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1.发明公开Indoxyl-beta-d-glucuronide and method for making 失效Indoxyl-beta-D-Glukuronid和Verfahren zur Herstellung。
公开(公告)号：EP0284725A2
公开(公告)日：1988-10-05
申请号：EP88101407.0
申请日：1988-02-01
发明人： Wolfe, Saul , Bowers, Raymond J.
摘要： Indoxyl-β- -glucuronide. its stable salts and analogs thereof are described, together with a process for the production thereof in which a compound of the formula:
where X is halogen and R is lower alkyl is reacted with a compound of the formula:
where R 1 is any common carboxyl-protecting group, X, Y, Z and Q are the same or different and selected from hydrogen, halogen, trihalogenated alkene, trihalo-methyl, nitro, saturated or unsaturated alkyl and an aromatic moiety in water and methylene chloride containing an alkali hydroxide in the presence of a phase transfer catalyst, with subsequent removal of the blocking groups and conversion to the desired stable salt.摘要翻译： 描述了吲哚基-β-β-葡糖苷酸，其稳定的盐和类似物及其制备方法，其中下式化合物：其中X为卤素且R为低级烷基的式为：CHEM，与化合物 其中R 1是任何常见的羧基保护基，X，Y，Z和Q相同或不同，选自氢，卤素，三卤代烯烃，三卤代甲基，硝基，饱和或 不饱和烷基和在水相中的芳族部分和含有碱金属氢氧化物的二氯甲烷，在相转移催化剂存在下，随后除去封闭基团并转化成所需的稳定盐。
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公开(公告)号：EP0284725A3
公开(公告)日：1990-03-21
申请号：EP88101407.0
申请日：1988-02-01
发明人： Wolfe, Saul , Bowers, Raymond J.
摘要： Indoxyl-β- -glucuronide. its stable salts and analogs thereof are described, together with a process for the production thereof in which a compound of the formula:
where X is halogen and R is lower alkyl is reacted with a compound of the formula:
where R 1 is any common carboxyl-protecting group, X, Y, Z and Q are the same or different and selected from hydrogen, halogen, trihalogenated alkene, trihalo-methyl, nitro, saturated or unsaturated alkyl and an aromatic moiety in water and methylene chloride containing an alkali hydroxide in the presence of a phase transfer catalyst, with subsequent removal of the blocking groups and conversion to the desired stable salt.摘要翻译： 描述了吲哚基-β-β-葡糖苷酸，其稳定的盐和类似物及其制备方法，其中下式化合物：其中X为卤素且R为低级烷基的式为：CHEM，与化合物 其中R 1是任何常见的羧基保护基，X，Y，Z和Q相同或不同，选自氢，卤素，三卤代烯烃，三卤代甲基，硝基，饱和或 不饱和烷基和在水相中的芳族部分和含有碱金属氢氧化物的二氯甲烷，在相转移催化剂存在下，随后除去封闭基团并转化成所需的稳定盐。
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公开(公告)号：EP0144170B1
公开(公告)日：1989-01-25
申请号：EP84307731.4
申请日：1984-11-08
发明人： Wolfe, Saul , Westlake, Donald , Jensen, Susan
IPC分类号： C12P37/00 , C12P35/00 , C12P35/06 , C07K5/06 , C07D501/22 , A61K31/545
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公开(公告)号：EP0144170A1
公开(公告)日：1985-06-12
申请号：EP84307731.4
申请日：1984-11-08
发明人： Wolfe, Saul , Westlake, Donald , Jensen, Susan
IPC分类号： C12P37/00 , C12P35/00 , C12P35/06 , C07K5/06 , C07D501/22 , A61K31/545
摘要： A process for producing unnatural penicillins and cephalosporin derivatives thereof in which peptide analogs of ACV in which the L-a-aminodipyl moiety is replaced by L-S-carboxymethyl cysteine or other substituents, are reacted with cyclase, epimerase and ring expansion enzyme isolated from a cell free extract of a prokaryotic organism such as S. clavuligerus. The product depends upon the presence or absence of co-factors such as ferrous ion, a-ketoglutarate, and ascorbate. In an alternative embodiment, a penicillin analog having the formula
may be reacted with L-cysteine to produce an analog of isopenicillin N which may be reacted with the enzyme reagent to produce the desired penicillin or cephalosporin.摘要翻译： 一种生产非天然青霉素和头孢菌素衍生物的方法，其中将由L-羧甲基半胱氨酸或其它取代基取代的L-氨基脯氨酰部分的ACV的肽类似物与从细胞分离的环化酶，差向异构酶和环膨化酶反应 游离提取物的原核生物，如克拉维氏梭菌。 该产品取决于辅助因子如亚铁离子，α-酮戊二酸和抗坏血酸的存在或不存在。 在替代实施方案中，具有式CHEM的青霉素类似物可以与L-半胱氨酸反应以产生异青霉素N的类似物，其可与酶试剂反应以产生所需的青霉素或头孢菌素。
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公开(公告)号：EP0280051A1
公开(公告)日：1988-08-31
申请号：EP88101105.0
申请日：1988-01-26
CPC分类号： C12N9/93 , C07K5/0215 , C12P35/00 , C12P37/00
摘要： A process for producing peptides and β-lactam antibiotics from their amino acid precursors, and analogs thereof, is described. A mixture of L -a-aminoadipic acid (A), L -cysteine (C) and L -valine (V) is enzymatically converted into LLD -ACV by a glycerol stabilized cell free extracted of Cephalosporium acremonium (Acremonium chrysogenum ATCC48272). The cell free extract is a single enzyme defined as ACV-synthetase which requires all three L-amino acids for maximum activity.
摘要翻译： 描述了从其氨基酸前体及其类似物产生肽和β-内酰胺抗生素的方法。 将α-氨基己二酸（A），β-半胱氨酸（C）和β-缬氨酸（V）的混合物通过甘油稳定化的细胞从顶头孢霉（Acremonium chrysogenum ATCC48272）提取而被酶转化为@@-ACV， 。 无细胞提取物是定义为ACV合成酶的单一酶，其需要所有三种β-氨基酸用于最大活性。
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公开(公告)号：EP0102216A3
公开(公告)日：1985-05-08
申请号：EP83304687
申请日：1983-08-12
发明人： Wolfe, Saul , Westlake, Donald , Jensen, Susan
CPC分类号： C07K5/06139 , C12N9/00 , C12N9/90 , C12N11/18 , C12P35/00 , C12P35/06 , C12P37/00 , Y10S435/814 , Y10S435/815 , Y10S435/816 , Y10S435/886
摘要： A peptide precursor of the ACV (aminoadipyl- cysteinylvaline) type, in which the valine moiety may be replaced by any readily available amino acid may be converted into a cephalosporin of the type
where R, is H, lower alkyl or functionalized carboxylic group and R 2 is H or lower alkyl, by reacting the precursor with novel cyclase, epimerase and ring expansion enzymes isolated from a cell-free extract of a prokaryotic organism such as Streptomyces clavuligerus. The three novel enzymes may be immobilized separately or together on a suitable support medium and the conversion may be carried out in a continuous mode.-
公开(公告)号：EP0102216A2
公开(公告)日：1984-03-07
申请号：EP83304687.3
申请日：1983-08-12
发明人： Wolfe, Saul , Westlake, Donald , Jensen, Susan
CPC分类号： C07K5/06139 , C12N9/00 , C12N9/90 , C12N11/18 , C12P35/00 , C12P35/06 , C12P37/00 , Y10S435/814 , Y10S435/815 , Y10S435/816 , Y10S435/886
摘要： A peptide precursor of the ACV (aminoadipyl- cysteinylvaline) type, in which the valine moiety may be replaced by any readily available amino acid may be converted into a cephalosporin of the type
where R, is H, lower alkyl or functionalized carboxylic group and R 2 is H or lower alkyl, by reacting the precursor with novel cyclase, epimerase and ring expansion enzymes isolated from a cell-free extract of a prokaryotic organism such as Streptomyces clavuligerus. The three novel enzymes may be immobilized separately or together on a suitable support medium and the conversion may be carried out in a continuous mode.摘要翻译： ACV（氨基己二酰基半胱氨酰缬氨酸）类型的肽前体，其中缬氨酸部分可被任何容易获得的氨基酸替代，可转化为类型
的头孢菌素，其中R 1为H，低级烷基或官能化羧基，R 2 通过使前体与从原核生物例如链霉菌（Streptomyces clavuligerus）的无细胞提取物分离的新型环化酶，差向异构酶和环膨化酶反应而形成H或低级烷基。 三种新型酶可以单独地或一起固定在合适的载体介质上，并且转化可以以连续模式进行。
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