KR100760429B1 - 세팔로스포린 제조용 중간체로 사용되는2-아미노티아졸-4-일 아세틸클로라이드 염산염의 개선된제조방법 - Google Patents
세팔로스포린 제조용 중간체로 사용되는2-아미노티아졸-4-일 아세틸클로라이드 염산염의 개선된제조방법 Download PDFInfo
- Publication number
- KR100760429B1 KR100760429B1 KR1020060020210A KR20060020210A KR100760429B1 KR 100760429 B1 KR100760429 B1 KR 100760429B1 KR 1020060020210 A KR1020060020210 A KR 1020060020210A KR 20060020210 A KR20060020210 A KR 20060020210A KR 100760429 B1 KR100760429 B1 KR 100760429B1
- Authority
- KR
- South Korea
- Prior art keywords
- formula
- aminothiazol
- acetic acid
- oxalyl chloride
- organic solvent
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D277/38—Nitrogen atoms
- C07D277/40—Unsubstituted amino or imino radicals
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Cephalosporin Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims (4)
- 제 1항에 있어서,1) 2-아미노티아졸-4-일 아세트산을 메틸렌클로라이드, 다이메틸폼아마이드, 클로로폼, 에틸렌다이클로라이드 및 이들의 혼합용매로 구성된 군으로부터 선택되는 유기용매에 현탁하여 -5 내지 3℃로 냉각시킨 후 20 내지 30분간 교반하는 단계;2) 옥살일 클로라이드를 메틸렌클로라이드, 다이메틸폼아마이드, 클로로폼, 에틸렌다이클로라이드 및 이들의 혼합용매로 구성된 군으로부터 선택되는 유기용매에 현탁하여 제조된 옥살일 클로라이드 용액을 상기 단계 1)의 2-아미노티아졸-4-일 아세트산 용액에 첨가하고 0 내지 5℃를 유지하면서 20 내지 30분간 첨가한 후 2 내지 3시간 동안 동일한 온도에서 교반하는 단계; 및3) 상기 혼합액에 0 내지 5℃로 유지된 아세토나이트릴을 천천히 첨가한 후 0 내지 5℃를 유지하면서 0.5 내지 1시간 동안 교반하여 화학식 1의 화합물을 생성시키는 단계를 포함하는 것을 특징으로 하는 제조방법.
- 삭제
- 제 2항에 있어서,단계 2)에서 2-아미노티아졸-4-일 아세트산 용액과 옥살일 클로라이드 용액의 혼합몰비가 1:1 내지 1:1.5 범위인 것을 특징으로 하는 제조방법.
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020060020210A KR100760429B1 (ko) | 2006-03-03 | 2006-03-03 | 세팔로스포린 제조용 중간체로 사용되는2-아미노티아졸-4-일 아세틸클로라이드 염산염의 개선된제조방법 |
CN2006100683155A CN1824658B (zh) | 2006-03-03 | 2006-03-29 | 作为头孢菌素制造用中间体使用的2-氨基噻唑-4-基乙酰氯盐酸盐的改进制造方法 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020060020210A KR100760429B1 (ko) | 2006-03-03 | 2006-03-03 | 세팔로스포린 제조용 중간체로 사용되는2-아미노티아졸-4-일 아세틸클로라이드 염산염의 개선된제조방법 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR20060039410A KR20060039410A (ko) | 2006-05-08 |
KR100760429B1 true KR100760429B1 (ko) | 2007-10-04 |
Family
ID=36935519
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1020060020210A KR100760429B1 (ko) | 2006-03-03 | 2006-03-03 | 세팔로스포린 제조용 중간체로 사용되는2-아미노티아졸-4-일 아세틸클로라이드 염산염의 개선된제조방법 |
Country Status (2)
Country | Link |
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KR (1) | KR100760429B1 (ko) |
CN (1) | CN1824658B (ko) |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100268959B1 (en) * | 1992-08-07 | 2000-10-16 | Finpael A P A | Method for the acylation of the 7-amino group of the cephalosporanic ring |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MY108872A (en) * | 1991-09-10 | 1996-11-30 | Bristol Myers Squibb Co | Preparation of a cephalosporin antibiotic using the syn-isomer of a thiazolyl intermediate. |
-
2006
- 2006-03-03 KR KR1020060020210A patent/KR100760429B1/ko active IP Right Grant
- 2006-03-29 CN CN2006100683155A patent/CN1824658B/zh not_active Expired - Fee Related
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100268959B1 (en) * | 1992-08-07 | 2000-10-16 | Finpael A P A | Method for the acylation of the 7-amino group of the cephalosporanic ring |
Also Published As
Publication number | Publication date |
---|---|
CN1824658B (zh) | 2011-10-05 |
CN1824658A (zh) | 2006-08-30 |
KR20060039410A (ko) | 2006-05-08 |
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