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    • 6. 发明申请
    • CEPHEM COMPOUND
    • CEPHEM化合物
    • WO2004106347A1
    • 2004-12-09
    • PCT/NL2004/000367
    • 2004-05-24
    • DSM IP ASSETS B.V.VAN DEN BERG, Marco, AlexanderBOVENBERG, Roelof, Ary, LansRAAMSDONK, Lourina, Madeleine, LeonieSUTHERLAND, John, DavidDE VROOM, ErikVOLLINGA, Roeland, Christiaan, Roel
    • VAN DEN BERG, Marco, AlexanderBOVENBERG, Roelof, Ary, LansRAAMSDONK, Lourina, Madeleine, LeonieSUTHERLAND, John, DavidDE VROOM, ErikVOLLINGA, Roeland, Christiaan, Roel
    • C07D501/00
    • C07D501/00
    • The present invention is concerned with a novel cephem compound, with a process for the production of this compound, which process may contain or consist of fermentative steps, chemical steps, and/or biotransformation steps. A cephem compound according to the present invention characterised by formula (I) or a salt or ester thereof, wherein R is selected from the group consisting of (carboxymethylthio)propionyl (carboxyethylthio)propionyl Y- CH2-CO15 wherein Y is phenyl, phenoxy or tetrazolyl HOOC-X-CO wherein X is defined as (CH 2 ) 4 or wherein X is defined as (CH 2 )P-A-(CH 2 )q, wherein p and q each individually are 0, 1, 2, 3 or 4, and A is CH=CH, C-=C, CHB, C=O, O, S, NH, the nitrogen optionally being substituted or the sulfur optionally being oxidized, and B is hydrogen, halogen, C 1-3 alkoxy, hydroxyl, or optionally substituted methyl, with the proviso that p+q should be 2 or 3, when A is CH=CH or C=-C, or p+q should be 3 or 4, when A is CHB, C=O, 0, S or NH or wherein X is (CH 2 ) m -CH=A-(CH2) n or (CH 2 ) m -C=-C-(CH 2 ) n , wherein m and n each individually are 0, 1, 2 or 3 and m+n = 2 or 3, and A is CH or N, or wherein X is (CH2)p-CH=CH-C H=C-(CH2)q wherein p and q each individually are 0 or 1 and p+q = 0 or 1 and wherein R' is selected from the group consisting of OH O-(alkyl 1-6C) wherein the alkyl can be straight or branched and O-C(alkyl 1-6C)-O-(alkyl 1-6C) wherein the alkyl groups can be straight or branched can inter alia be prepared by fermentative techniques according to the invention and in particular using a suitable microorganism possessing or being transformed with the genes needed for conversion of an appropriate acyl-6-aminopenicillanic acid into the desired compound.
    • 本发明涉及一种新的头孢烯化合物,其具有生产该化合物的方法,该方法可以含有或由发酵步骤,化学步骤和/或生物转化步骤组成。 根据本发明的头孢烯化合物,其特征在于式(I)化合物或其盐或酯,其中R选自(羧甲硫基)丙酰基(羧乙硫基)丙酰基Y-CH 2 -CO 15,其中Y是苯基,苯氧基或 四唑基HOOC-X-CO,其中X定义为(CH 2)4或其中X定义为(CH 2)PA-(CH 2)q,其中p和q各自独立地为0,1,2,3或4,并且A 是CH = CH,C = C,CHB,C = O,O,S,NH,任选被取代的氮或任选被氧化的硫,B是氢,卤素,C 1-3烷氧基,羟基或任选地 取代的甲基,条件是当A为CH = CH或C = -C时,p + q应为2或3,或p + q应为3或4,当A为CHB时,C = O,O,S 或NH或其中X是(CH 2)m -CH = A-(CH 2)n或(CH 2)m C = -C-(CH 2)n,其中m和n各自独立地是0,1,2或3和m + n = 2或3,A为CH或N,或其中X为(CH 2)p -CH = CH-C H = C-(CH 2)q,其中p和q各自各自为0或1,p + q = 0或1和 其中R'选自OH -O-(烷基1-6C),其中烷基可以是直链或支链和OC(烷基1-6C)-O-(烷基1-6C),其中烷基可以是 直链或支链可以特别通过根据本发明的发酵技术制备,特别是使用具有或正在转化合适的酰基-6-氨基青霉烷酸所需基因的合适微生物进入所需化合物。