KR850001747A - Method of Making Quinolone - Google Patents

Method of Making Quinolone Download PDF

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Publication number
KR850001747A
KR850001747A KR1019840004978A KR840004978A KR850001747A KR 850001747 A KR850001747 A KR 850001747A KR 1019840004978 A KR1019840004978 A KR 1019840004978A KR 840004978 A KR840004978 A KR 840004978A KR 850001747 A KR850001747 A KR 850001747A
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KR
South Korea
Prior art keywords
compound
general formula
formula
lower alkyl
give
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Application number
KR1019840004978A
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Korean (ko)
Inventor
빅토 데이비스 로이 (외 1)
Original Assignee
티이. 지이. 리챠드선, 데렉 노르만 에드먼드선
부츠 캄파니 피이 엘 시이
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Application filed by 티이. 지이. 리챠드선, 데렉 노르만 에드먼드선, 부츠 캄파니 피이 엘 시이 filed Critical 티이. 지이. 리챠드선, 데렉 노르만 에드먼드선
Publication of KR850001747A publication Critical patent/KR850001747A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/24—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in positions 2 and 4
    • C07D265/26—Two oxygen atoms, e.g. isatoic anhydride
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

내용 없음No content

Description

퀴놀론의 제조방법Method of Making Quinolone

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

Claims (1)

(a) 일반식(Ⅱ)의 화합물을 알킬화시켜서, R이 1-메틸 또는 2-저급알킬이고 임의의 2,3결합이 존재하는 일반식(Ⅰ)의 화합물을 수득하거나, (b) 일반식(Ⅴ)의 화합물을 트리(저급알킬) 오르토포르메이트 또는 포밀화제와 반응시켜서 임의의 2,3-결합이 존재하는 일반식(Ⅴ)의 화합물을 수득하거나, (c) 일반식(Ⅸ)의 화합물을 포름알데히드, 또는 아세탈, 티오아세탈 또는 이의 아미날과 반응시켜서, 임의의 2,3-결합이 존재하지 않는 일반식(X)의 화합물을 수득하거나, (d) 임의의 2,3-결합이 존재하지 않는 일반식(Ⅰ)의 화합물을 산화시켜서, 임의의 2,3-결합이 존재하지 않는 일반식(Ⅰ)의 화합물을 수득하거나, (e) 일반식(XI)화합물을 디아조화 시켜서 임의의 2,3-결합이 존재하지 않는 일반식(I)의 화합물을 수득하거나, (f) R2가 플루오로인 일반식(Ⅰ)의 화합물을 시안화이온, 저급알콕사이드이온 또는 일반식 HNR4R5의 아민과 반응시켜서, R2가 시아노, 저급알콕시 또는 -NR4R5인 일반식(I)의 화합물을 수득하거나, (g) R2가 히드록시인 일반식(I)의 화합물을 클로로디플루오로메탄과 반응시켜서 R2가 디플루오로메톡시인 일반식(Ⅰ)의 화합물을 수득하거나, (h) R2가 저급알킬티오 또는 페닐티오인 일반식(Ⅰ)의 화합물을 산화시켜서, R2가 저급알킬술피닐 또는 페닐술피닐인 일반식(Ⅰ)의 화합물을 수득함을 특징으로 하는 일반식(Ⅰ)퀴놀린 및 그의 약학적으로 허용되는 염의 제조방법.(a) alkylating a compound of formula (II) to yield a compound of formula (I) wherein R is 1-methyl or 2-lower alkyl and any 2,3 bond is present, or (b) Reacting the compound of (V) with a tri (lower alkyl) orthoformate or formylating agent to give a compound of formula (V) in which any 2,3-linkage is present, or (c) Reacting the compound with formaldehyde or acetal, thioacetal or an aminol thereof to give a compound of formula (X), wherein no 2,3-linkage is present, or (d) any 2,3-linkage The compound of general formula (I) which does not exist is oxidized to obtain a compound of general formula (I) which does not have any 2,3-bond, or (e) diazotizes the general formula (XI) compound. to give the compound of formula (I) is any of 2,3-bond is not present, or the compound of (f) of the general formula (ⅰ) as R 2 is fluoro Cyanide ion, lower alkoxide ion or by the general formula HNR 4 R 5 in the amine and the reaction, R 2 is cyano, lower alkoxy or -NR 4 R 5 a to give a compound represented by the general formula (I) or, (g) R 2 A compound of formula (I) wherein is hydroxy is reacted with chlorodifluoromethane to give a compound of formula (I) wherein R 2 is difluoromethoxy, or (h) R 2 is lower alkylthio or phenyl A compound of the general formula (I) quinoline and pharmaceutically thereof, wherein the compound of the general formula (I) is oxidized to obtain a compound of the general formula (I) wherein R 2 is lower alkylsulfinyl or phenylsulfinyl. Acceptable Methods of Making Salts. 상기식에서, 퀴놀론 환중에서 2와 3위치사이의 점선은 임의 결합을 나타내며,Wherein the dotted line between positions 2 and 3 in the quinolone ring represents an arbitrary bond, R은 수소, 1-메틸, 또는 2-저급알킬이고,R is hydrogen, 1-methyl, or 2-lower alkyl, R1은 저급알킬이며,R 1 is lower alkyl, R2는 수소, 할로, 저급알킬, 저급알콕시, 트리플루오로메틸, 시아노, 디플루오로메톡시, 저급알킬술피닐 페닐술피닐 또는 -NR4R5그룹 또는 이의 N-옥사이드이고, R4와 R5는 동일하거나 상이할 수 있으며 저급알킬이거나, 이들이 부착된 질소원자와 함께 피롤리디노, 피페리디노, 또는 모르폴리노라디칼을 형성하며, R3는 수소, 플루오로, 저급알킬 또는 저급알콕시이고, 단, R3가 저급알콕시일때는, R2가 저급알콕시 이외의 것이다.R 2 is hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, cyano, difluoromethoxy, lower alkylsulfinyl phenyl sulfinyl or -NR 4 R 5 group or a N- oxide, and R 4 R 5 may be the same or different and is lower alkyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, or morpholino radical, R 3 is hydrogen, fluoro, lower alkyl or lower alkoxy However, when R <3> is lower alkoxy, R <2> is other than lower alkoxy. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019840004978A 1983-08-20 1984-08-18 Method of Making Quinolone KR850001747A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB838322470A GB8322470D0 (en) 1983-08-20 1983-08-20 Therapeutic agents
GB8322470 1983-08-20

Publications (1)

Publication Number Publication Date
KR850001747A true KR850001747A (en) 1985-04-01

Family

ID=10547634

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019840004978A KR850001747A (en) 1983-08-20 1984-08-18 Method of Making Quinolone

Country Status (4)

Country Link
JP (1) JPS6058975A (en)
KR (1) KR850001747A (en)
GB (1) GB8322470D0 (en)
ZA (1) ZA846174B (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62202846U (en) * 1986-06-13 1987-12-24

Also Published As

Publication number Publication date
JPS6058975A (en) 1985-04-05
ZA846174B (en) 1985-03-27
GB8322470D0 (en) 1983-09-21

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