[go: up one dir, main page]

MX169619B - Procedimiento para sintetizar derivados de aminometil-oxo-oxalidinil-benceno utiles como agentes antibacterianos - Google Patents

Procedimiento para sintetizar derivados de aminometil-oxo-oxalidinil-benceno utiles como agentes antibacterianos

Info

Publication number
MX169619B
MX169619B MX006049A MX604984A MX169619B MX 169619 B MX169619 B MX 169619B MX 006049 A MX006049 A MX 006049A MX 604984 A MX604984 A MX 604984A MX 169619 B MX169619 B MX 169619B
Authority
MX
Mexico
Prior art keywords
compounds
formula
solvent
amine
reaction
Prior art date
Application number
MX006049A
Other languages
English (en)
Inventor
Walter Adelman Gregory
Original Assignee
Du Pont Merck Pharma
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 Du Pont Merck Pharma filed Critical Du Pont Merck Pharma
Publication of MX169619B publication Critical patent/MX169619B/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente invención se refiere a procedimiento para sintetizar derivados de amino-metil-oxooxazolidinil-benceno útiles como agentes antibacterianos, de la fórmula I: caracterizado el procedimiento porque comprende reaccionar un compuesto de fórmula II: para dar compuestos de fórmula III: a) los cuales se hacen reaccionar a temperatura aproximada de 60 a 125 grados C con azidas de sodio, potasio, litio, cesio o rubidio en presencia de un solvente dipolar aprótico, en cuyos compuestos de grupo A puede ser -H ó cualquiera de los grupos previamente mostrados excepto cuando R1 es -N3, -NX2,-NR9X, -NXZ+, para obtener compuestos de la fórmula IV: los cuales se reducen a compuestos de aminometilo (V): por hidrogenación en paladio sobre carbón, por tratamiento con 1,3-propanditiol y una base, sulfuro de hidrógeno, compuestos de fósforo, trivalentes o mercaptanos, en la presencia de un solvente, luego los compuestos de fórmula V se acilan por reacción de la amina con un cloruro o anhídrido de ácido en un solvente básico tal como piridina o por reacción en un solvente miscible en agua, o alternativamente un ácido libre se hace reaccionar con la amina empleando N,N-diciclohexilcarbodiimida o primero se forma un anhídrido mixto a partir del ácido empleando un ester clorofórmico y una base terciaria, seguido por reacción con la amina.
MX006049A 1983-06-07 1984-06-06 Procedimiento para sintetizar derivados de aminometil-oxo-oxalidinil-benceno utiles como agentes antibacterianos MX169619B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US50189783A 1983-06-07 1983-06-07
US57833284A 1984-02-14 1984-02-14

Publications (1)

Publication Number Publication Date
MX169619B true MX169619B (es) 1993-07-15

Family

ID=27053956

Family Applications (1)

Application Number Title Priority Date Filing Date
MX006049A MX169619B (es) 1983-06-07 1984-06-06 Procedimiento para sintetizar derivados de aminometil-oxo-oxalidinil-benceno utiles como agentes antibacterianos

Country Status (16)

Country Link
EP (1) EP0127902B1 (es)
AU (1) AU583250B2 (es)
CA (2) CA1254213A (es)
DE (1) DE3485162D1 (es)
DK (1) DK279584A (es)
ES (2) ES8506659A1 (es)
FI (1) FI83216C (es)
GR (1) GR82361B (es)
HU (1) HU194194B (es)
IE (1) IE57619B1 (es)
IL (1) IL72028A (es)
MX (1) MX169619B (es)
NO (1) NO163451C (es)
NZ (1) NZ208395A (es)
PT (1) PT78703A (es)
SU (2) SU1505442A3 (es)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4705799A (en) * 1983-06-07 1987-11-10 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl benzenes useful as antibacterial agents
CA1260948A (en) * 1984-12-05 1989-09-26 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl benzene derivatives useful as antibacterial agents
CA1323370C (en) * 1986-09-12 1993-10-19 Davis H. Crater Fluorochemical oxazolidinones
US5099026A (en) * 1986-09-12 1992-03-24 Crater Davis H Fluorochemical oxazolidinones
US5032605A (en) * 1987-10-09 1991-07-16 Du Pont Merck Pharmaceutical Company Aminomethyl oxooxazolidinyl oxa or thia cycloalkylbenzene derivatives useful as antibacterial agents
US5039690A (en) * 1987-10-09 1991-08-13 Du Pont Merck Pharmaceutical Company Aminomethyl oxooxazolidinyl oxa or thia cycloalkylbenzene derivatives useful as antibacterial agents
US4921869A (en) * 1987-10-09 1990-05-01 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives useful as antibacterial agents
US4801600A (en) * 1987-10-09 1989-01-31 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives useful as antibacterial agents
US4965268A (en) * 1987-10-09 1990-10-23 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives useful as antibacterial agents
US5036093A (en) * 1987-10-09 1991-07-30 Du Pont Merck Pharmaceutical Aminomethyl oxooxazolidinyl azacycloalkylbenzene derivatives useful as antibacterial agents
US5036092A (en) * 1987-10-09 1991-07-30 Du Pont Merck Pharmaceutical Aminomethyl oxooxazolidinyl azacycloalkylbenzene derivatives useful as antibacterial agents
US4985429A (en) * 1987-10-09 1991-01-15 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives useful as antibacterial agents
CA1320730C (en) * 1987-10-16 1993-07-27 The Du Pont Merck Pharmaceutical Company Aminomethyl oxooxazolidinyl aroylbenzene derivatives useful as antibacterial agents
US4942183A (en) * 1987-10-16 1990-07-17 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl aroylbenzene derivatives useful as antibacterial agents
ATE95176T1 (de) * 1987-10-21 1993-10-15 Du Pont Merck Pharma Aminomethyl-oxo-oxazolidinyl-ethenylbenzenderivate, nuetzlich als antibakterielles mittel.
US4977173A (en) * 1987-10-21 1990-12-11 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl ethenylbenzene derivatives useful as antibacterial agents
US4948801A (en) * 1988-07-29 1990-08-14 E. I. Du Pont De Nemours And Company Aminomethyloxooxazolidinyl arylbenzene derivatives useful as antibacterial agents
EP0359418B1 (en) * 1988-09-15 1994-10-12 The Upjohn Company 5'-Indolinyl-5beta-amidomethyloxazolidin-2-ones, 3-(fused-ring substituted)phenyl-5beta-amidomethyloxazolidin-2-ones and 3-(nitrogen substituted)phenyl-5beta-amidomethyloxazolidin-2-ones
US5225565A (en) * 1988-09-15 1993-07-06 The Upjohn Company Antibacterial 3-(fused-ring substituted)phenyl-5β-amidomethyloxazolidin-2-ones
US5182403A (en) * 1988-09-15 1993-01-26 The Upjohn Company Substituted 3(5'indazolyl) oxazolidin-2-ones
US5231188A (en) * 1989-11-17 1993-07-27 The Upjohn Company Tricyclic [6.5.51]-fused oxazolidinone antibacterial agents
KR100257418B1 (ko) * 1991-11-01 2000-05-15 로렌스 티. 마이젠헬더 치환된 아릴-및 헤테로아릴-페닐옥사졸리디논
AU670842B2 (en) * 1992-12-08 1996-08-01 Pharmacia & Upjohn Company Tropone-substituted phenyloxazolidinone antibacterial agents
TW299332B (es) * 1992-12-08 1997-03-01 Upjohn Co
US5688792A (en) * 1994-08-16 1997-11-18 Pharmacia & Upjohn Company Substituted oxazine and thiazine oxazolidinone antimicrobials
MY115155A (en) * 1993-09-09 2003-04-30 Upjohn Co Substituted oxazine and thiazine oxazolidinone antimicrobials.
CA2200433C (en) * 1994-10-26 2006-02-07 Douglas K. Hutchinson Phenyloxazolidinone antimicrobials
US5883093A (en) * 1995-09-12 1999-03-16 Pharmacia & Upjohn Company Phenyloxazolidinone antimicrobials
GB9601666D0 (en) * 1996-01-27 1996-03-27 Zeneca Ltd Chemical compounds
GB9702213D0 (en) 1996-02-24 1997-03-26 Zeneca Ltd Chemical compounds
GB9609919D0 (en) 1996-05-11 1996-07-17 Zeneca Ltd Chemical compounds
DE69829846T2 (de) 1997-05-30 2006-02-23 Pharmacia & Upjohn Co. Llc, Kalamazoo Antibakteriell wirksam oxazolidinone mit einer thiocarbonylfunktionalität
US6255304B1 (en) 1997-05-30 2001-07-03 Pharmacia & Upjohn Company Oxazolidinone antibacterial agents having a thiocarbonyl functionality
GB9717804D0 (en) 1997-08-22 1997-10-29 Zeneca Ltd Chemical compounds
GB9717807D0 (en) 1997-08-22 1997-10-29 Zeneca Ltd Chemical compounds
AU9001598A (en) * 1997-09-11 1999-03-29 Hokuriku Seiyaku Co. Ltd Thiourea derivatives
GB9725244D0 (en) 1997-11-29 1998-01-28 Zeneca Ltd Chemical compounds
JP2002501059A (ja) * 1998-01-23 2002-01-15 ファルマシア・アンド・アップジョン・カンパニー オキサゾリジノンの組合せライブラリー、組成物および調製方法
GB9821938D0 (en) * 1998-10-09 1998-12-02 Zeneca Ltd Chemical compounds
BR0010982A (pt) * 1999-05-27 2002-03-05 Upjohn Co Novas oxazolidinonas bicìclicas como agentes antibacterianos
US6297242B1 (en) * 1999-08-12 2001-10-02 Ortho-Mcneil Pharmaceutical, Inc. N-substituted amidine and guanidine oxazolidinone antibacterials and methods of use thereof
GB9928568D0 (en) 1999-12-03 2000-02-02 Zeneca Ltd Chemical compounds
US6518285B2 (en) 1999-12-21 2003-02-11 Ortho Mcneil Pharmaceutical, Inc. Piperidinyloxy and pyrrolidinyloxy oxazolidinone antibacterials
DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
GB0009803D0 (en) 2000-04-25 2000-06-07 Astrazeneca Ab Chemical compounds
WO2002032857A1 (en) * 2000-10-17 2002-04-25 Pharmacia & Upjohn Company Methods of producing oxazolidinone compounds
DE10129725A1 (de) 2001-06-20 2003-01-02 Bayer Ag Kombinationstherapie substituierter Oxazolidinone
DE10300111A1 (de) 2003-01-07 2004-07-15 Bayer Healthcare Ag Verfahren zur Herstellung von 5-Chlor-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarboxamid
DE10355461A1 (de) 2003-11-27 2005-06-23 Bayer Healthcare Ag Verfahren zur Herstellung einer festen, oral applizierbaren pharmazeutischen Zusammensetzung
EP1685841A1 (en) 2005-01-31 2006-08-02 Bayer Health Care Aktiengesellschaft Prevention and treatment of thromboembolic disorders
DE102005045518A1 (de) 2005-09-23 2007-03-29 Bayer Healthcare Ag 2-Aminoethoxyessigsäure-Derivate und ihre Verwendung
RU2429236C2 (ru) 2005-10-04 2011-09-20 Байер Шеринг Фарма Акциенгезельшафт Новая полиморфная форма и аморфная форма 5-хлор-n-({(5s)-2-оксо-3-[4-(3-оксо-4-морфолинил)-фенил]-1, 3-оксазолидин-5-ил}-метил)-2-тиофенкарбоксамида
DE102005047561A1 (de) 2005-10-04 2007-04-05 Bayer Healthcare Ag Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung
KR101653570B1 (ko) 2011-03-30 2016-09-02 주식회사 레고켐 바이오사이언스 신규한 옥사졸리디논 유도체 및 이를 함유하는 의약 조성물

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1222708A (en) * 1968-10-22 1971-02-17 Delalande Sa Novel 5-(n-substituted aminomethyl)-2-oxazolidinones and their process of preparation
US4348393A (en) * 1978-06-09 1982-09-07 Delalande S.A. N-Aryl oxazolidinones, oxazolidinethiones, pyrrolidinones, pyrrolidines and thiazolidinones
US4340606A (en) * 1980-10-23 1982-07-20 E. I. Du Pont De Nemours And Company 3-(p-Alkylsulfonylphenyl)oxazolidinone derivatives as antibacterial agents
FR2500450A1 (fr) * 1981-02-25 1982-08-27 Delalande Sa Nouveaux derives aminomethyl-5 oxazolidiniques, leur procede de preparation et leur application en therapeutique
AU560666B2 (en) * 1981-12-04 1987-04-16 E.I. Du Pont De Nemours And Company P(2-oxo oxazolidinyl)benzene sulphonamides
CA1260948A (en) * 1984-12-05 1989-09-26 E. I. Du Pont De Nemours And Company Aminomethyl oxooxazolidinyl benzene derivatives useful as antibacterial agents

Also Published As

Publication number Publication date
EP0127902B1 (en) 1991-10-16
ES533097A0 (es) 1985-08-01
DE3485162D1 (de) 1991-11-21
FI842273A0 (fi) 1984-06-06
NO842273L (no) 1984-12-10
CA1254213A (en) 1989-05-16
SU1426451A3 (ru) 1988-09-23
HU194194B (en) 1988-01-28
NZ208395A (en) 1987-07-31
HUT34462A (en) 1985-03-28
FI842273A (fi) 1984-12-08
DK279584A (da) 1984-12-08
AU583250B2 (en) 1989-04-27
EP0127902A3 (en) 1987-09-02
FI83216C (fi) 1991-06-10
IE57619B1 (en) 1993-02-10
SU1505442A3 (ru) 1989-08-30
PT78703A (en) 1984-07-01
CA1275652C (en) 1990-10-30
DK279584D0 (da) 1984-06-06
IL72028A0 (en) 1984-10-31
AU2909984A (en) 1984-12-13
ES540812A0 (es) 1988-03-16
NO163451C (no) 1990-05-30
IE841407L (en) 1984-12-07
ES8802037A1 (es) 1988-03-16
FI83216B (fi) 1991-02-28
ES8506659A1 (es) 1985-08-01
IL72028A (en) 1988-05-31
EP0127902A2 (en) 1984-12-12
GR82361B (es) 1984-12-13
NO163451B (no) 1990-02-19

Similar Documents

Publication Publication Date Title
MX169619B (es) Procedimiento para sintetizar derivados de aminometil-oxo-oxalidinil-benceno utiles como agentes antibacterianos
ES8507479A1 (es) Un metodo para producir un derivado de amina
KR840005718A (ko) 오메프라졸 중간체의 제조방법
PE20070318A1 (es) Metodo para purificar tigeciclina
KR880000408A (ko) 알키닐 아미노 누클레오티드
ES8607243A1 (es) Esteres de aminoacidos y de peptidos cromogenos
ES8604215A1 (es) Un procedimiento para la preparacion de derivados enol-eteres de oxicanis.
KR840007011A (ko) 세펨 화합물의 제조방법
Hayakawa et al. Allyl protection of internucleotide linkage
ES8604982A1 (es) Una composicion que contiene una sal preparada por reaccion de (a) por lo menos un compuesto de un acido ditiofosforado
ES8301883A1 (es) Procedimiento para la preparacion de derivados de ciclohexe-no
IT1165252B (it) Procedimento di purificazione dell'acido ursodesossicolico attraverso nuovi derivati
ES8505922A1 (es) Procedimiento para preparar nuevos derivados del acido 4-fenil-4-oxo-buten-2-oico
KR840001581A (ko) 베타-락타마제 억제제 2-베타-치환-2-알파-메틸-(5r)펜임-3-알파카복실산 1,1-디옥사이드 및 그 중간체의 제조방법
AR242396A1 (es) Procedimiento para preparar nelitimicina.
ES8602002A1 (es) Procedimiento para preparar nuevas 4-fenil-tetrahidrofurano-(2,3-c)priridinas
GB1410409A (en) Lincosamine derivatives
ES2114231T3 (es) Procedimiento para la produccion de una sal de adicion de acido del isomero z de un compuesto de trifeniletileno.
NO985619D0 (no) FremgangsmÕte for Õ fremstille et acylgruppeholdig heksaazaisowurtzitanderivat
BR9814266A (pt) Processo para a preparação de oxazafosforin-2-aminas
ES8200689A1 (es) Un procedimiento para la produccion de analogos de cefalosporina.
KR840005107A (ko) 피리미디온 및 그의 산부가염의 제조방법
US2269791A (en) Esters of p-aminobenzoic acid
ES8607971A1 (es) Procedimiento para la obtencion de compuestos de 2-heterociclil-tio-alquilo inferior-penem
MX9804311A (es) Procedimiento para preparar dioxoazabiciclohexanos.