KR830002704A - Method for preparing water-soluble cholesterol derivative - Google Patents

Method for preparing water-soluble cholesterol derivative Download PDF

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Publication number
KR830002704A
KR830002704A KR1019800002288A KR800002288A KR830002704A KR 830002704 A KR830002704 A KR 830002704A KR 1019800002288 A KR1019800002288 A KR 1019800002288A KR 800002288 A KR800002288 A KR 800002288A KR 830002704 A KR830002704 A KR 830002704A
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South Korea
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acid
organic dibasic
solvent
ketocholesterol
half ester
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KR1019800002288A
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Korean (ko)
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KR830002844B1 (en
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요시오 아라가와
아쓰유끼 다까나베
야히로 고우에무라
사또시 후나고시
다이스께 사또
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이시가끼 하찌로
가부시끼 가이샤 미도리 쥬우지
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Publication of KR830002844B1 publication Critical patent/KR830002844B1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음No content

Description

수용성 콜레스테롬 유도체의 제조방법Method for preparing water-soluble cholesteric derivative

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this content is publicly disclosed, the full text is not included.

Claims (22)

7-케토콜레스테롤을 제3급 아민의 존재하에서 하기 일반식(Ⅳ)로 표시되는 유기이염기산의 반응성 유도체와 반응시켜 에스테르화 반응시킴을 특징으로 하는 하기 일반식(Ⅰ)로 표시되는 7-케토콜레스테롤 유기이염기산 반에스테르의 제조방법.7-keto represented by the following general formula (I) characterized by reacting 7-ketocholesterol with a reactive derivative of an organic dibasic acid represented by the following general formula (IV) in the presence of a tertiary amine. Method for producing cholesterol organic dibasic half ester. (식들중에서, R1은 =0 또는 -OH기이고, R2는)C1∼C5알킬렌기 또는 페닐렌기임).(Wherein, R 1 =0 or -OH group, R 2 is a C 1 ~ C 5 alkylene group or phenylene group). 제3급 아민이 피리딘, 트리에틸아민 또는 디메틸아닐린임을 특징으로 하는 특허청구의 범위 제1항 기재의 방법.The method of claim 1, wherein the tertiary amine is pyridine, triethylamine or dimethylaniline. 유기이염기산이 호박산, 아디핀산, 글루타르산 또는 프탈산임을 특징으로 하는 특허청구의 범위 제1항 기재의 방법.The method of claim 1, wherein the organic dibasic acid is succinic acid, adipic acid, glutaric acid or phthalic acid. 유기이염기산의 반응성유도체가 이의 산무수물 또는 산할로겐화물임을 특징으로 하는 특허청구의 범위 제1항 기재의 방법.The method of claim 1, wherein the reactive derivative of the organic dibasic acid is an acid anhydride or an acid halide thereof. 유기 이염기산의 반응성 유도체를 7-케토콜레스테롤 1몰에 대하여 1.0 내지 3.0몰 양으로 사용합을 특징으로 하는 특허청구의 범위 제1항 기재의 방법.The method according to claim 1, characterized in that a reactive derivative of an organic dibasic acid is used in an amount of 1.0 to 3.0 moles per 1 mole of 7-ketocholesterol. 반응온도 범위가 60 내지 150℃임을 특징으로 하는 특허청구의 범위 제1항 기재의 방법.Method of claim 1, characterized in that the reaction temperature range is 60 to 150°C. 콜레스테롤을 상응하는 유기이염기산 반응성유도체와 반응시켜 얻어지는 콜레스테롤 유기이염기산 반에스테르를 용매중에서 크롬산화제에 의해 산화시킴을 특징으로 하는 7-케토콜레스테롤 유기이염기산 반에스테르의 제조방법.A method for producing a 7-ketocholesterol organic dibasic half ester, characterized in that the cholesterol organic dibasic half ester obtained by reacting cholesterol with a corresponding organic dibasic acid reactive derivative is oxidized in a solvent by a chromium oxidizing agent. 유기 이염기산이 호박산, 아디핀산, 글루타르산 또는 프탈산임을 특징으로 하는 특허청구의 범위 제7항 기재의 방법.Method of claim 7 characterized in that the organic dibasic acid is succinic acid, adipic acid, glutaric acid or phthalic acid. 반응성유도체가 이의 산무수물 또는 산할로겐화물임을 특징으로 하는 특허청구의 범위 제7항 기재의 방법.The method of claim 7 characterized in that the reactive derivative is an acid anhydride or an acid halide thereof. 크롬산기산화제가 무수크롬산, t-부틸크롬산에스테르, 중크롬칼륨 또는 중크롬산나트륨임을 특징으로 하는 특허청구의 범위 제7항 기재의 방법.The method according to claim 7 wherein the chromic acid oxidizing agent is chromic anhydride, t-butylchromate ester, potassium bichromate or sodium dichromate. 크롬산기 산화제를 콜레스테롤 유기 이염기산 반에스테르 1몰에 대하여 3.0 내지 15.0몰 양으로 사용합을 특징으로 하는 특허청구의 범위 제7항 기재의 방법.The method according to claim 7, characterized in that a chromic acid oxidizing agent is used in an amount of 3.0 to 15.0 moles per 1 mole of cholesterol organic dibasic acid ester. 용매가 초산, 프로피온산, 초산무수물 또는 이들 중 어느 하나를 합유하여 4염화탄소, 클로로포름, 염화메틸렌 및 벤젠 중에서 선택되는 용매임을 특징으로 하는 특허청구의 범위 제7항의 기재의 방법.The method according to claim 7, wherein the solvent is a solvent selected from carbon tetrachloride, chloroform, methylene chloride and benzene by mixing acetic acid, propionic acid, acetic anhydride or any one of them. 반응 온도 범위가 40 내지 70℃ 또는 사용하는 용매의 비점임을 특징으로 하는 특허청구의 범위 제7항 기재의 방법.The method of claim 7 characterized in that the reaction temperature range is 40 to 70°C or the boiling point of the solvent used. 7-케토콜레스테롤 유기이염기산 반에스테르 또는 이의 염을 용매 중에서 착금속수소화물에 의해 환원시킴을 특징으로 하는 7-히드록시콜레스테롤 유기이염기산 반에스테르의 제조방법.A method for producing a 7-hydroxycholesterol organic dibasic half ester, characterized in that 7-ketocholesterol organic dibasic half ester or a salt thereof is reduced in a solvent by a complex metal hydride. 유기 이염기산이 호박산, 아디핀산, 글루타르산 또는 프탈산 임을 특징으로 하는 특허청구의 범위 제14항 기재의 방법.The method according to claim 14, wherein the organic dibasic acid is succinic acid, adipic acid, glutaric acid or phthalic acid. 착금속 수소화물을 7-케토콜레스테롤 유기이염기산 반에스테르 1몰에 대하여 1.0 내지 10.0몰 양으로 사용합을 특징으로 하는 특허청구의 범위 제14항 기재의 방법.The method according to claim 14, characterized in that the complex metal hydride is used in an amount of 1.0 to 10.0 mol with respect to 1 mol of the 7-ketocholesterol organic dibasic half ester. 착금속 수소화물이 수소화붕소나트륨, 수소화붕소칼륨 또는 수소화알루미늄리튬임을 특징으로 하는 특허청구의 범위 제16항 기재의 방법.The method of claim 16 wherein the complex metal hydride is sodium borohydride, potassium borohydride or lithium aluminum hydride. 용매가 물, 메탄올, 에탄올, 디옥산 또는 테트라히드로푸란 임을 특징으로 하는 특허청구의 범위 제14항 기재의 방법.The method of claim 14, wherein the solvent is water, methanol, ethanol, dioxane or tetrahydrofuran. 반응 온도범위가 0 내지 실온임을 특징으로 하는 특허청구의 범위 제14항 기재의 방법.Method according to claim 14, characterized in that the reaction temperature range is from 0 to room temperature. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: Disclosure is based on the original application.
KR1019800002288A 1980-06-11 1980-06-11 Method for preparing a water soluble cholesterol derivative KR830002844B1 (en)

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KR830002704A true KR830002704A (en) 1983-05-30
KR830002844B1 KR830002844B1 (en) 1983-12-27

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