (1)	MXPA03010960A (de)
NO (1)	NO20035572L (de)
NZ (1)	NZ530153A (de)
PL (1)	PL364369A1 (de)
PT (1)	PT1401816E (de)
WO (1)	WO2002102776A1 (de)
ZA (1)	ZA200308697B (de)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US7498443B2 (en) *	2004-09-17	2009-03-03	Albany Molecular Research, Inc.	Process for production of carebastine
US7498345B2 (en) *	2004-09-17	2009-03-03	Albany Molecular Research, Inc.	Process for production of piperidine derivatives
CN100453522C (zh) *	2005-01-26	2009-01-21	中国科学技术大学	4-[4-(1-乙氧基酰基-1-甲基乙基苯)]-4-氧代丁酸的制备方法
WO2007135693A2 (en) *	2006-05-18	2007-11-29	Ind-Swift Laboratories Limited	Intermediates useful for the preparation of antihistaminic piperidine derivative
ITMI20061491A1 (it) *	2006-07-27	2008-01-28	Archimica Srl	Processo per la preparazione di fexofenadina.
ITMI20061492A1 (it) *	2006-07-27	2008-01-28	Archimica Srl	Processo per la preparazione di fexofenadina.
CN102070490B (zh) *	2009-11-21	2014-07-30	浙江华海药业股份有限公司	一种非索非那定中间体2-(4-(4-羟基丁酰基)苯基)-2-甲基丙氰的制备方法
CN102070570A (zh) *	2009-11-21	2011-05-25	浙江华海药业股份有限公司	一种非索非那定中间体2-甲基-2(4-(2-氧代四氢呋喃-3-羰基)苯基)丙氰及其盐的制备方法
ES2930050T3 (es)	2015-06-15	2022-12-05	Asana Biosciences Llc	Inhibidores heterocíclicos de ERK1 y ERK2 y su uso en el tratamiento de cáncer
CN104876853B (zh) *	2015-06-17	2017-06-16	苏州卫生职业技术学院	盐酸非索非那定的合成方法
EP3365327B1 (de)	2015-10-22	2019-11-20	Sanofi-Aventis Deutschland GmbH	Verfahren zur herstellung von fexofenadin und darin verwendete zwischenprodukte
TW202128665A (zh)	2019-10-28	2021-08-01	美商阿沙納生物科學公司	使用ｅｒｋ１與ｅｒｋ２之雜環抑制劑之改良之方法、套組、組成物及給藥攝生法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE2946809A1 (de) *	1979-11-20	1981-06-11	A. Nattermann & Cie GmbH, 5000 Köln	4-phenyl-4-oxo-buttersaeuren, deren salze und ester, verfahren zu deren herstellung und diese enthaltende arzneimittel
IT1200123B (it)	1985-09-27	1989-01-05	Ind Chimica Srl	Procedimento per la preparazione di alfa-(p-terbutilfenil)-4-(idrossidifenilmetil)-1-piperidinobutanolo
EP0347123A3 (de)	1988-06-17	1991-07-03	Fisons Corporation	Dibenzo-cycloheptenyl-, -cycloheptyl- und -oxepinylamine mit antihistaminischer Aktivität
IT1249684B (it)	1991-07-19	1995-03-09	Sorin Biomedica Spa	Epitopi della proteina env del virus dell'epatite c.
CA2117892C (en) *	1992-04-10	2001-12-18	Chi-Hsin R. King	4-diphenylmethyl piperidine derivatives and process for their preparation
DE69434696T2 (de)	1993-06-24	2006-11-16	Amr Technology, Inc.	Verfahren zur Herstellung von Verbindungen geeignet als Zwischenprodukte

2002
- 2002-06-11 US US10/166,893 patent/US6743941B2/en not_active Expired - Lifetime
- 2002-06-12 MX MXPA03010960A patent/MXPA03010960A/es active IP Right Grant
- 2002-06-12 NZ NZ530153A patent/NZ530153A/en not_active IP Right Cessation
- 2002-06-12 IL IL15930402A patent/IL159304A0/xx unknown
- 2002-06-12 DK DK02754657T patent/DK1401816T3/da active
- 2002-06-12 EP EP02754657A patent/EP1401816B1/de not_active Expired - Lifetime
- 2002-06-12 KR KR1020037016429A patent/KR100903285B1/ko not_active IP Right Cessation
- 2002-06-12 CN CNB028119312A patent/CN1229347C/zh not_active Expired - Fee Related
- 2002-06-12 CA CA2450313A patent/CA2450313C/en not_active Expired - Fee Related
- 2002-06-12 PL PL02364369A patent/PL364369A1/xx not_active Application Discontinuation
- 2002-06-12 AU AU2002320847A patent/AU2002320847B2/en not_active Ceased
- 2002-06-12 PT PT02754657T patent/PT1401816E/pt unknown
- 2002-06-12 HU HU0401125A patent/HUP0401125A2/hu unknown
- 2002-06-12 DE DE60225008T patent/DE60225008T2/de not_active Expired - Lifetime
- 2002-06-12 WO PCT/EP2002/006424 patent/WO2002102776A1/en active IP Right Grant
- 2002-06-12 AT AT02754657T patent/ATE386021T1/de active
- 2002-06-12 ES ES02754657T patent/ES2298384T3/es not_active Expired - Lifetime
- 2002-06-12 JP JP2003505319A patent/JP4344230B2/ja not_active Expired - Fee Related
- 2002-06-12 BR BR0210410-5A patent/BR0210410A/pt not_active IP Right Cessation
- 2002-06-14 AR ARP020102261A patent/AR037005A1/es unknown
2003
- 2003-11-07 ZA ZA200308697A patent/ZA200308697B/en unknown
- 2003-12-10 IL IL159304A patent/IL159304A/en not_active IP Right Cessation
- 2003-12-12 NO NO20035572A patent/NO20035572L/no unknown
2004
- 2004-04-22 US US10/829,803 patent/US7235665B2/en not_active Expired - Lifetime
- 2004-09-03 HK HK04106643A patent/HK1063795A1/xx not_active IP Right Cessation

Also Published As

Publication number	Publication date
HUP0401125A2 (hu)	2004-09-28
DE60225008T2 (de)	2009-01-29
NZ530153A (en)	2005-07-29
AR037005A1 (es)	2004-10-20
US7235665B2 (en)	2007-06-26
CN1516689A (zh)	2004-07-28
IL159304A0 (en)	2004-06-01
CA2450313C (en)	2010-08-10
MXPA03010960A (es)	2004-02-27
KR20040010720A (ko)	2004-01-31
NO20035572D0 (no)	2003-12-12
US20040198983A1 (en)	2004-10-07
PT1401816E (pt)	2008-04-08
PL364369A1 (en)	2004-12-13
DK1401816T3 (da)	2008-06-09
ES2298384T3 (es)	2008-05-16
KR100903285B1 (ko)	2009-06-17
EP1401816B1 (de)	2008-02-13
JP2005502603A (ja)	2005-01-27
EP1401816A1 (de)	2004-03-31
ATE386021T1 (de)	2008-03-15
CN1229347C (zh)	2005-11-30
JP4344230B2 (ja)	2009-10-14
CA2450313A1 (en)	2002-12-27
US6743941B2 (en)	2004-06-01
HK1063795A1 (en)	2005-01-14
US20030105329A1 (en)	2003-06-05
WO2002102776A1 (en)	2002-12-27
NO20035572L (no)	2004-02-16
AU2002320847B2 (en)	2007-09-20
DE60225008D1 (de)	2008-03-27
BR0210410A (pt)	2004-08-17
IL159304A (en)	2010-02-17

Publication	Publication Date	Title
ZA200308697B (en)	2004-09-03	Process for the production of the piperidine derivative fexofenadine.
AU653364B2 (en)	1994-09-29	Xanthine derivatives
NO2015020I2 (no)	2015-09-10	Ceritinib eller et farmasøytisk akseptabelt salt derav
WO2004103977A3 (en)	2005-01-06	Process for the preparation of pyrimidine derivatives
AU645698B2 (en)	1994-01-20	4-pyrimidinecarboxamide derivatives, their preparation and their application in therapy
RS49836B (sr)	2008-08-07	Postupci i intermedijeri za dobijanje anti-kancernih jedinjenja
KR900018034A (ko)	1990-12-20	치환 4-(퀴놀린-2-일-메톡시)페닐-아세트산 유도체
RS52163B (en)	2012-08-31	DERIVATES THE BICYCLESTER
DK0979821T3 (da)	2007-01-29	Tricykliske forbindelser
IE38318B1 (en)	1978-02-15	Derivatives of 2-amino-and 4-amino quinazoline and pharmaceutical compositions containing them
ES8701774A1 (es)	1986-12-01	Procedimiento para preparar analogos de adenosinas n6 susti-tuidas
KR860007221A (ko)	1986-10-08	시클로펜타[d] 피리미딘 유도체의 제조방법
ES8307760A1 (es)	1983-08-01	Un procedimiento para la preparacion de derivados de 4-anilino-pirimidina.
KR850008666A (ko)	1985-12-21	치환된 비스-(4-아미노페닐)-설폰의 제조방법
BR9206499A (pt)	1995-11-21	Esteres de 3-quinuclidina,processo e intermediários para sua preparação e composições farmacêuticas contendo os mesmos
ATE45738T1 (de)	1989-09-15	1-cyclopropyl-1,4-dihydro-4-oxo-7-(4-(2-oxo-1,3 dioxol-4-yl-methyl)-1-piperazinyl>-3chinolincarbons\|uren, verfahren zu ihrer herstellung sowie diese enthaltende antibakterielle mittel.
SE461654B (sv)	1990-03-12	Saett att framstaella racemiska cis- och/eller trans-apovinkaminsyraestrar
HRP20120971T1 (hr)	2012-12-31	Postupak za pripravu supstituranih 1,3-oksatiolana
Biel et al.	1954	Bronchodilators, N-Substituted Derivatives of 1-(3', 4'-Dihydroxyphenyl)-2-aminoethanol (Arterenol)
WO2003016279A1 (fr)	2003-02-27	Composes polycycliques fusionnes
PT97032A (pt)	1992-02-28	Processo para a preparacao de derivado do acido (benzidriloxi-etilpiperidil)-alifatico utilizaveis como agente anti-histaminicos
SE8501988D0 (sv)	1985-04-24	Iminothiazolidine derivatives
NO330965B1 (no)	2011-08-29	Fremgangsmate for fremstilling av substituerte imidazolderivater, mellomprodukter anvendt i fremgangsmaten samt fremgangsmate for fremstilling av mellomprodukt
PT968189E (pt)	2002-04-29	Processo para a preparacao de acidos nicotinicos
US4507308A (en)	1985-03-26	Analgesically or anti-inflammatory effective 4-quinolyl anthranilic acid derivatives