KR830005359A - Method for preparing cholesterol biosynthesis inhibitor - Google Patents

Method for preparing cholesterol biosynthesis inhibitor Download PDF

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Publication number
KR830005359A
KR830005359A KR1019810001067A KR810001067A KR830005359A KR 830005359 A KR830005359 A KR 830005359A KR 1019810001067 A KR1019810001067 A KR 1019810001067A KR 810001067 A KR810001067 A KR 810001067A KR 830005359 A KR830005359 A KR 830005359A
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KR
South Korea
Prior art keywords
mentioned
acylation
process according
halide
organic base
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KR1019810001067A
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Korean (ko)
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KR840001958B1 (en
Inventor
아이야 사또
아끼라 데라하라
요시요 쓰지따
Original Assignee
가와무라 요시부미
상꾜가부시끼가이샤
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Priority claimed from JP55041292A external-priority patent/JPH0692381B2/en
Application filed by 가와무라 요시부미, 상꾜가부시끼가이샤 filed Critical 가와무라 요시부미
Priority to KR1019810001067A priority Critical patent/KR840001958B1/en
Publication of KR830005359A publication Critical patent/KR830005359A/en
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Publication of KR840001958B1 publication Critical patent/KR840001958B1/en

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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/18—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin

Abstract

내용 없음No content

Description

콜레스테롤 생합성 억제제의 제조방법Method for preparing cholesterol biosynthesis inhibitor

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

제1도는 본 발명에 따른 MB-530A의 자외선 흡수 스펙트럼.1 is an ultraviolet absorption spectrum of MB-530A according to the present invention.

제2도는 본 발명에 따른 MB-530A의 적외선 흡수 스펙트럼.2 is an infrared absorption spectrum of MB-530A according to the present invention.

제3도는 본 발명에 따른 MB-530A의 NMR 스펙트럼.3 is an NMR spectrum of MB-530A according to the present invention.

Claims (11)

배양 배지중에서 균주 모나스쿠스의 MB-530A-생성 미생물의 배양과, 생성 배양 육즙으로부터 MB-530A를 분리시키는 것을 특징으로 하는 BM-530A 제조방법.A method for producing BM-530A, characterized by culturing MB-530A-producing microorganism of strain Monascus and separating MB-530A from the resulting culture broth. 언급한 미생물이 모나스쿠스 러버종 임을 특징으로 하는 특허청구범위 제1항 기재에 의한 방법.Method according to claim 1, characterized in that the microorganism mentioned is a Monascus rubber species. 언급한 미생물이 모노스쿠스 러버 SANK 15177 (FERM 4956, NRRL 12081)임을 특징으로 하는 특허청구범위 제2항 기재에 의한 방법.Method according to claim 2, characterized in that the microorganism mentioned is Monoscus rubber SANK 15177 (FERM 4956, NRRL 12081). R1및 R2중 하나 또는 양자가 수소원자를 나타내는 하기식(I)의 화합물을 아실화제로 아실화시키고, 생성물을 반응 혼합물로부터 분리시키는 것을 특징으로 하는 하기식(I)의 화합물의 제조방법.A process for preparing a compound of formula (I), wherein one or both of R 1 and R 2 represent a hydrogen atom, acylating with an acylating agent and separating the product from the reaction mixture. . (식중, R1및 R2중 하나는 수소원자를 나타내고 다른 하나는 아실기를 나타태거나; 또는 R1및 R2모두 아실기를 나타내고; R3는 수소원자 또는 메틸기를 나타낸다.)(Wherein one of R 1 and R 2 represents a hydrogen atom and the other represents an acyl group; or both R 1 and R 2 represent an acyl group; R 3 represents a hydrogen atom or a methyl group.) 언급한 아실화를 초산의 반응 유도체 또는 축합제의 존재하에서 초산으로 수행시키는 것을 특징으로 하는 특허청구범위 제4항 기재에 의한 방법.The process according to claim 4, wherein the acylation mentioned is carried out with acetic acid in the presence of a reactive derivative or a condensing agent of acetic acid. 언급한 아실화제가 무수산 또는 할라이드 이고 언급한 아실화를 유기염기의 존재하에서 수행시키는 것을 특징으로 하는 특허청구범위 제5항 기재에 의한 방법.The process according to claim 5, wherein the acylation agent mentioned is anhydrous acid or halide and the acylation mentioned is carried out in the presence of an organic base. 언급한 유기염기가 피리딘임을 특징으로 하는 특허청구 범위 제6항 기재에 의한 방법.Process according to claim 6, characterized in that the mentioned organic base is pyridine. 언급한 산화제가 무수산 또는 할라이드이고 언급한 아실화를 유기염기의 존재하에서 -20℃부터 0℃까지 수행시켜 탁월한 생성물인 모노에스테르를 생성시키는 것을 특징으로 하는 특허청구범위 제6항 기재에 의한 방법.The process according to claim 6, wherein the oxidant mentioned is anhydrous acid or halide and the mentioned acylation is carried out in the presence of an organic base from -20 ° C to 0 ° C to produce a monoester which is an excellent product. . 언급한 아실화제가 산할라이드와 언급한 식(I)의 화합물이 약 1당량 대 1당량임을 특징으로 하는 특허청구범위 제8항 기재에 의한 방법.The process according to claim 8, wherein the acylating agent mentioned is about 1 equivalent to 1 equivalent of the acid halide and the compound of formula (I) mentioned. 언급한 아실화제가 언급한 식(I)의 화합물 1당량 대 2당량 이하인 무수한 또는 할라이드이고, 언급한 아실화를 상기 실온에서 유기염기의 존재하에서 수행시키고, 탁월한 생성물인 디에스테르를 생성하는 것을 특징으로 하는 특허청구범위 제6항기재에 의한 방법.The acylating agent mentioned is a myriad or halide having up to 1 equivalent to 2 equivalents of the compound of formula (I) mentioned, characterized in that the mentioned acylation is carried out in the presence of an organic base at said room temperature, yielding an excellent product diester. Method according to claim 6 to claim. 언급한 아실화를 축합제의 존재하에서 초산으로 시키는 것을 특징으로 하는 특허청구범위 제4항 기재에 의한 방법.A process according to claim 4 characterized in that the acylation mentioned is brought to acetic acid in the presence of a condensing agent. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019810001067A 1980-03-31 1981-03-31 Process for preparing compounds having inhibitory activity against the biosyn-thesis of cholesterol KR840001958B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1019810001067A KR840001958B1 (en) 1980-03-31 1981-03-31 Process for preparing compounds having inhibitory activity against the biosyn-thesis of cholesterol

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP55041292A JPH0692381B2 (en) 1980-03-31 1980-03-31 MB-530A derivative
KR1019810001067A KR840001958B1 (en) 1980-03-31 1981-03-31 Process for preparing compounds having inhibitory activity against the biosyn-thesis of cholesterol

Publications (2)

Publication Number Publication Date
KR830005359A true KR830005359A (en) 1983-08-13
KR840001958B1 KR840001958B1 (en) 1984-10-26

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