HK59293A - Preparing clindamycin and analogues thereof - Google Patents

Preparing clindamycin and analogues thereof Download PDF

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Publication number
HK59293A
HK59293A HK592/93A HK59293A HK59293A HK 59293 A HK59293 A HK 59293A HK 592/93 A HK592/93 A HK 592/93A HK 59293 A HK59293 A HK 59293A HK 59293 A HK59293 A HK 59293A
Authority
HK
Hong Kong
Prior art keywords
adduct
chloride
lincomycin
amide
chloromethylene
Prior art date
Application number
HK592/93A
Other languages
German (de)
English (en)
Inventor
Douglas Alan Livingston
Original Assignee
The Upjohn Company
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 The Upjohn Company filed Critical The Upjohn Company
Publication of HK59293A publication Critical patent/HK59293A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/06—Heterocyclic 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 halogen atoms or nitro radicals
    • C07D295/067—Heterocyclic 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 halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/14—Acyclic radicals, not substituted by cyclic structures attached to a sulfur, selenium or tellurium atom of a saccharide radical
    • C07H15/16—Lincomycin; Derivatives thereof

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Cephalosporin Compounds (AREA)

Claims (10)

1. Procédé de préparation de 7-halogéno-désoxylincomycine ou d'un de ses analogues, qui consiste
(a) à faire réagir un composé de départ choisi entre la lincomycine et un de ses analogues, avec un halogénure d'amide répondant à la formule dans laquelle chaque groupe Hal représente le brome ou le chlore, et R, et R2 sont choisis indépendamment entre un groupe aryle et un groupe alkyle en C1-8, ou bien NR1R2 représente un groupe morpholino ou un noyau hétérocyclique contenant dans le cycle 4 à 8 atomes choisis entre le carbone et l'azote, pour former un produit d'addition;
(b) à chauffer le produit d'addition pour former un 7-halogéno-7-désoxy-(produit d'addition); et
(c) à hydrolyser le 7-halogéno-7-désoxy(produit d'addition) avec une solution aqeueuse de base.
2. Procédé suivant la revendication 1, dans lequel l'halogénure d'amide est un chlorure d'amide.
3. Procédé suivant la revendication 1, dans lequel le chlorure d'amide est choisi entre le chlorure de N-(chlorométhylène)-N-méthylméthanaminium, le chlorure de N-(chlorométhylène) pipéridinium, le chlorure de N-(chlorométhylène) morpholinium et le chlorure de N-(chlorométhylène) pyrrolidinium.
4. Procédé suivant l'une quelconque des revendications précédentes, destiné à la préparation de clindamycine, dans lequel le composé de départ est la lincomycine.
5. Procédé suivant la revendication 3, dans lequel le chlorure d'amide est le chlorure de N-(chlorométhylène)-N-méthylméthanaminium et le composé de départ est le chlorhydrate de lincomycine hydraté.
6. Procédé suivant la revendication 3, dans lequel le chlorure d'amide est le chlorure de N-(chlorométhylène) pipéridinium et le composé de départ est le chlorhydrate de lincomycine hydraté.
7. Procédé suivant la revendication 5 ou 6, destiné à la préparation d'hydrate de chlorhydrate de clindamycine, dans lequel le composé de départ est l'hydrate de chlorhydrate de lincomycine.
8. Produit d'addition de lincomycine ou d'un de ses analogues et d'un halogénure d'amide suivant l'une quelconque des revendications 1 à 3.
9. Produit d'addition de lincomycine et d'un halogénure d'amide suivant l'une quelconque des revendications 1 à 3.
10. Produit d'addition d'hydrate de chlorhydrate de lincomycine et d'un chlorure d'amide suivant la revendication 5 ou la revendication 6.
HK592/93A 1984-05-15 1993-06-17 Preparing clindamycin and analogues thereof HK59293A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US06/610,364 US4568741A (en) 1984-05-15 1984-05-15 Synthesis of 7-halo-7-deoxylincomycins

Publications (1)

Publication Number Publication Date
HK59293A true HK59293A (en) 1993-06-25

Family

ID=24444721

Family Applications (1)

Application Number Title Priority Date Filing Date
HK592/93A HK59293A (en) 1984-05-15 1993-06-17 Preparing clindamycin and analogues thereof

Country Status (18)

Country Link
US (1) US4568741A (fr)
EP (1) EP0161794B1 (fr)
JP (1) JPS60260591A (fr)
KR (1) KR910002224B1 (fr)
AT (1) ATE54150T1 (fr)
AU (1) AU574453B2 (fr)
CA (1) CA1229592A (fr)
DE (1) DE3578425D1 (fr)
DK (1) DK166390C (fr)
ES (1) ES8606877A1 (fr)
FI (1) FI78108C (fr)
GR (1) GR851150B (fr)
HK (1) HK59293A (fr)
HU (1) HU196820B (fr)
IL (2) IL74971A (fr)
MX (1) MX163480B (fr)
PT (1) PT80463B (fr)
ZA (1) ZA852592B (fr)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1004002B (zh) * 1984-11-29 1989-04-26 厄普约翰公司 制备7-卤-7-去氧林可霉素及其类似化合物的改进方法
TW282399B (fr) * 1990-05-25 1996-08-01 Takeda Pharm Industry Co Ltd
DE4039750A1 (de) * 1990-12-13 1992-06-17 Basf Ag Verfahren zur entfernung von phosgen aus abgasen
JP3202960B2 (ja) * 1998-02-17 2001-08-27 大塚化学株式会社 ハロゲン化剤及び水酸基のハロゲン化方法
US6565882B2 (en) * 2000-02-24 2003-05-20 Advancis Pharmaceutical Corp Antibiotic composition with inhibitor
US6544555B2 (en) * 2000-02-24 2003-04-08 Advancis Pharmaceutical Corp. Antibiotic product, use and formulation thereof
US20020068078A1 (en) * 2000-10-13 2002-06-06 Rudnic Edward M. Antifungal product, use and formulation thereof
US6541014B2 (en) * 2000-10-13 2003-04-01 Advancis Pharmaceutical Corp. Antiviral product, use and formulation thereof
US20020197314A1 (en) * 2001-02-23 2002-12-26 Rudnic Edward M. Anti-fungal composition
US20030073648A1 (en) * 2001-08-28 2003-04-17 Chao Robert S. Crystaline clindamycin free base
US7199105B2 (en) * 2002-08-15 2007-04-03 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antibacterial activity
US7164011B2 (en) * 2002-08-15 2007-01-16 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antibacterial activity
GB0222522D0 (en) 2002-09-27 2002-11-06 Controlled Therapeutics Sct Water-swellable polymers
ES2637956T3 (es) 2003-01-24 2017-10-18 Stiefel Research Australia Pty Ltd Espuma farmacéutica
US7256177B2 (en) 2003-06-17 2007-08-14 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antibacterial activity
US7199106B2 (en) 2003-06-17 2007-04-03 Vicuron Pharmaceuticals, Inc. Lincomycin derivatives possessing antimicrobial activity
AU2004258949B2 (en) * 2003-07-21 2011-02-10 Shionogi, Inc. Antibiotic product, use and formulation thereof
JP2006528185A (ja) * 2003-07-21 2006-12-14 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法及び作成方法
AU2004258953B2 (en) * 2003-07-21 2011-02-10 Shionogi, Inc. Antibiotic product, use and formulation thereof
CA2535177A1 (fr) 2003-08-11 2005-02-24 Advancis Pharmaceutical Corporation Pastille robuste
US8062672B2 (en) * 2003-08-12 2011-11-22 Shionogi Inc. Antibiotic product, use and formulation thereof
AU2004270170B2 (en) * 2003-08-29 2011-01-27 Shionogi, Inc. Antibiotic product, use and formulation thereof
CA2538064C (fr) * 2003-09-15 2013-12-17 Advancis Pharmaceutical Corporation Antibiotique, son utilisation et sa formulation
AU2004308419B2 (en) * 2003-12-24 2011-06-02 Victory Pharma, Inc. Enhanced absorption of modified release dosage forms
US7361743B2 (en) * 2004-02-11 2008-04-22 Pfizer Inc Lincomycin derivatives possessing antibacterial activity
CA2572292A1 (fr) * 2004-07-02 2006-02-09 Advancis Pharmaceutical Corporation Comprime pour distribution par impulsion
GB0417401D0 (en) * 2004-08-05 2004-09-08 Controlled Therapeutics Sct Stabilised prostaglandin composition
US8357394B2 (en) 2005-12-08 2013-01-22 Shionogi Inc. Compositions and methods for improved efficacy of penicillin-type antibiotics
US8778924B2 (en) * 2006-12-04 2014-07-15 Shionogi Inc. Modified release amoxicillin products
EP2010133B1 (fr) 2006-03-31 2016-05-04 Stiefel Research Australia Pty Ltd Gel de suspension moussant
US8299052B2 (en) * 2006-05-05 2012-10-30 Shionogi Inc. Pharmaceutical compositions and methods for improved bacterial eradication
GB0613333D0 (en) 2006-07-05 2006-08-16 Controlled Therapeutics Sct Hydrophilic polyurethane compositions
GB0613638D0 (en) 2006-07-08 2006-08-16 Controlled Therapeutics Sct Polyurethane elastomers
GB0620685D0 (en) * 2006-10-18 2006-11-29 Controlled Therapeutics Sct Bioresorbable polymers
CN101205245B (zh) * 2007-12-06 2011-04-06 河南天方药业股份有限公司 盐酸克林霉素的制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3496163A (en) * 1965-02-08 1970-02-17 Upjohn Co 7-halo-7-deoxylincomycins and process for preparing the same
US3435025A (en) * 1966-03-18 1969-03-25 Upjohn Co 7-deoxylincomycin and analogs and isomers thereof and process for making the same
US3475407A (en) * 1967-12-22 1969-10-28 Upjohn Co Process for preparing 7(r)- and 7(s)-halolincomycins
US3509127A (en) * 1968-04-30 1970-04-28 Upjohn Co Isologs of lincomycins and process for preparing the same
US3574186A (en) * 1969-10-08 1971-04-06 Upjohn Co Process for making 7-chloro-7-deoxylincomycin and related compounds and novel intermediates produced therein
US3714141A (en) * 1970-05-26 1973-01-30 Upjohn Co Process for making 7-halolincomycins
CA1138443A (fr) * 1979-03-09 1982-12-28 Tate & Lyle Patent Holdings Limited Methode de preparation de chloro-desoxysucres
CN1004002B (zh) * 1984-11-29 1989-04-26 厄普约翰公司 制备7-卤-7-去氧林可霉素及其类似化合物的改进方法

Also Published As

Publication number Publication date
IL74971A (en) 1991-07-18
KR910002224B1 (ko) 1991-04-08
ES8606877A1 (es) 1986-05-16
FI78108C (fi) 1989-06-12
HU196820B (en) 1989-01-30
FI851941A0 (fi) 1985-05-15
IL74971A0 (en) 1985-08-30
DE3578425D1 (de) 1990-08-02
EP0161794A3 (en) 1987-07-29
KR850008349A (ko) 1985-12-16
MX163480B (es) 1992-05-19
AU4095085A (en) 1985-11-21
GR851150B (fr) 1985-11-25
AU574453B2 (en) 1988-07-07
HUT40805A (en) 1987-02-27
DK196185A (da) 1985-11-16
JPS60260591A (ja) 1985-12-23
ATE54150T1 (de) 1990-07-15
DK166390C (da) 1993-09-27
PT80463B (pt) 1987-08-19
FI851941L (fi) 1985-11-16
ZA852592B (en) 1985-11-27
JPH0533711B2 (fr) 1993-05-20
DK166390B (da) 1993-05-10
EP0161794B1 (fr) 1990-06-27
US4568741A (en) 1986-02-04
CA1229592A (fr) 1987-11-24
IL75175A0 (en) 1985-09-29
FI78108B (fi) 1989-02-28
ES542940A0 (es) 1986-05-16
PT80463A (en) 1985-06-01
EP0161794A2 (fr) 1985-11-21
DK196185D0 (da) 1985-05-01

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Effective date: 20050408