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KR860001818A - D-6-{α-〔(2-옥소-3- 푸르푸릴리덴- 아미노-이미다졸리딘-1-일)카르보닐아미노〕-2-티에닐아세트아미도}-페니실란산의 결정성 나트륨의 제조방법 - Google Patents

D-6-{α-〔(2-옥소-3- 푸르푸릴리덴- 아미노-이미다졸리딘-1-일)카르보닐아미노〕-2-티에닐아세트아미도}-페니실란산의 결정성 나트륨의 제조방법 Download PDF

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Publication number
KR860001818A
KR860001818A KR1019850006132A KR850006132A KR860001818A KR 860001818 A KR860001818 A KR 860001818A KR 1019850006132 A KR1019850006132 A KR 1019850006132A KR 850006132 A KR850006132 A KR 850006132A KR 860001818 A KR860001818 A KR 860001818A
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South Korea
Prior art keywords
sodium salt
formula
ethanol
acid
furfurylidene
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KR1019850006132A
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English (en)
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쾨니히(외 2) 한스-보도
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게젤하르트 뷔네만, 클라우스 데너
바이엘 악티엔 게젤샤프트
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Publication of KR860001818A publication Critical patent/KR860001818A/ko

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D499/00Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D499/21Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a nitrogen atom directly attached in position 6 and 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
    • C07D499/44Compounds with an amino radical acylated by carboxylic acids, attached in position 6
    • C07D499/48Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical
    • C07D499/58Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical substituted in alpha-position to the carboxamido radical
    • C07D499/64Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical substituted in alpha-position to the carboxamido radical by nitrogen atoms
    • C07D499/70Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical substituted in alpha-position to the carboxamido radical by nitrogen atoms with hetero rings as additional substituents on the carbon chain
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D499/00Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring

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  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

내용 없음

Description

D-6-{α-[(2-옥소-3-푸르푸릴리덴-아미노-이미다졸리딘-1-일)카르보닐아미노]-2-티에닐아세트아미도}-페니실란산의 결정성 나트륨의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 무정형 나트륨염(EP-A 0 000 392의 실시예 5에 의한 친핵성)의 IR스펙트럼을 나타낸 것임.
주파수(cm-1)은 X축에 나타내고 Y축의 수치는 투과율(%)을 나타냄.
스펙트럼 상단의 수치는 파장(미크론)임.
뉴졸을 용매로 사용했음.
제2도는 i-프로필알코올을 사용해서 얻은 무정형 나트륨염에 대한 IR스펙트럼을 나타낸 것임(비교예 2참조).
제3도는 에틸알코올을 사용해서 얻은 결정성 나트륨염에 대한 IR스펙트럼을 나타낸 것임(실시예 1,2참조).
제2도 및 제3도의 X축 및 Y축의 수치는 제1도에서 정의한 단위와 같음.

Claims (14)

  1. 순수한 결정질 형으로 하기 구조식(Ⅰ)의 D-6-{α-[(2-옥소-3-푸르푸릴리덴-아미노-이미다졸리딘-1-일)카르보닐아미노]-2-티에닐아세트아미도}-페니실란산의 결정성 나트륨염.
  2. 제1항에 있어서, NMR시그날이 δ=9.36(1H), 9.23(1H), 7.8(2H), 7.5(1H), 7.25(1H), 7.05(1H),(1H), 6.89(1H), 6.62(1H), 6.2(1H), 5.74(1H), 5.74(1H), 5.56(1H), 4.35(1H), 3.92(4H), 1.6(3H) 및 1.5pp(3H) (DMF-d7중에서)인것을 특징으로 하는 결정성 나트륨염.
  3. 순수한 결정질 형태로 다음 구조식(Ⅰ)의 화합물의 나트륨염을 제조하는 방법에 있어서,
  4. 구조식(Ⅰ)의 D-페닐실란산의 무정형 나트륨염을 에탄올/물 혼합물로부터 결정화시킴을 특징으로 하는 방법.
  5. 제3항에 있어서, 결정화를 에탄올:물의 비가 5;1내지 15:1로 되는 에탄올/물 혼합물로부터 행함을 특징으로 하는 방법.
  6. 제3항 및 제4항에 있어서, 공정을 0℃내지 50℃의 온도에서 행함을 특징으로 하는 방법.
  7. 순수한 결정형으로 제2항에 의한 구조식(Ⅰ)의 D-페닐실린산의 나트륨을 제조하는 방법에 있어서, 제2항에 의한 구조식(Ⅰ)의 결정산성을 나트륨염으로 전환시키고, 이 나트륨염을 에탄올/물 혼합물로부터 결정화시킴을 특징으로 하는 방법.
  8. 제2항에 의한 구조식(Ⅰ)의 D-페니실린산의 결정성 나트륨염을 유효 화합물로서 함유하는 약재.
  9. 제4항에 있어서, 유효 화합물을 적당한 투여형으로 전환시키고, 필요에 따라서 통상의 보조제 및 부형제를 사용하는 것을 특징으로 하는 약제의 제조방법.
  10. 제1항에 의한 물질의 질병 치료용도.
  11. 제1항에 의한 물질의 약제 제조용도.
  12. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019850006132A 1984-08-25 1985-08-24 D-6-{α-〔(2-옥소-3- 푸르푸릴리덴- 아미노-이미다졸리딘-1-일)카르보닐아미노〕-2-티에닐아세트아미도}-페니실란산의 결정성 나트륨의 제조방법 KR860001818A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DEP3431273.0 1984-08-25
DE19843431273 DE3431273A1 (de) 1984-08-25 1984-08-25 Kristallines natriumsalz der d-6-((alpha)-(2-oxo-3-furfuryl-iden-amino-imidazolidin-1-yl)-carbonylamino)-thienyl-2-acetamido)-penicillansaeure, verfahren zur herstellung und seine verwendung in arzneimitteln
CN85106479A CN85106479B (zh) 1984-08-25 1985-08-29 晶状的右旋-6-{α-[(2-氧代-3-亚糠基-氨基-咪唑烷-1-基)碳酰氨基]-2-噻吩基乙酰氨基}-青霉烷酸钠盐制备方法

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KR860001818A true KR860001818A (ko) 1986-03-22

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KR1019850006132A KR860001818A (ko) 1984-08-25 1985-08-24 D-6-{α-〔(2-옥소-3- 푸르푸릴리덴- 아미노-이미다졸리딘-1-일)카르보닐아미노〕-2-티에닐아세트아미도}-페니실란산의 결정성 나트륨의 제조방법

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EP (1) EP0176716B1 (ko)
JP (1) JPS6157589A (ko)
KR (1) KR860001818A (ko)
CN (1) CN85106479B (ko)
AT (1) ATE34576T1 (ko)
AU (1) AU559040B2 (ko)
DE (2) DE3431273A1 (ko)
DK (1) DK385085A (ko)
ES (1) ES8609340A1 (ko)
FI (1) FI853211L (ko)
GR (1) GR852047B (ko)
HU (1) HU194893B (ko)
IL (1) IL76164A0 (ko)
NO (1) NO853188L (ko)
NZ (1) NZ213198A (ko)
PH (1) PH21842A (ko)
PT (1) PT81014B (ko)
ZA (1) ZA856413B (ko)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW347383B (en) * 1995-10-26 1998-12-11 Biochemie Gmbh A process for the production of a crystalline sodium salt of amoxicillin in ethanol as solvent
US9844374B2 (en) 2014-12-18 2017-12-19 Ethicon Llc Surgical instrument systems comprising an articulatable end effector and means for adjusting the firing stroke of a firing member

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL85039B1 (pl) * 1972-02-17 1977-02-26 Tarchomińskie Zakłady Farmaceutyczne Sposób wytwarzania soli sodowej a-ftminobenzylopeiiicylmy
PL87153B1 (pl) * 1973-07-13 1976-12-15 Tarchomińskie Zakłady Farmaceutyczne Sposób otrzymywania krystalicznej soli dwusodowej penicyliny a-karboksybenzylowej
DE2732323A1 (de) * 1977-07-16 1979-01-25 Bayer Ag Beta-lactam-verbindungen, verfahren zu ihrer herstellung sowie ihre verwendung
DE2732283A1 (de) * 1977-07-16 1979-01-25 Bayer Ag Beta-lactam-verbindungen
JPS5940727A (ja) * 1982-07-28 1984-03-06 Fujitsu Ltd 自動等化方式

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CN85106479B (zh) 1988-07-27
DK385085A (da) 1986-02-26
AU559040B2 (en) 1987-02-19
ZA856413B (en) 1986-04-30
HU194893B (en) 1988-03-28
PT81014A (en) 1985-09-01
FI853211L (fi) 1986-02-26
PT81014B (pt) 1987-12-30
PH21842A (en) 1988-03-17
EP0176716B1 (de) 1988-05-25
DK385085D0 (da) 1985-08-23
JPS6157589A (ja) 1986-03-24
NO853188L (no) 1986-02-26
IL76164A0 (en) 1985-12-31
ES546379A0 (es) 1986-07-16
GR852047B (ko) 1985-12-20
NZ213198A (en) 1989-02-24
EP0176716A1 (de) 1986-04-09
ATE34576T1 (de) 1988-06-15
DE3562918D1 (en) 1988-06-30
FI853211A0 (fi) 1985-08-21
ES8609340A1 (es) 1986-07-16
AU4657785A (en) 1986-02-27
CN85106479A (zh) 1987-03-18
HUT38354A (en) 1986-05-28
DE3431273A1 (de) 1986-03-06

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