Products of a microbiological process for the production of
2-halo-pyrimidine-4-carboxylic acids
    1.
    发明授权
    Products of a microbiological process for the production of 2-halo-pyrimidine-4-carboxylic acids 失效
    用于生产2-卤代嘧啶-4-羧酸的微生物过程的产物

    公开(公告)号:US5591853A

    公开(公告)日:1997-01-07

    申请号:US344122

    申请日:1994-11-23

    CPC分类号: C07D239/30 C12P17/12 C12R1/40

    摘要: A 2-halo-pyrimidine-4-carboxylic acid of formula: ##STR1## wherein X is a halogen atom, for example, 2-chloro-pyrimidine-4-carboxylic acid. A 2-substituted-pyrimidine-4-carboxylic acid derivative of formula: ##STR2## wherein R.sub.1 is a halogen atom, NH.sub.2 --, HO-- or a C.sub.1 -C.sub.4 alkoxy group and R.sub.2 is a C.sub.1 -C.sub.4 alkoxy group or a halogen atom with the proviso that, if R.sub.1 is a HO-- group, R.sub.2 is not a halogen atom and with the proviso that, if R.sub.2 is a halo group, R.sub.1 is not an amino group. A 2-substituted-pyrimidine-4-carboxylic acid derivative of formula III wherein R.sub.1 is a HO-- group and R.sub.2 is an ethoxy group.

    摘要翻译: 具有下式的其中X是卤素原子的2-卤代 - 嘧啶-4-羧酸,例如2-氯 - 嘧啶-4-甲酸。 2-取代的嘧啶-4-羧酸衍生物,其结构式如下:其中R1是卤素原子,NH2-,HO-或C1-C4烷氧基,R2是C1-C4烷氧基或卤素 原子,条件是,如果R1是HO-基团,则R2不是卤素原子,条件是如果R2是卤素基团,则R1不是氨基。 式III的2-取代 - 嘧啶-4-羧酸衍生物,其中R1是HO-基团,R2是乙氧基。

    Microbiological process for the production of aromatic
hydroxy-heterocyclic carboxylic acids
    5.
    发明授权
    Microbiological process for the production of aromatic hydroxy-heterocyclic carboxylic acids 失效
    用于生产芳香族羟基 - 杂环羧酸的微生物过程

    公开(公告)号:US5516661A

    公开(公告)日:1996-05-14

    申请号:US384695

    申请日:1995-02-03

    摘要: The microbiological process for the production of hydroxy-heterocyclic carboxylic acid of formula ##STR1## wherein R.sub.1 means a hydrogen or a halogen atom and X means a nitrogen atom or a CR.sub.2 function, wherein R.sub.2 means a hydrogen or halogen atom, starting from the corresponding heterocyclic carboxylic acid. The process is performed so that an aerobic biomass which utilizes nicotinic acid, is cultivated in a molar ratio of nicotinic acid to mineral acid of 1 to 8. The ratio is assured over the entire cultivation phase. The the hydroxylation of the corresponding heterocyclic carboxylic acid of the general formula ##STR2## wherein R.sub.1 and X have the above-mentioned meanings, is performed with the biomass. Under these conditions, strain Pseudomonas acidovorans DSM 7205, strain Pseudomonas acidovorans DSM 7203, strain Alcaligenes faecalis DSM 7204 and strain Arthrobacter crystallopoietes DSM 7202 are concentrated in the cultivation phase.

    摘要翻译: 用于制备式基因原子的羟基 - 杂环羧酸的微生物方法,X表示氮原子或CR 2官能团,其中R2表示氢或卤素原子,从相应的杂环羧酸开始。 以烟碱酸与无机酸的摩尔比为1〜8培养利用烟酸的好氧生物质的方法进行。在整个培养阶段确保比例。 通过生物质进行其中R1和X具有上述含义的通式“IMAGE”II的相应杂环羧酸的羟基化。 在这些条件下,将菌株Pseudomonas acidovorans DSM 7205,耐酸假单胞菌DSM 7203,粪肠杆菌粪肠球菌DSM 7204和菌株节杆菌结晶洗脱液DSM2202浓缩在培养阶段。

    Di and trisubstituted pyridines
    8.
    发明授权
    Di and trisubstituted pyridines 失效
    二取代和三取代吡啶

    公开(公告)号:US5760236A

    公开(公告)日:1998-06-02

    申请号:US561230

    申请日:1995-11-21

    摘要: Substituted pyridines of the general formula: ##STR1## wherein R.sup.1 is hydroxyl or chlorine, and a) X is hydrogen or chlorine, R.sup.2 and R.sup.3 together are .dbd.O, R.sup.4 is a group of the formula --OR.sup.5 and R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or benzyl, or b) X is hydrogen and R.sup.2, R.sup.3 and R.sup.4 together are .dbd.N--NH--, or c) X and R.sup.2 each is hydrogen and R.sup.3 and R.sup.4 together are --O--, or d) X and R.sup.2 each is hydrogen, R.sup.3 is hydroxyl and R.sup.4 is amino or hydroxyl. The compounds are obtained by subjecting nicotine to microbiological oxidation to give 5-succinoyl-2-pyridone, followed by chemical reactions. The compounds are suitable as intermediates for the preparation of pharmaceutically active compounds.

    摘要翻译: 取代的具有以下通式的吡啶:其中R1是羟基或氯,以及a)X是氢或氯,R2和R3一起是= O,R4是式-OR5的基团,R5是氢,C1 C 1-4烷基或苄基,或b)X是氢,R 2,R 3和R 4一起是N-NH-,或c)X和R 2各自是氢,R 3和R 4一起是-O-,或d)X R2各自为氢,R3为羟基,R4为氨基或羟基。 该化合物通过使尼古丁进行微生物氧化得到5-琥珀酰基-2-吡啶酮,然后进行化学反应。 该化合物适合作为制备药物活性化合物的中间体。