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    Resolution of the racemates of primary and secondary amines by enzyme-catalyzed acylation
    4.
    发明授权
    Resolution of the racemates of primary and secondary amines by enzyme-catalyzed acylation 失效
    通过酶催化酰化拆分伯胺和仲胺的外消旋体

    公开(公告)号：US5728876A

    公开(公告)日：1998-03-17

    申请号：US596238

    申请日：1996-03-11

    申请人： Friedhelm Balkenhohl ,  Bernhard Hauer ,  Wolfgang Ladner ,  Uwe Pressler ,  Christoph Nubling

    发明人： Friedhelm Balkenhohl ,  Bernhard Hauer ,  Wolfgang Ladner ,  Uwe Pressler ,  Christoph Nubling

    IPC分类号： C12P13/02 ,  C12P41/00 ,  C12R1/38 ,  C07C231/02 ,  C07C231/16

    CPC分类号： C12P13/02 ,  C12P41/007

    摘要： A process for producing optically active primary and secondary amines from the corresponding racemates is characterised in that (a) a racemic amine is enantioselectively acylated in the presence of a hydrolase with an ester whose acid component bears a fluorine, nitrogen, oxygen or sulphur atom at the proximity of the carbonyl carbon atom; (b) the mixture of optically active amine and optically active acylated amine is separated so that an enantiomer of amine is produced; (c) if desired the other enantiomer of the amine is extracted from the acylated amine by amide cleavage.

    摘要翻译： PCT No.PCT / EP94 / 03102 Sec。 371日期：1996年3月11日 102（e）1996年3月11日PCT PCT 1994年9月16日PCT公布。 出版物WO95 / 08636 日期：1995年3月30日从相应的外消旋体制备光学活性伯胺和仲胺的方法的特征在于：（a）外消旋胺在水解酶存在下被对映选择性酰化，其中酸组分含有氟，氮， 在羰基碳原子附近的氧或硫原子; （b）分离光学活性胺和光学活性酰化胺的混合物，使得产生胺的对映异构体; （c）如果需要，胺的另一对映异构体通过酰胺裂解从酰化胺中提取。

    Process for producing n-acyl-acyloxy aromatic amines
    5.
    发明授权
    Process for producing n-acyl-acyloxy aromatic amines 失效
    制备正酰基 - 酰氧基芳族胺的方法

    公开(公告)号：US4665216A

    公开(公告)日：1987-05-12

    申请号：US710787

    申请日：1985-03-12

    申请人： Theodore Horlenko ,  James H. George

    发明人： Theodore Horlenko ,  James H. George

    IPC分类号： C07B61/00 ,  B01J27/00 ,  B01J27/16 ,  B01J31/00 ,  B01J31/04 ,  C07C67/00 ,  C07C231/00 ,  C07C231/10 ,  C07C231/12 ,  C07C231/14 ,  C07C231/16 ,  C07C233/16 ,  C07C233/25 ,  C07C233/27 ,  C07C69/017

    CPC分类号： C07C233/16

    摘要： A process is provided for producing N-acyl-acyloxy aromatic amine, such as 4-acetoxyacetanilide by reacting a hydroxy-aromatic ketoxime with a carboxylic acid anhydride, e.g. acetic anhydride, in the presence of phosphoric or oxalic acid as a Beckmann rearrangement catalyst. Preferably the ketoxime is prepared by reacting a hydroxy aromatic ketone such as 4-hydroxyacetophone with a hydroxyl amine salt, and the ketone is obtained by the Fries rearrangement of a phenolic ester, e.g. phenyl acetate or the Friedel-Crafts acylation of a phenolic compound, e.g. phenol, with an acylating agent, e.g. acetic acid.

    摘要翻译： 提供了通过使羟基 - 芳族酮肟与羧酸酐反应生成N-酰基酰氧基芳族胺如4-乙酰氧基乙酰苯胺的方法，例如， 乙酸酐，在磷酸或草酸存在下作为Beckmann重排催化剂。 优选地，酮肟通过羟基芳族酮如4-羟基乙睾酮与羟胺盐反应制备，并且酮通过酚酯的Fries重排获得。 苯基乙酸酯或Friedel-Crafts酰化酚类化合物，例如 苯酚，与酰化剂，例如 醋酸。

    PROCESS FOR PREPARING OPTICALLY PURE MILNACIPRAN AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
    7.
    发明申请
    PROCESS FOR PREPARING OPTICALLY PURE MILNACIPRAN AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS 审中-公开
    制备光敏米拉宁药物及其药物接受口服的方法

    公开(公告)号：US20120289744A1

    公开(公告)日：2012-11-15

    申请号：US13574775

    申请日：2010-12-20

    申请人： Ganesh Gurpur Pai ,  Arun Kanti Mandal ,  Kamlesh Jayantilal Ranbhan ,  Vikram Sarjerao Jagtap ,  Dayaghan Gangadhar Patil ,  Yuvraj Kashinath Zunjarrao

    发明人： Ganesh Gurpur Pai ,  Arun Kanti Mandal ,  Kamlesh Jayantilal Ranbhan ,  Vikram Sarjerao Jagtap ,  Dayaghan Gangadhar Patil ,  Yuvraj Kashinath Zunjarrao

    IPC分类号： C07C231/16 ,  C07C237/20

    CPC分类号： C07C231/20 ,  C07B2200/07 ,  C07C59/50 ,  C07C237/20 ,  C07C2601/02

    摘要： The present invention relates to an improved and commercially, viable process for the resolution of racemic cis milnacipran of formula I and its pharmaceutically acceptable salts of formula II. The present invention comprises using racemic cis milnacipran or its pharmaceutically acceptable salts as starting material, a low cost and commercially available resolving agent of formula III and industrially safe and economically low cost material such as water as a solvent. The said process results into optical isomers of racemic cis milnacipran having excellent optical purity without involving multiple crystallization steps. The present invention also comprises the concept of green chemistry as the invention works well with water as a solvent thereby minimizing the use of any other solvent. (Formular I and II should be inserted here) Wherein X is anion selected from Cl, Br, I, HSO4, Phosphate or organic acid (Formular III should be inserted here) *represent asymmetric centre Compound of formula III represent mandelic acid and its derivatives.

    摘要翻译： 本发明涉及用于拆分式I的外消旋顺式米那普仑及其药学上可接受的式II的盐的改进且商业上可行的方法。 本发明包括使用外消旋的顺式米那普仑或其药学上可接受的盐作为起始原料，低成本和市售的式III拆分剂和工业上安全和经济低成本的材料如水作为溶剂。 所述方法产生具有优异光学纯度的外消旋顺式米那普仑的光学异构体，而不涉及多个结晶步骤。 本发明还包括绿色化学的概念，因为本发明与水作为溶剂良好地工作，从而最小化任何其它溶剂的用途。 （此处应插入式I和II）其中X为选自Cl，Br，I，HSO4，磷酸盐或有机酸的阴离子（此处应插入式III）*表示式III的不对称中心化合物，表示扁桃酸及其衍生物 。

    Process for racemization of N-acetyl-(D)L-.alpha.-amino carboxylic acids
    10.
    发明授权
    Process for racemization of N-acetyl-(D)L-.alpha.-amino carboxylic acids 失效
    N-乙酰基 - （D）L-α-氨基羧酸外消旋化的方法

    公开(公告)号：US06080887A

    公开(公告)日：2000-06-27

    申请号：US95409

    申请日：1998-06-10

    申请人： Karlheinz Drauz ,  Michael Karrenbauer ,  Andreas Bommarius ,  Gunter Knaup

    发明人： Karlheinz Drauz ,  Michael Karrenbauer ,  Andreas Bommarius ,  Gunter Knaup

    IPC分类号： C07C231/16 ,  C07C233/47 ,  C07B55/00

    CPC分类号： C07C231/16

    摘要： With known methods of racemizing N-acetyl-D(L)-.alpha.-amino carboxylic acids in the non-aqueous state by heating them to temperatures above room temperatures, significant quantities of by-products are formed, especially acetyl dipeptides. By converting at least a proportion of the N-acetyl-D(L)-.alpha.-amino carboxylic acids to corresponding N-acetyl-D(L)-.alpha.-amino carboxylic acid salts before or during the heating, it is possible to increase the sojourn time of the educt which is to be racemized at higher temperatures without any evident increase in the quantity of by-product formed (in particular acetylated dipeptides). Also disclosed is the production of optically active amino acids by enzymatic splitting of racemic compounds.

    摘要翻译： 通过将N-乙酰基-D（L）-α-氨基羧酸在非水状态下外消旋加热到室温以上的已知方法，形成显着量的副产物，特别是乙酰二肽。 通过在加热之前或期间将至少一部分N-乙酰基-D（L）-α-氨基羧酸转化为相应的N-乙酰基-D（L）-α-氨基羧酸盐，可以增加 即将在更高的温度下外消旋的流出物的停留时间不会形成副产物（特别是乙酰化的二肽）的量的明显增加。 还公开了通过外消旋化合物的酶裂解生产光学活性氨基酸。