KR830006184A - 알콕시-아실 카르니틴의 제조방법 - Google Patents

알콕시-아실 카르니틴의 제조방법 Download PDF

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KR830006184A
KR830006184A KR1019810001703A KR810001703A KR830006184A KR 830006184 A KR830006184 A KR 830006184A KR 1019810001703 A KR1019810001703 A KR 1019810001703A KR 810001703 A KR810001703 A KR 810001703A KR 830006184 A KR830006184 A KR 830006184A
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South Korea
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acyl
carnitine
alkoxy
halogenated alkoxy
treatment
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KR1019810001703A
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KR850000628B1 (ko
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카아바아쟈아 크로오디이오
구아레시이마 에마
데 왯 파오로
오넬라틴티이 마리아
Original Assignee
피이에트로 아네시이
시구마-투우 인더스트리 화아마슈티히 리유니잇 에스. 피. 에이
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Publication of KR830006184A publication Critical patent/KR830006184A/ko
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Publication of KR850000628B1 publication Critical patent/KR850000628B1/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/16—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/221—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/22—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated the carbon skeleton being further substituted by oxygen atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음

Description

알콕시-아실 카르니틴의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 일반식(Ⅰ)
    할로겐화 알콕시-아실 카느니틴.
    위식에서 X-는 염소와 브롬중에서 선택된 할로겐 음이온이고 ;
    R는 4내지 6개의 탄소원자를 가진 알콕시 - 아실기이다;
  2. 상기 알콕시-아실 라티칼 R가 2-및 3-메톡시프로피오닐, 2- 및 3-에톡시프로피오닐, 프로폭시아세틸과 4-메톡시부티릴로 구성된 종류로 부터 선택된, 청구범위 1에 의거한 할로겐화 알콕시 - 아실-카르니틴.
  3. 광학적인 활성형의 청구범위 1 및 2에 의거한할로겐화 알콕시-아실 카느니틴.
  4. 라세미형의 청구범위 1 및 2에 의거한 할로겐화 알콕시-아실 카느니틴.
  5. 일반식(Ⅰ)
    할로겐화 알콕시-아실 카르니틴의 제조방법.
    위식에서 X-는 브로중에서 선택된 할로겐 음이온이고; R은, 다음과 같은 단계들을 포함하는 4내지 6개의 탄소원자를 가진 알콕시-아실기이다 : (a) 유기용매에 가용성인 카르니틴의 염을 유기용매에 용해시킨다 : (b) 이렇게하여 얻어진 용액에 R은 앞서 상술한 뜻과 같고 X는 염소와 브롬중에서 선택된 할로겐인 일반식 RX의 할로겐화 알콕시-아실을 첨가하고, 생성반응 혼합물을 실온화 40℃사이의 온도에서 2내지 16일동안 방치하여 알콕시-아실 카르니티의 대응염을 얻는다 ; (c) 단계 (b) 의 알콕시-아실-카르니틴의 염을 X- 의 형으로 활성화된 이온교환 수지로 상기염의 수용액을 처리하여 일반식(Ⅰ)의 할로겐화 알콕시-아실 카르니틴으로 전환시킨다.
  6. 상기 알콕시-아실 라디칼 R이 2- 및 3-메톡시프로피오닐, 2-및 에톡시프로피오닐, 프로폭시아세틸과 4-메톡시부틸리로 구성된 종류로부터 선택된 것인, 청구범위 5에 의거한 방법.
  7. 단계(a)의 카르니틴의 상기염이 과염소산 카르니틴이고 상기 유기용매가 아세토니트릴인 청구범위 5에 의거한 방법.
  8. 카르니틴의 상기염이 염산 카르니틴이고 상기 유기용매가 트리플루오로아세트산인 청구범위 5에 의거한 방법.
  9. 단계(b)에서 상기 반응 혼합물이 교반하여 방치되고 되풀이하여 반응의 기체 부산물의 제거하기 위해 처리되는 청구범위 5에 의거한 방법.
  10. 반응의 기체부산물을 제거하기 위한 상기의 처리가 상기반응 혼합물에 불어 넣는 것을 포함하는 청구범위 8과 9에 의거한 방법.
  11. 반응의 기체부산물을 제거하기 위한 상기의 처리가 상기반응 혼합물을 OH-형태로 활성화된 이은교환 수지로 처리하는 것을 포함하는 청구범위 8과 9에 의거한 방법.
  12. 청구범위 1에 의거한 할로겐화 알콕시-아실 카르니틴의 제조에서 중간 생성물로서의 과염소산 알콕시-아실 카르니틴.
  13. 일반식(Ⅰ)의 할로겐화 알콕시-아실 카르니틴의 치료에 효과적인 양과 약제로 사용가능한 부형제를 포함하는 심장병들의 치료를 위한 약제조성물.
  14. 일반식(Ⅰ)의 할로겐화 알콕시-아실 카르니틴의 치료에 효과적인 양과 약제로 사용가능한 부형제를 포함하는 과유지방 단백질혈증의 치료를 위한 약제조성물,
  15. 일반식(Ⅰ)의 할로겐화 알콕시-아실 카르니틴의 치료에 효과적인 양과 약제로 사용가능한 부형제를 포함하는 과유지질혈증의 치료를 위한 약제조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019810001703A 1980-05-30 1981-05-18 알콕시-아실 카트니틴의 제조방법 KR850000628B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT48854/80A IT1145371B (it) 1980-05-30 1980-05-30 Alcossi-acil carnitine procedimento per la loro preparazione e composizioni farmaceutiche che le contengono
IT48854A/80 1980-05-30

Publications (2)

Publication Number Publication Date
KR830006184A true KR830006184A (ko) 1983-09-20
KR850000628B1 KR850000628B1 (ko) 1985-05-06

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ID=11268803

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KR1019810001703A KR850000628B1 (ko) 1980-05-30 1981-05-18 알콕시-아실 카트니틴의 제조방법

Country Status (17)

Country Link
US (1) US4590209A (ko)
JP (1) JPS5724339A (ko)
KR (1) KR850000628B1 (ko)
AT (1) AT373231B (ko)
AU (1) AU540842B2 (ko)
BE (1) BE888984A (ko)
CA (1) CA1151208A (ko)
CH (1) CH649528A5 (ko)
DE (1) DE3120913A1 (ko)
ES (1) ES8203329A1 (ko)
FR (1) FR2483407A1 (ko)
GB (1) GB2077258B (ko)
IE (1) IE51447B1 (ko)
IL (1) IL62890A (ko)
IT (1) IT1145371B (ko)
NL (1) NL191367C (ko)
SE (1) SE454509B (ko)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1209564B (it) * 1984-06-29 1989-08-30 Magis Farmaceutici Derivati della l-carnitina o di l-acil carnitina.
IT1177874B (it) * 1984-07-04 1987-08-26 Sigma Tau Ind Farmaceuti Estere della acetil carnitina,procedimenti per la sua preparazione e composizioni farmaceutiche che lo contengono
IT1208753B (it) * 1986-07-02 1989-07-10 Sigma Tau Ind Farmaceuti L-amminoacil derivati della l-carnitina, procedimento per la loro preparazione e composizioni farmaceutiche ad attivita' epatoprotettrice che li contengono
IT1240799B (it) * 1990-03-15 1993-12-17 Sigma Tau Ind Farmaceuti Composizioni farmaceutiche contenenti 3-metiltiopropionil l-carnitina ad attivita' sul sistema cardiovascolare.

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS531812B2 (ko) * 1972-12-07 1978-01-23
US4032641A (en) * 1976-06-09 1977-06-28 Tanabe Seiyaku Co., Ltd. Nicotinoyl carnitine derivatives
AU518617B2 (en) * 1977-04-29 1981-10-08 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Therapeutic application of acetyl-d, 1-carnitine
IT1156741B (it) * 1978-05-15 1987-02-04 Sigma Tau Ind Farmaceuti Applicazione terapeutica della carnitina e di alcuni derivati acilati della carnitina nell'emodialisi
IT1156769B (it) * 1978-05-25 1987-02-04 Sigma Tau Ind Farmaceuti Applicazione terapeutica della carnitina e di altri acil derivati della carnitina
IT1156840B (it) * 1978-06-27 1987-02-04 Sigma Tau Ind Farmaceuti Acil derivati della carnitina
JPS5633054A (en) * 1979-08-29 1981-04-03 Matsushita Electric Ind Co Ltd Dehydrator
IT1145362B (it) * 1980-03-06 1986-11-05 Sigma Tau Ind Farmaceuti Classe di acil-derivati della carnitina procedimento per la loro preparazione e loro uso terapeutico

Also Published As

Publication number Publication date
IT8048854A0 (it) 1980-05-30
GB2077258B (en) 1984-01-11
ES502593A0 (es) 1982-04-01
CA1151208A (en) 1983-08-02
AU7088381A (en) 1981-12-03
ES8203329A1 (es) 1982-04-01
FR2483407B1 (ko) 1985-05-17
JPS5724339A (en) 1982-02-08
IE811097L (en) 1981-11-30
KR850000628B1 (ko) 1985-05-06
NL8102538A (nl) 1981-12-16
DE3120913A1 (de) 1982-04-01
NL191367B (nl) 1995-01-16
DE3120913C2 (ko) 1991-07-18
CH649528A5 (it) 1985-05-31
IL62890A (en) 1986-04-29
FR2483407A1 (fr) 1981-12-04
ATA222981A (de) 1983-05-15
IL62890A0 (en) 1981-07-31
AT373231B (de) 1983-12-27
SE454509B (sv) 1988-05-09
GB2077258A (en) 1981-12-16
AU540842B2 (en) 1984-12-06
JPH0320384B2 (ko) 1991-03-19
SE8103368L (sv) 1981-12-01
NL191367C (nl) 1995-06-16
US4590209A (en) 1986-05-20
IT1145371B (it) 1986-11-05
BE888984A (fr) 1981-09-16
IE51447B1 (en) 1986-12-24

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