KR890005099A - 결정상 항생제 중간물질 - Google Patents

결정상 항생제 중간물질 Download PDF

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Publication number
KR890005099A
KR890005099A KR1019880011519A KR880011519A KR890005099A KR 890005099 A KR890005099 A KR 890005099A KR 1019880011519 A KR1019880011519 A KR 1019880011519A KR 880011519 A KR880011519 A KR 880011519A KR 890005099 A KR890005099 A KR 890005099A
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KR
South Korea
Prior art keywords
hydroxy
crystalline
alkyl
acetic acid
solvate
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KR1019880011519A
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English (en)
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KR960015966B1 (ko
Inventor
파울 가드너 존
Original Assignee
메리 앤 터커
일라이 릴리 앤드 캄파니
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Publication of KR890005099A publication Critical patent/KR890005099A/ko
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Publication of KR960015966B1 publication Critical patent/KR960015966B1/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D463/00—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D463/10—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
    • C07D463/14—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hetero atoms directly attached in position 7
    • C07D463/16—Nitrogen atoms
    • C07D463/18—Nitrogen atoms further acylated by radicals derived from carboxylic acids or by nitrogen or sulfur analogues thereof
    • C07D463/20—Nitrogen atoms further acylated by radicals derived from carboxylic acids or by nitrogen or sulfur analogues thereof with the acylating radicals further substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Abstract

내용 없음

Description

결정상 항생제 중간물질
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는, 3-하이드록시-1-카바(데티아)-3-세펨 에스테르의 모노-아세트산 용매화물의 X-선 분말회절 양상을 컴퓨터-재생 플롯으로 도시한 것이다.
제2도는 결정상 p-니트로벨질 7β-펜옥시아세틸아미노-3-하이드록시-1-카바(데티아)-3-세펨-4-카복실레이트의 X-선 분말 회절 양상을 컴퓨터-재생 플롯으로 도시한 것이다.

Claims (7)

  1. 결정상의 구조식(1)의 화합물.
    (1)
  2. 결정상의 구조식(2)의 아세트산 용매화물
    (2)
  3. 약 15℃ 내지 약 30℃의 온도에서 디메틸 포롬아미드 또는 디메틸아세트아미드중의 3-하이드록시 P-니트로벤질 에스테르의 용액을 카복실산 RCOOH 또는 설폰산 R1SO3H(여기에서, R은 수소, C1-C8알킬, 할로겐, 카복시, 히이드록시 또는 C1-C4알콕시로 치환된 C1-C8알킬, C2-C8알케닐, 또는 할로겐, 카복시, 하이드록시 또는 C1-C4알콕시로 치환된 C2-C8알케닐이고, R1은 C1-C4알킬, 페닐, 또는 C1-C4알킬, C1-C4알콕시, 할로겐 또는 하이드록시로부터 선택된 동일하거나 상이한 그룹 1 또는 2개에 의해 치환된 페닐이다)와 혼합하고, R이 메틸인 경우 결정상 아세트산 용매화물을 분리하거나, R이 메틸이 아니거나 R1SO3H가 혼합되는 경우, 비-용매화된 결정상 3-하이드록시 P-니트로벤질 에스테르를 분리함을 특징으로 하여, 결정상 P-니트로벤질 7β-펜옥시아세틸-3-하이드록시-1-카바(데티아)-3-세펨-4-카복실레이트 또는 이의 결정상 모노-아세트산 용매화물을 제조하는 방법.
  4. 제3항에 있어서, 디메틸포롬아미드 또는 디메틸아세트아미드중의 3-하이드록시 에스테르의 농도가 약50mg/ml 내지 약 300mg/ml인 방법.
  5. 제4항에 있어서, 용매가 디메틸포륨아미드인 방법.
  6. 제5항에 있어서, 포롬산을 혼합하고 결정상 모노-아세트산 용매화물을 분리하는 방법.
  7. 제5항에 있어서, 아세트산을 혼합하고, 결정상, 3-하이드록시 에스테르를 분리하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880011519A 1987-09-14 1988-09-07 결정상 항생제 중간물질 KR960015966B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/095,721 1987-09-14
US07/095,721 US4782144A (en) 1987-09-14 1987-09-14 1-carba(dethia)-3-hydroxy-3-cephem ester crystalline and crystalline solvate thereof

Publications (2)

Publication Number Publication Date
KR890005099A true KR890005099A (ko) 1989-05-11
KR960015966B1 KR960015966B1 (ko) 1996-11-25

Family

ID=22253299

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019880011519A KR960015966B1 (ko) 1987-09-14 1988-09-07 결정상 항생제 중간물질

Country Status (11)

Country Link
US (1) US4782144A (ko)
EP (1) EP0308123B1 (ko)
JP (1) JPH01100170A (ko)
KR (1) KR960015966B1 (ko)
AT (1) ATE98242T1 (ko)
CA (1) CA1334590C (ko)
DE (1) DE3886151T2 (ko)
ES (1) ES2061666T3 (ko)
HU (1) HU201073B (ko)
IE (1) IE61559B1 (ko)
IL (1) IL87697A (ko)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE104977T1 (de) * 1988-06-22 1994-05-15 Lilly Co Eli Zwischenprodukt fuer 1-carba(dethia)cephalosporin.
US5412094A (en) * 1993-06-28 1995-05-02 Eli Lilly And Company Bicyclic beta-lactam/paraben complexes
US6001996A (en) * 1995-05-11 1999-12-14 Eli Lilly And Company Complexes of cephalosporins and carbacephalosporins with parabens

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE49374B1 (en) * 1979-02-01 1985-09-18 Lilly Co Eli Crystalline 3-hydroxycephalosporin solvates
US4237279A (en) * 1979-07-27 1980-12-02 Eli Lilly And Company Crystalline 3-hydroxycephalosporin solvates
US4665171A (en) * 1985-07-17 1987-05-12 Harvard University Process and intermediates for β-lactam antibiotics
US4673737A (en) * 1985-08-02 1987-06-16 Harvard University 7-acylamino-(or 7-amino)-3-trifluoromethylsulfonyloxy-1-carba(1-dethia)-3-cephem-4-carboxylic acids and esters thereof

Also Published As

Publication number Publication date
US4782144A (en) 1988-11-01
HU201073B (en) 1990-09-28
ATE98242T1 (de) 1993-12-15
EP0308123B1 (en) 1993-12-08
ES2061666T3 (es) 1994-12-16
HUT47931A (en) 1989-04-28
DE3886151D1 (de) 1994-01-20
EP0308123A1 (en) 1989-03-22
IL87697A (en) 1993-04-04
DE3886151T2 (de) 1994-04-28
IE882721L (en) 1989-03-14
KR960015966B1 (ko) 1996-11-25
IL87697A0 (en) 1989-02-28
JPH01100170A (ja) 1989-04-18
IE61559B1 (en) 1994-11-16
CA1334590C (en) 1995-02-28

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