FI84484B - Foerfarande foer framstaellning av temperaturstabila, kristallina cefalosporinsalt. - Google Patents

Foerfarande foer framstaellning av temperaturstabila, kristallina cefalosporinsalt. Download PDF

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Publication number
FI84484B
FI84484B FI863155A FI863155A FI84484B FI 84484 B FI84484 B FI 84484B FI 863155 A FI863155 A FI 863155A FI 863155 A FI863155 A FI 863155A FI 84484 B FI84484 B FI 84484B
Authority
FI
Finland
Prior art keywords
acid addition
salt
crystalline
zwitterion
methyl
Prior art date
Application number
FI863155A
Other languages
English (en)
Finnish (fi)
Other versions
FI84484C (sv
FI863155A0 (fi
FI863155A (fi
Inventor
Murray A Kaplan
Thomas W Hudyma
Robert A Lipper
Original Assignee
Squibb Bristol Myers Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Squibb Bristol Myers Co filed Critical Squibb Bristol Myers Co
Publication of FI863155A0 publication Critical patent/FI863155A0/fi
Publication of FI863155A publication Critical patent/FI863155A/fi
Priority to FI912560A priority Critical patent/FI912560A0/fi
Application granted granted Critical
Publication of FI84484B publication Critical patent/FI84484B/fi
Publication of FI84484C publication Critical patent/FI84484C/sv

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/38—Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof
    • C07D501/46—Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof with the 7-amino radical acylated by carboxylic acids containing hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (8)

1. Förfarande för framställning av temperatursta-bila, kristallina svavel-, di-kväve-, mono-klorväte- och 5 di-klorvätesyraadditionssalter av 7-[a-(2-aminotiazol-4- yl)-α-(Z)-metoxi-iminoacetamido]-3-[(1-metyl-l-pyrrolidi-nio)-metyl]-3-cefem-4-karboxylat, och ortofosforsyraaddi-tionssalter innehällande 1,5-2 molekvivalenter H3P04, kännetecknat därav, att förfarandet omfattar 10 följande steg: (a) bildande av en vattenhaltig blandning av syran med en zwitterjon, som motsvarar ifrägavarande sait, (b) bringande av saltet att kristallisera, och (c) isolering av det kristallina saltet. 15
2. Förfarande enligt patentkravet 1 för framställ ning av det i patentkravet 1 definierade svavelsyraaddi-tionssaltet, kännetecknat därav, att det omfattar följande steg: (a) bildande av en vattenhaltig blandning av (i) ätminstone 1 molekvivalent svavelsyra 20 och (ii) en zwitterjon, som motsvarar ifrägavarande sait, (b) bringande av svavelsyraadditionssaltet att kristallisera, förutsatt, att dä zwitterjonhalten i blandningen är under 25 mg/ml, utförs kristalliseringen i närvaro av ett organiskt lösningsmedel, och (c) isolering av det kris-25 tallina svavelsyraadditionssaltet.
3. Förfarande enligt patentkravet 2, kännetecknat därav, att steget (b) utförs i ett vatten-haltigt medium, som ej innehäller ett organiskt lösningsmedel . 30
4. Förfarande enligt patentkravet 3, känne tecknat därav, att zwitterjonen i steget (a) an-vänds i en sädan mängd, att dess hait i blandningen är under 500 mg/ml.
5. Förfarande enligt patentkravet 2, k ä n n e -35 tecknat därav, att mängden av zwitterjonen i ste- 2i 84 4 84 get (a) är sädan, att dess halt i blandningen är över 25 mg/ml.
6. Förfarande enllgt patentkravet 3, känne-t e c k n a t därav, att zwitterjonen i steget (a) an- 5 vänds i en sädan mängd, att dess halt i blandningen va-rierar mellan cirka 100 mg/ml och 200 mg/ml.
7. Förfarande enligt patentkravet 1, känne- t e c k n a t därav, att man framställer ett kristallini sulfatsalt av 7-[α-(2-aminotiazol-4-yl)-α-(Z)-metoxi-imi-10 noacetamido]—3—[(l-metyl-l-pyrrolidinio)-metyl]-3-cefem- 4-karboxylat, som har följande röntgendiffraktionsvärden i pulverform: d dlstans (A) 1/1° (%) 9,20 100 15 6,86 50 5.50 28 5,09 22 4.50 38 4,41 44 20 4,19 63 3,78 38 3,64 44 3,39 25 3,31 31 25 3,15 47
8. Förfarande enligt patentkravet 1, känne- t e c k n a t därav, att man framställer ett kristallint 7-[a-(2-aminotiazol-4-yl)-a-(Z)-metoxi-iminoacetamido]-30 3-[(l-metyl-l-pyrrolidinio)-metyl]-3-cefem-4-karboxylat- fosfat, som har följande röntgendiffraktionsvärden i pulverform: 22 8 4 484 d 1/1° 11,04 - 32 9,2 - 16 7,89 - 24 5 7,02 - 42 6,7 - 32 5,5 - 26 4,64 - 100 4,456 - 53 10 4,3 - 58 3,88 - 26 3,75 - 89 3,56 - 21 3,31 - 26 15 3,05 - 16
FI863155A 1985-08-05 1986-08-01 Förfarande för framställning av temperaturstabila, kristallina cefalos porinsalt FI84484C (sv)

Priority Applications (1)

Application Number Priority Date Filing Date Title
FI912560A FI912560A0 (fi) 1985-08-05 1991-05-28 Foerfarande foer framstaellning av fysikaliska blandningar som innehaoller kefalosporinsalter.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US76223585A 1985-08-05 1985-08-05
US76223585 1985-08-05

Publications (4)

Publication Number Publication Date
FI863155A0 FI863155A0 (fi) 1986-08-01
FI863155A FI863155A (fi) 1987-02-06
FI84484B true FI84484B (fi) 1991-08-30
FI84484C FI84484C (sv) 1991-12-10

Family

ID=25064475

Family Applications (1)

Application Number Title Priority Date Filing Date
FI863155A FI84484C (sv) 1985-08-05 1986-08-01 Förfarande för framställning av temperaturstabila, kristallina cefalos porinsalt

Country Status (34)

Country Link
JP (1) JPH0615548B2 (sv)
KR (1) KR930003121B1 (sv)
AR (1) AR243894A1 (sv)
AT (1) AT390957B (sv)
AU (1) AU597262B2 (sv)
BE (1) BE905219A (sv)
CA (1) CA1284994C (sv)
CH (1) CH675581A5 (sv)
CS (2) CS276717B6 (sv)
CY (1) CY1614A (sv)
DD (2) DD254941A5 (sv)
DE (1) DE3626375A1 (sv)
DK (1) DK162053C (sv)
EG (1) EG18003A (sv)
ES (1) ES2002112A6 (sv)
FI (1) FI84484C (sv)
FR (1) FR2585705B1 (sv)
GB (1) GB2179936B (sv)
GR (1) GR862055B (sv)
HK (1) HK99691A (sv)
HU (1) HU196602B (sv)
IE (1) IE59222B1 (sv)
IL (1) IL79608A (sv)
IT (1) IT1197067B (sv)
LU (2) LU88574I2 (sv)
MY (1) MY102212A (sv)
NL (1) NL8601991A (sv)
OA (1) OA08672A (sv)
PT (1) PT83134B (sv)
SE (1) SE469633B (sv)
SG (1) SG79791G (sv)
SU (1) SU1516013A3 (sv)
YU (1) YU45793B (sv)
ZA (1) ZA865842B (sv)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4883868A (en) * 1984-12-27 1989-11-28 Banyu Pharmaceutical Co., Ltd. 7-amino-3-(substituted isoindolinium)methyl-3-cephem derivatives
US4959469A (en) * 1984-12-27 1990-09-25 Banyu Pharmaceutical Company, Ltd. Crystalline cephalosporin compounds
US5244891A (en) * 1985-08-05 1993-09-14 Bristol-Myers Squibb Company Injectable compositions of cefepime dihydrochloride hydrate
US4910301A (en) * 1985-08-05 1990-03-20 Bristol-Myers Company Cefepime cephalosporin salts
US4808617A (en) * 1985-12-18 1989-02-28 Bristol-Myers Company Lyophilized or precipitated cephalosporin zwitterion and salt combination
EP0321562B1 (en) * 1987-06-25 1993-11-24 Banyu Pharmaceutical Co., Ltd. Crystalline cephalosporin compounds, process for their preparation, and intermediates for their preparation
JPH02101081A (ja) * 1988-10-08 1990-04-12 Meiji Seika Kaisha Ltd セファロスポリン誘導体結晶性二塩酸塩及びその製造法
CA2011116C (en) * 1989-03-06 1999-11-16 Murray A. Kaplan Lyophilized bmy-28142 dihydrochloride for parenteral use
CA2101571A1 (en) * 1992-09-08 1994-03-09 Elizabeth A. Garofalo Crystalline dihydrate of a cephalosporin dihydrate salt and injectable compositions thereof
EP0638573A1 (en) * 1993-08-10 1995-02-15 Lucky Ltd. Crystalline hydrates of cephalosporin and process for preparation thereof
CN100543027C (zh) 2003-12-23 2009-09-23 桑多斯有限公司 制备用于合成头孢菌素的中间体的方法
WO2008056221A2 (en) * 2006-11-06 2008-05-15 Orchid Chemicals & Pharmaceuticals Limited Crystalline sulfate salt of cephalosporin antibiotic
DE102012101680A1 (de) * 2012-02-29 2013-08-29 Aicuris Gmbh & Co. Kg Pharmazeutische Zubereitung enthaltend ein antiviral wirksames Dihydrochinazolinderivat

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS55151588A (en) * 1979-05-14 1980-11-26 Takeda Chem Ind Ltd Preparation of cephalosporin salt crystal
CA1213882A (en) * 1982-03-04 1986-11-12 Jun Okumura Cephalosporins
US4406899A (en) * 1982-03-04 1983-09-27 Bristol-Myers Company Cephalosporins
US4525473A (en) * 1983-03-30 1985-06-25 Bristol-Myers Company Cephalosporins
DE3419015A1 (de) * 1984-05-22 1985-11-28 Bayer Ag, 5090 Leverkusen Verfahren zur herstellung von cephalosporinen
GB8424692D0 (en) * 1984-10-01 1984-11-07 Glaxo Group Ltd Chemical compounds
GB2165245B (en) * 1984-10-01 1988-05-25 Glaxo Group Ltd Chemical compounds

Also Published As

Publication number Publication date
SU1516013A3 (ru) 1989-10-15
CS276717B6 (en) 1992-08-12
AT390957B (de) 1990-07-25
FR2585705A1 (fr) 1987-02-06
OA08672A (en) 1989-03-31
GB2179936B (en) 1989-04-26
CS276849B6 (en) 1992-08-12
CY1614A (en) 1992-07-10
HUT41802A (en) 1987-05-28
DK162053C (da) 1992-02-10
BE905219A (fr) 1987-02-04
DK162053B (da) 1991-09-09
IE59222B1 (en) 1994-01-26
ZA865842B (en) 1987-04-29
AU6069486A (en) 1987-02-12
YU45793B (sh) 1992-07-20
FI84484C (sv) 1991-12-10
HK99691A (en) 1991-12-13
IE862078L (en) 1987-02-05
PT83134B (pt) 1989-07-31
FI863155A0 (fi) 1986-08-01
ES2002112A6 (es) 1988-07-16
DK371886D0 (da) 1986-08-04
LU88574I2 (fr) 1995-03-01
DK371886A (da) 1987-02-06
SE469633B (sv) 1993-08-09
YU137186A (en) 1987-12-31
DE3626375A1 (de) 1987-02-12
GB2179936A (en) 1987-03-18
CA1284994C (en) 1991-06-18
IT8621409A0 (it) 1986-08-04
AU597262B2 (en) 1990-05-31
LU86540A1 (fr) 1987-03-06
HU196602B (en) 1988-12-28
IT8621409A1 (it) 1988-02-04
IT1197067B (it) 1988-11-25
FI863155A (fi) 1987-02-06
IL79608A (en) 1991-07-18
MY102212A (en) 1992-05-15
GB8618989D0 (en) 1986-09-17
AR243894A1 (es) 1993-09-30
NL8601991A (nl) 1987-03-02
EG18003A (en) 1991-08-30
ATA211086A (de) 1990-01-15
DD268395A5 (de) 1989-05-31
IL79608A0 (en) 1986-11-30
KR930003121B1 (ko) 1993-04-19
SE8603308L (sv) 1987-02-06
DD254941A5 (de) 1988-03-16
JPH0615548B2 (ja) 1994-03-02
KR880002530A (ko) 1988-05-09
CH675581A5 (sv) 1990-10-15
SE8603308D0 (sv) 1986-08-04
SG79791G (en) 1991-11-15
PT83134A (en) 1986-09-01
GR862055B (en) 1986-12-24
JPS62103090A (ja) 1987-05-13
FR2585705B1 (fr) 1989-01-13

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FI84484B (fi) Foerfarande foer framstaellning av temperaturstabila, kristallina cefalosporinsalt.
FI76094B (fi) Foerfarande foer framstaellning av terapeutiskt anvaendbara kristallina 7-(2-(2-aminotiazol-4-yl)-2- syn-metoxiiminoacetamido)-3-((2,3-cyklopenteno-1-pyridino)-metyl)- cef-3-em-4-karboxylat-syraadditionssalter.
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FG Patent granted

Owner name: BRISTOL-MYERS SQUIBB COMPANY

MA Patent expired