KR940021558A - Method for preparing a novel crystalline cephalosporin derivative - Google Patents

Method for preparing a novel crystalline cephalosporin derivative Download PDF

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Publication number
KR940021558A
KR940021558A KR1019930003097A KR930003097A KR940021558A KR 940021558 A KR940021558 A KR 940021558A KR 1019930003097 A KR1019930003097 A KR 1019930003097A KR 930003097 A KR930003097 A KR 930003097A KR 940021558 A KR940021558 A KR 940021558A
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South Korea
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formula
compound
iii
process according
preparing
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KR1019930003097A
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Korean (ko)
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KR960011778B1 (en
Inventor
문순구
이관순
김용립
장영길
김맹섭
이향원
고준형
천종필
이재헌
유승원
길영환
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임성기
한미약품 공업주식회사
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    • 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
    • C07D501/02—Preparation
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

본 발명은 구조식(Ⅱ)의 세펨 화합물을 일반식(Ⅲ) 화합물의 존재하에서 구조식(Ⅳ)의 피리딘과 반응시킴을 특징으로 하여, 안정한 결정성 세프타지딤 펜타하이드레이트의 제조에 유용한 신규한 구조식(Ⅰ)의 세프타지딤 비스하이드로요오다이드 모노하이드레이트를 제조하는 방법에 관한 것이다.The present invention is characterized by reacting a cefe compound of formula (II) with pyridine of formula (IV) in the presence of a compound of formula (III), thereby providing a novel structural formula useful for the preparation of stable crystalline ceftazidime pentahydrate ( The present invention relates to a method for producing ceftazidime bishydroiodide monohydrate of I).

상기식에서, R1,R2및 R3는 각각 독립적으로 탄소수 1 내지 4의 알킬기이다.In the above formula, R 1 , R 2 and R 3 are each independently an alkyl group having 1 to 4 carbon atoms.

Description

신규한 결정성 세팔로스포린 유도체의 제조방법Method for preparing a novel crystalline cephalosporin derivative

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

제1도 및 제2도는 각각 본 발명에 따라 구조식(Ⅰ)의 결정성 세프타지딤 비스하이드로요오다이드 모노하이드레이트 화합물의 X-선 분말회절 스펙트럼 및 IR 스펙트럼을 나타낸다.1 and 2 respectively show the X-ray powder diffraction spectrum and the IR spectrum of the crystalline ceftazidime bishydroiodide monohydrate compound of formula (I) according to the present invention.

Claims (7)

다음 구조식(Ⅱ)의 세펨 화합물을 일반식(Ⅲ) 화합물의 존재하에서 구조식(Ⅳ)의 피리딘과 반응시킴을 특징으로 하여, 구조식(Ⅰ)의 결정성 세프타지딤 비스하이드로요오다이드 모노하이드레이트 화합물을 제조하는 방법.A crystalline ceftazidime bishydroiodide monohydrate compound of formula (I), characterized by reacting a cefem compound of formula (II) with a pyridine of formula (IV) in the presence of a compound of formula (III) How to prepare. 상기식에서, R1,R2및 R3는 각각 독립적으로 탄소수 1 내지 4의 알킬기이다.In the above formula, R 1 , R 2 and R 3 are each independently an alkyl group having 1 to 4 carbon atoms. 제1항에 있어서, 일반식(Ⅲ) 화합물이 트리메틸요오드실란임을 특징으로 하는 방법.The method of claim 1, wherein the compound of formula III is trimethyliodinesilane. 제1항에 있어서, 구조식(Ⅱ)의 화합물 1당량에 대해 일반식(Ⅲ)의 화합물 1 내지 8당량 및 구조식(Ⅳ)의피리딘 1 내지 8당량을 사용함을 특징으로 하는 방법.A process according to claim 1, characterized in that 1 to 8 equivalents of compound of formula (III) and 1 to 8 equivalents of pyridine of formula (IV) are used for 1 equivalent of compound of formula (II). 제1항에 있어서, 일반식(Ⅲ)의 화합물을 추가의 실릴화제와의 혼합물로 사용함을 특징으로 하는 방법.2. Process according to claim 1, characterized in that the compound of formula (III) is used in admixture with an additional silylating agent. 제4항에 있어서, 실릴화제가 비스트리메틸실릴아세트아마이드, 비스트리메틸실릴트리플루오로아세트아마이드, 헥사메틸디실라잔 및 비스트리메틸실릴우레아 중에서 선택됨을 특징으로 하는 방법.The method of claim 4, wherein the silylating agent is selected from bistrimethylsilylacetamide, bistrimethylsilyltrifluoroacetamide, hexamethyldisilazane and bistrimethylsilylurea. 제4항에 있어서, 구조식(Ⅱ)의 화합물 1당량에 대하여 실릴화제 1 내지 6당량을 사용함을 특징으로 하는 방법.5. Process according to claim 4, characterized in that 1 to 6 equivalents of silylating agent is used relative to 1 equivalent of compound of formula (II). 제1항에 있어서, 추가로 요오드화수소산을 첨가하여 반응을 완결시킴을 특징으로 하는 방법.The process according to claim 1, wherein further hydroiodic acid is added to complete the reaction. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019930003097A 1993-03-03 1993-03-03 Novel process for preparing crystalline hydrate of cephalosporin KR960011778B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1019930003097A KR960011778B1 (en) 1993-03-03 1993-03-03 Novel process for preparing crystalline hydrate of cephalosporin

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1019930003097A KR960011778B1 (en) 1993-03-03 1993-03-03 Novel process for preparing crystalline hydrate of cephalosporin

Publications (2)

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KR940021558A true KR940021558A (en) 1994-10-19
KR960011778B1 KR960011778B1 (en) 1996-08-30

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