KR890002164A - Macrolide Compound - Google Patents

Macrolide Compound Download PDF

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KR890002164A
KR890002164A KR1019870006809A KR870006809A KR890002164A KR 890002164 A KR890002164 A KR 890002164A KR 1019870006809 A KR1019870006809 A KR 1019870006809A KR 870006809 A KR870006809 A KR 870006809A KR 890002164 A KR890002164 A KR 890002164A
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South Korea
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group
compound
hydroxyl group
formula
compound according
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KR1019870006809A
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Korean (ko)
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KR950010078B1 (en
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알 서더랜드 데렉
브이 제이 램세이 마이클
피 틸레이 에드워드
제트 페레이라 오스와이
비 와드 존
포터 네일
엠 노블 해젤
에이 플레톤 리챠드
노블 데이비드
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배리 에이 뉴샘
글락소 그륨 리미티드
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/01Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing oxygen
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/90Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/18Preparation 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
    • C12P17/181Heterocyclic compounds containing oxygen atoms as the only ring heteroatoms in the condensed system, e.g. Salinomycin, Septamycin

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  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Dentistry (AREA)
  • Environmental Sciences (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

내용없음No content

Description

마크롤라이드 화합물Macrolide Compound

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (15)

하기 일반식(Ⅰ)로 표시되는 화합물 및 그 염류.The compound represented by the following general formula (I), and its salt. 상기 식중 R1은 메틸, 에틸 또는 이소프로필기이고, R2는 수소 원자, C1-e알킬기 또는 C3-e알케닐기이되, =NOR2기는 E-배열이고, OR3은 히드록실기 또는 최대를 25개의 탄소 원자를 갖는 치환 히드록기이다.Wherein R 1 is a methyl, ethyl or isopropyl group, R 2 is a hydrogen atom, a C 1-e alkyl group or a C 3-e alkenyl group, wherein = NOR 2 group is an E-array and OR 3 is a hydroxyl group Or a substituted hydroxyl group having up to 25 carbon atoms. 제1항에 있어서, OR3이 메톡시카르보닐옥시, 아세톡시, 메톡시 또는 히드록실기인 화합물.The compound of claim 1, wherein OR 3 is a methoxycarbonyloxy, acetoxy, methoxy, or hydroxyl group. 제1항에 있어서, OR3이 히드록실기인 화합물.The compound of claim 1, wherein OR 3 is a hydroxyl group. 상기 전 항 중 어느 하나의 항에 있어서, R1이 이소프로필기인 화합물.The compound according to any one of the preceding claims, wherein R 1 is an isopropyl group. 상기 전 항 중 어느 하나의 항에 있어서, R2가 메틸기인 화합물.The compound according to any one of the preceding claims, wherein R 2 is a methyl group. 제1항에 있어서, R1이 이소프로필기이고, R2가 메틸기이고, OR3이 히드록시, 아세톡시 또는 메톡시카르보닐옥시기인 화합물.A compound according to claim 1, wherein R 1 is an isopropyl group, R 2 is a methyl group, and OR 3 is a hydroxy, acetoxy or methoxycarbonyloxy group. 제1항에 있어서, R1이 이소프로필기이고, R2가 메틸기이고, OR3이 히드록실기인 화합물.The compound of claim 1, wherein R 1 is an isopropyl group, R 2 is a methyl group, and OR 3 is a hydroxyl group. 제1항에 있어서, R1이 메틸기이고, R2가 메틸기이고, OR3가 메톡시기이거나, R1이 에틸기이고, R2가 메틸기이고, OR3이 히드록실기인 화합물.The compound according to claim 1, wherein R 1 is a methyl group, R 2 is a methyl group, OR 3 is a methoxy group, R 1 is an ethyl group, R 2 is a methyl group, and OR 3 is a hydroxyl group. 제1항에 의한 화합물 중 적어도 하나의 화합물 유효량을 1개 이상의 담체 및(또는) 부형제와 함께 함유하는 인체 의약품용 조성물.A pharmaceutical composition for human medicine containing an effective amount of at least one compound of the compound according to claim 1 together with one or more carriers and / or excipients. 제1항에 의한 화합물 중 적어도 하나의 화합물 유효량을 1개 이상의 담체 및(또는) 부형제와 함께 함유하는 수의 약품용 조성물.A veterinary pharmaceutical composition containing an effective amount of at least one compound of the compound according to claim 1 together with one or more carriers and / or excipients. 제1항에 의한 화합물 중 적어도 하나의 화합물 유효량을 1개 이상의 담체 및(또는) 부형제와 함께 함유하는 해충 억제 조성물.A pest control composition comprising an effective amount of at least one compound of the compound according to claim 1 together with one or more carriers and / or excipients. 제9항 내지 제11항 중 어느 하나의 항에 있어서, 제7항에 의한 유효량을 1개 이상의 담체 및(또는)부형제와 함께 함유하는 조성물.The composition according to any one of claims 9 to 11, containing an effective amount according to claim 7 together with one or more carriers and / or excipients. 식물 또는 기타 초목에, 또는 해충 그자체에, 또는 그의 소재지에 제1항에 의한 화합물 중 1개 이상의 화합물 유효량을 투여하는 것으로되는, 농업, 원예 또는 임업, 또는 창고, 건물 또는 기타 공공 장소 또는 해충이 있는 장소에서의 해충 박멸 방법.Agriculture, horticulture or forestry, or warehouse, building, or other public place or pest, which comprises administering to a plant or other vegetation, or to a pest itself, or to its location an effective amount of at least one compound of the compound according to claim 1 How to exterminate pests in the same place. 제13항에 있어서, 상기 해충이 곤충, 진드기 또는 선충류 해충인 방법.The method of claim 13, wherein the pest is an insect, mite or nematode pest. (A) 하기 일반식(Ⅱ)의 화합물을 시약 H2NOR2(여기서, R2는 제1항에서 정의한 바와 같음) 또는 그 염과 반응시킨 후, 필요에 따라서 생성된 OR3이 보호된 히드록실기인 일반식(Ⅰ)화합물의 보호기를 제거하거나, (B) R2가 C1-e알킬또는 C3-e알케닐이고, OR3이 치환히드록실기인 대응하는 일반식(Ⅰ)의 화합물을 히드록실기를 치환 히드록실기로 전환시키는 시약과 반응시키거나, (C) R2가 C1-e알킬는 C3-e알케닐기인 일반식(Ⅰ)화합물의 제조의 경우에는, R2가 수소 원자이고, OR3이 치환 히드록실기인 일반식(Ⅰ)의 화합물을 에테르화제 R2Y(여기에서, R2는 C1-8알킬 또는 C3-8알케닐기이고, Y이탈기임)와 반응시킨 후, 필요에 따라서 OR2이 보호된 히드록실기인 일반식(Ⅰ)화합물의 보호기를 제거하거나, (D) OR3이 히드록실기인 일반식(Ⅰ)화합물의 제조의 경우에는, 하기 일반식(Ⅲ)의 화합물을 환원시키거나, (E) OR3이 히드록실기인 일반식(Ⅰ)화합물의 제조의 경우에는, OR3이 보호된 히드록실기인 대응하는 일반식(Ⅰ)화합물의 보호기를 제거하거나, 또는 (F) 일반식(Ⅰ)의 산의 염을 제조하는 경우에는, 상기 산을 염기로 처리하거나, 한 염을 이온 교환에 의해 또 다른 염으로 전환시키는 것으로 되는, 제1항에 의한 화합물의 제조방법.(A) reacting a compound of formula (II) below with reagent H 2 NOR 2 (wherein R 2 is as defined in claim 1) or a salt thereof, if necessary, protecting the resulting OR 3 The protecting group of the compound of formula (I), which is a hydroxyl group, or (B) R 2 is C 1-e alkyl or C 3-e alkenyl, and OR 3 is a substituted hydroxyl group, Or a compound of formula (I) in which R 2 is C 1-e alkyl is a C 3-e alkenyl group, or is reacted with a reagent that converts a hydroxyl group to a substituted hydroxyl group. A compound of formula (I) wherein R 2 is a hydrogen atom and OR 3 is a substituted hydroxyl group is substituted with an etherification agent R 2 Y (wherein R 2 is a C 1-8 alkyl or C 3-8 alkenyl group, Y after reaction with the leaving group), removing the protective group of the general formula (ⅰ) compound, oR 2 is a protected hydroxyl group, if necessary, or, (D) oR 3 are of formula (ⅰ) compound a hydroxyl group When Joe, to let the reduction of a compound of formula (Ⅲ), or, (E) OR 3 is hydroxyl group in the general formula (Ⅰ) in the case of producing a compound, OR 3 a corresponding of a protected hydroxyl group When the protecting group of the compound of formula (I) is removed or (F) a salt of the acid of formula (I) is prepared, the acid is treated with a base or one salt is converted to another salt by ion exchange. The method for producing a compound according to claim 1, which is to be converted. 상기 식중, R1, R2및 OR3은 제1항에서 정의한 바와 같다.Wherein R 1 , R 2 and OR 3 are as defined in claim 1. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019870006809A 1986-06-06 1987-07-01 Macrolide compounds KR950010078B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1019870006809A KR950010078B1 (en) 1986-06-06 1987-07-01 Macrolide compounds

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Application Number Priority Date Filing Date Title
GB8613790 1986-06-06
GB8625854 1986-10-29
GB8708423 1987-04-08
KR1019870006809A KR950010078B1 (en) 1986-06-06 1987-07-01 Macrolide compounds

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KR890002164A true KR890002164A (en) 1989-04-08
KR950010078B1 KR950010078B1 (en) 1995-09-06

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