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FI72980B - Foerfarande foer framstaellning av 4ç-epi-9-deoxo-9a-metyl-9a-aza-9a-homoerytromycin a och dess farmaceutiskt godtagbara salter samt mellanprodukterna anvaenda i foerfarandet. - Google Patents

Foerfarande foer framstaellning av 4ç-epi-9-deoxo-9a-metyl-9a-aza-9a-homoerytromycin a och dess farmaceutiskt godtagbara salter samt mellanprodukterna anvaenda i foerfarandet. Download PDF

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Publication number
FI72980B
FI72980B FI834163A FI834163A FI72980B FI 72980 B FI72980 B FI 72980B FI 834163 A FI834163 A FI 834163A FI 834163 A FI834163 A FI 834163A FI 72980 B FI72980 B FI 72980B
Authority
FI
Finland
Prior art keywords
aza
deoxo
homoerythromycin
methyl
epi
Prior art date
Application number
FI834163A
Other languages
English (en)
Finnish (fi)
Other versions
FI834163A (fi
FI72980C (sv
FI834163A0 (fi
Inventor
Gene Michael Bright
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of FI834163A0 publication Critical patent/FI834163A0/fi
Publication of FI834163A publication Critical patent/FI834163A/fi
Application granted granted Critical
Publication of FI72980B publication Critical patent/FI72980B/fi
Publication of FI72980C publication Critical patent/FI72980C/sv

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
    • 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
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Communicable Diseases (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Cosmetics (AREA)
  • Developing Agents For Electrophotography (AREA)
  • Other Investigation Or Analysis Of Materials By Electrical Means (AREA)
  • Investigating Or Analysing Materials By The Use Of Chemical Reactions (AREA)

Claims (4)

1. Förfarande för framställning av 4"-epi-9-deoxo-9a-metyl-9a-aza-9a-homoerytromycin A med formeln: 5 ^v'‘‘CH3 N(CH3)2 CH -N9a 7\ CH I , yCii3 Jr s*l HO/, CH- io H°"% H(A‘‘ 3 K°\ll2 Λ 3/^CH3 ?Η2'Ί ,Γ"°1(| ,/<ΚΤΗ CH3 °v1^CH3 f T 3 0
15 CH3 OCH3 eller ett farmaceutiskt godtagbart sait därav, kanne-t e c k n a t därav, att a) 4"-epi-9-deoxo-9a-aza-9a-homoerytromycin A metyle-20 ras med formaldehyd i närvaro av ett reduktionsmedel, vilket valts bland myrsyra, cyanborhydrid eller väte samt en ädel-metallkatalysator i ett reaktionsinert lösningsmedel vid en temperatur av 20-100°C; b) 4"-epi-9-deoxo-9a-metyl-9a-aza-9a-homoerytromycin-25 A-3'-N-oxid reduceras med väte över en ädelmetalkatalysator eller en Raney-nickelkatalysator i ett reaktionsinert lösningsmedel vid 20-100°C; eller c) 4"-deoxi-4"-oxo-9-deoxo-9a-metyl-9a-aza-9a-homo-erytromycin A hydreras över en ädelmetall- eller Raney-nickel- 30 katalysator i ett reaktionsinert lösningsmedel vid 20-100°C.
2. Förfarande enligt patentkravet 1, känneteck-n a t därav, att 4"-epi-9-deoxo-9a-aza-9a-homoerytromycin A framställs genom reduktion av 4”-epi-9a-aza-9a-homoerytro-mycin A med ett överskott av NaBH^ i ett protiskt lösnings- 35 medel vid 0-50°C.
FI834163A 1982-11-15 1983-11-14 Förfarande för framställning av 4 erytromycin A och dess farmaceutiskt godtagbara salter samt mellanprod ukterna använda i förfarandet. FI72980C (sv)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US44197982A 1982-11-15 1982-11-15
US44197982 1982-11-15

Publications (4)

Publication Number Publication Date
FI834163A0 FI834163A0 (fi) 1983-11-14
FI834163A FI834163A (fi) 1984-05-16
FI72980B true FI72980B (fi) 1987-04-30
FI72980C FI72980C (sv) 1987-08-10

Family

ID=23755068

Family Applications (1)

Application Number Title Priority Date Filing Date
FI834163A FI72980C (sv) 1982-11-15 1983-11-14 Förfarande för framställning av 4 erytromycin A och dess farmaceutiskt godtagbara salter samt mellanprod ukterna använda i förfarandet.

Country Status (26)

Country Link
EP (1) EP0109253B1 (sv)
JP (1) JPS59104398A (sv)
KR (1) KR850000968B1 (sv)
AT (1) ATE30237T1 (sv)
AU (1) AU544790B2 (sv)
CA (1) CA1239639A (sv)
CS (1) CS241069B2 (sv)
DD (1) DD216017A5 (sv)
DE (1) DE3374065D1 (sv)
DK (1) DK159322C (sv)
EG (1) EG16641A (sv)
ES (2) ES527249A0 (sv)
FI (1) FI72980C (sv)
GR (1) GR79425B (sv)
GT (1) GT198304062A (sv)
HU (1) HU193886B (sv)
IE (1) IE56234B1 (sv)
IL (1) IL70228A (sv)
NO (1) NO160262C (sv)
NZ (1) NZ206259A (sv)
PH (2) PH19293A (sv)
PL (2) PL142601B1 (sv)
PT (1) PT77645B (sv)
SU (1) SU1272996A3 (sv)
YU (2) YU43198B (sv)
ZA (1) ZA838460B (sv)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4465674A (en) * 1983-09-06 1984-08-14 Pfizer Inc. Azahomoerythromycin D derivative and intermediates therefor
EP0136831B1 (en) * 1983-09-06 1988-11-09 Pfizer Inc. Azahomoerythromycin b derivatives and intermediates thereof
WO1989000576A1 (en) * 1987-07-09 1989-01-26 Pfizer Inc. Azithromycin dihydrate
WO1989002271A1 (en) * 1987-09-10 1989-03-23 Pfizer Azithromycin and derivatives as antiprotozoal agents
JP2751385B2 (ja) * 1988-05-19 1998-05-18 大正製薬株式会社 エリスロマイシンａオキシム及びその塩の製造方法
US5075289A (en) * 1988-06-07 1991-12-24 Abbott Laboratories 9-r-azacyclic erythromycin antibiotics
SI8911498B (sl) * 1989-07-26 1998-10-31 Pliva Postopek za pripravo derivatov tilozina
US5912331A (en) * 1991-03-15 1999-06-15 Merck & Co., Inc. Process for the preparation of 9-deoxo-9(Z)-hydroxyiminoerythromycin A
CA2064634C (en) * 1991-04-04 1998-08-04 James V. Heck 9-deoxo-8a-aza-8a-homoerythromycin a derivatives modified at the 4"- and8a-positions
US5985844A (en) * 1992-03-26 1999-11-16 Merck & Co., Inc. Homoerythromycin A derivatives modified at the 4"-and 8A-positions
CA2064985A1 (en) * 1991-04-05 1992-10-06 Robert R. Wilkening 8a-aza-8a-homoertyhromycin cyclic lactams
CA2065222A1 (en) * 1991-04-09 1992-10-10 Robert R. Wilkening Process for the preparation of 8a-aza-8a-homoerythromycin cyclic iminoethers
US5189159A (en) * 1992-04-02 1993-02-23 Merck & Co., Inc. 8a-AZA-8a-homoerythromycin cyclic iminoethers
CA2065674A1 (en) * 1991-04-10 1992-10-11 Robert R. Wilkening 8a-aza-8a-homoerythromycin cyclic iminoethers
CA2065218A1 (en) * 1991-04-11 1992-10-12 Robert R. Wilkening Process for the preparation of 9-deoxo-8a-aza-8a-homoerythromycin a and its 8a-alkyl derivatives
EP0515141A1 (en) * 1991-05-20 1992-11-25 Merck & Co. Inc. Novel process for the preparation of 8A-aza-8A-homoerythromycin cyclic lactams
EP0549040A1 (en) * 1991-12-20 1993-06-30 Merck & Co. Inc. Methods of making 4" derivatives of 9-deoxo-8a-aza-8a-alkyl-8a-homoerythromycin A
US5215980A (en) * 1992-01-17 1993-06-01 Merck & Co., Inc. 10-AZA-9-deoxo-11-deoxy-erythromycin A and derivatives thereof
US5210235A (en) * 1992-08-26 1993-05-11 Merck & Co., Inc. Methods of elaborating erythromycin fragments into amine-containing fragments of azalide antibiotics
HRP930014A2 (en) * 1993-01-08 1994-08-31 Pliva Pharm & Chem Works 9-deoxo-9a-aza-11-deoxy-9a-homoeritromycin a 9a, 11-cyclic carbamates
US5332807A (en) * 1993-04-14 1994-07-26 Merck & Co., Inc. Process of producing 8A- and 9A-azalide antibiotics
PT758244E (pt) * 1994-05-06 2002-04-29 Pfizer Formas de dosagem libertacao controlada de azitromicina
PT102006B (pt) * 1997-05-19 2000-06-30 Hovione Sociedade Quimica S A Novo processo de preparacao de azitromicina
TW546302B (en) * 1998-05-08 2003-08-11 Biochemie Sa Improvements in macrolide production
EP1437360A3 (en) * 1998-08-19 2005-04-06 Pfizer Products Inc. C11 Carbamates of macrolide antibacterials
US6043227A (en) * 1998-08-19 2000-03-28 Pfizer Inc. C11 carbamates of macrolide antibacterials
DK1206476T3 (da) * 1999-08-24 2006-05-15 Abbott Lab 9a-azalider med antibakteriel virkning
US6764996B1 (en) 1999-08-24 2004-07-20 Abbott Laboratories 9a-azalides with antibacterial activity
AU2928701A (en) * 2000-01-04 2001-07-16 Teva Pharmaceutical Industries Ltd. Preparation method of azithromycin dihydrate
ATE306491T1 (de) 2000-08-23 2005-10-15 Wockhardt Ltd Verfahren zur herstellung von wasserfreiem azithromycin
US6852262B2 (en) 2002-05-09 2005-02-08 The Gillette Company Insert molding razor cartridges
JP2007513139A (ja) 2003-12-04 2007-05-24 ファイザー・プロダクツ・インク 安定性の改善した多粒子組成物
WO2005053652A1 (en) 2003-12-04 2005-06-16 Pfizer Products Inc. Multiparticulate crystalline drug compositions containing a poloxamer and a glyceride
AU2004294817B2 (en) 2003-12-04 2007-01-25 Pfizer Products Inc. Method for making pharmaceutical multiparticulates

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YU43116B (en) * 1979-04-02 1989-04-30 Pliva Pharm & Chem Works Process for preparing 11-aza-4-o-cladinosyl-6-o-desosaminyl-15-ethyl-7,13,14-trihydroxy-3,5,7,9,12,14-hexamethyl-oxacyclopentadecane-2-one(11-aza-10-deox
JPS5788193A (en) * 1980-11-21 1982-06-01 Pliva Pharm & Chem Works 11-aza-10-deoxo-10-dihydroerythromycin a, derivatives and manufacture
YU43006B (en) * 1981-03-06 1989-02-28 Pliva Pharm & Chem Works Process for preparing n-methyl-11-aza-10-deoxo-10-dihydro erythromycin and derivatives thereof
US4382085A (en) * 1982-03-01 1983-05-03 Pfizer Inc. 4"-Epi erythromycin A and derivatives thereof as useful antibacterial agents

Also Published As

Publication number Publication date
AU2130983A (en) 1984-05-24
NO834146L (no) 1984-05-16
PH19293A (en) 1986-03-04
DK159322C (da) 1991-02-25
PL143281B1 (en) 1988-01-30
IL70228A0 (en) 1984-02-29
PL142601B1 (en) 1987-11-30
YU43425B (en) 1989-06-30
EG16641A (en) 1990-08-30
ATE30237T1 (de) 1987-10-15
HU193886B (en) 1987-12-28
FI834163A (fi) 1984-05-16
FI72980C (sv) 1987-08-10
YU197285A (en) 1986-08-31
EP0109253A2 (en) 1984-05-23
NZ206259A (en) 1986-08-08
SU1272996A3 (ru) 1986-11-23
DD216017A5 (de) 1984-11-28
GR79425B (sv) 1984-10-22
PH21560A (en) 1987-12-11
ES8600327A1 (es) 1985-10-01
ES527249A0 (es) 1985-10-01
EP0109253B1 (en) 1987-10-14
KR840006673A (ko) 1984-12-01
GT198304062A (es) 1985-05-04
ES543638A0 (es) 1986-01-16
PT77645A (en) 1983-12-01
IL70228A (en) 1987-03-31
CA1239639A (en) 1988-07-26
EP0109253A3 (en) 1984-09-12
AU544790B2 (en) 1985-06-13
IE56234B1 (en) 1991-05-22
JPS59104398A (ja) 1984-06-16
FI834163A0 (fi) 1983-11-14
YU43198B (en) 1989-04-30
CS845583A2 (en) 1985-07-16
YU224383A (en) 1986-04-30
HUT35273A (en) 1985-06-28
DK518683A (da) 1984-05-16
PL244557A1 (en) 1985-03-26
ZA838460B (en) 1985-06-26
DK518683D0 (da) 1983-11-14
NO160262C (no) 1989-03-29
DK159322B (da) 1990-10-01
PT77645B (en) 1986-05-12
JPH0140038B2 (sv) 1989-08-24
NO160262B (no) 1988-12-19
DE3374065D1 (en) 1987-11-19
ES8604257A1 (es) 1986-01-16
PL250350A1 (en) 1985-04-24
KR850000968B1 (ko) 1985-07-02
IE832652L (en) 1984-05-15
CS241069B2 (en) 1986-03-13

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Owner name: PFIZER INC.