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    Optical resolution of alkyl chroman-2-carboxylates
    2.
    发明授权
    Optical resolution of alkyl chroman-2-carboxylates 失效
    烷基色满-2-羧酸酯的光学拆分

    公开(公告)号：US5658796A

    公开(公告)日：1997-08-19

    申请号：US475007

    申请日：1995-06-07

    Applicant: Richard F. Rossi, Jr. ,  Charles M. Zepp ,  Donald L. Heefner

    Inventor： Richard F. Rossi, Jr. ,  Charles M. Zepp ,  Donald L. Heefner

    IPC: C07D311/66 ,  C12P41/00

    CPC classification number: C07D311/66 ,  C12P41/004 ,  Y10S435/881

    Abstract: Described herein is a process for resolving a racemic (C>3) alkyl (R, S) chroman-2-carboxylate compound useful as intermediates in the synthesis of optically pure pharmaceutical compounds is disclosed. The process utilizes a microbial enzyme derived from Serratia marcescens to catalyze the enantioselective hydrolysis of the (C>3) alkyl (S)-chroman-2-carboxylate enantiomer of the racemic mixture to its corresponding carboxylic acid at a faster rate than the R-enantiomer. An enantiomerically pure S-configured carboxylic acid is thereby formed which can undergo acidic esterification to provide an optically pure (C>3) alkyl (S)-chroman-2-carboxylate intermediate for subsequent pharmaceutical synthesis. The nonhydrolyzed (C>3) alkyl (R)-chroman-2-carboxylate enantiomer can also be isolated to provide an optically pure pharmaceutical precursor.

    Abstract translation: 本文描述了一种拆分用作光学纯药物化合物合成中的中间体的外消旋（C 3）烷基（R 3，S）色满-2-羧酸酯化合物的方法。 该方法利用来自粘质沙雷氏菌的微生物酶催化外消旋混合物的（C 3）烷基（S） - 苯并二氢吡喃-2-羧酸酯对映异构体对映体选择性水解速率比R- 对映体。 由此形成对映异构体纯的S-构型的羧酸，其可进行酸性酯化以提供用于随后的药物合成的光学纯的（C 3）烷基（S） - 苯并二氢吡喃-2-羧酸酯中间体。 也可以分离非水解（C 3）烷基（R） - 苯并二氢吡喃-2-羧酸酯对映异构体以提供光学纯的药物前体。

    Methods for preparing captopril and its analogues
    4.
    发明授权
    Methods for preparing captopril and its analogues 失效
    卡托普利及其类似物的制备方法

    公开(公告)号：US5166361A

    公开(公告)日：1992-11-24

    申请号：US766958

    申请日：1991-09-25

    Applicant: Charles M. Zepp

    Inventor： Charles M. Zepp

    IPC: C07D205/04 ,  C07D207/16 ,  C07D211/60

    CPC classification number: C07D205/04 ,  C07D207/16 ,  C07D211/60

    Abstract: This invention relates to novel methods for converting a diastereomeric mixture of S-protected derivatives of an orally active inhibitor of an angiotensin-converting enzyme (ACE) and its analogues into its separate optically resolved diastereomeric components. Specifically the invention relates to methods for the preparation of optically purified captopril and its analogs from racemic precursors. This resolution process is achieved through the fractional crystallization of S-protected derivatives of captopril and its precursors, which derivatives are useful for the reason that they are (1) easily prepared from novel precursors, (2) resolvable to their optically purified stereoisomeric species and (3) convertible to non-derivatized stereoisomeric species which correspond to the pharmacologically active inhibitor and its analogues. Novel methods for preparing the derivatives and their precursors are also noted herein. In addition, the novel derivatives and their precursors are also described herein.

    Abstract translation: 本发明涉及将血管紧张素转换酶（ACE）的口服活性抑制剂的S-保护衍生物与其类似物的非对映异构体混合物转化成其单独的光学拆分的非对映体组分的新方法。 具体地说，本发明涉及从外消旋前体制备光学纯化的卡托普利及其类似物的方法。 该解决方法是通过巯基及其前体的S-保护衍生物的分级结晶来实现的，该衍生物是有用的，因为它们是（1）容易地由新型前体制备，（2）可分解成其光学纯化的立体异构物质， （3）可转化成对应于药理活性抑制剂及其类似物的非衍生化立体异构体。 本文还注意到制备衍生物及其前体的新方法。 此外，本文还描述了新的衍生物及其前体。

    Image dye-providing materials
    5.
    发明授权
    Image dye-providing materials 失效
    图像染料提供材料

    公开(公告)号：US4619784A

    公开(公告)日：1986-10-28

    申请号：US200953

    申请日：1980-10-27

    Applicant: Louis Locatell, Jr. ,  Charles M. Zepp ,  Ronald F. Cieciuch

    Inventor： Louis Locatell, Jr. ,  Charles M. Zepp ,  Ronald F. Cieciuch

    IPC: C07D209/08 ,  C07D223/16 ,  C09B11/24 ,  C09B11/28 ,  G03C8/10 ,  C07D209/12 ,  C07D215/14

    CPC classification number: C07D223/16 ,  C07D209/08 ,  C09B11/24 ,  C09B11/28 ,  G03C8/10

    Abstract: There are disclosed diffusion transfer color processes and products which employ novel image dye-providing materials which provide image dyes having the chromophoric system represented by the formula ##STR1## X is H, alkyl, aryl or substituted aryl; W is H or alkyl, R is H or alkyl; m and n are each integers of from 2 to 6.The image dye-providing material includes a diffusion control moiety such as a hydroquinonyl group and may be diffusible or nondiffusible as a function of the diffusion control moiety.

    Abstract translation: 公开了扩散转移色彩工艺和产品，其使用提供具有由下式表示的发色体系的图像染料提供材料：X是H，烷基，芳基或取代的芳基; W是H或烷基，R是H或烷基; m和n各自为2至6的整数。图像染料提供材料包括扩散控制部分如氢醌基，并且作为扩散控制部分的函数可以是可扩散的或不可扩散的。

    Methods and apparatus for rendering an optically encoded medium unreadable
    7.
    发明授权
    Methods and apparatus for rendering an optically encoded medium unreadable 失效
    用于渲染光学编码介质的方法和装置不可读

    公开(公告)号：US06338933B1

    公开(公告)日：2002-01-15

    申请号：US09338959

    申请日：1999-06-24

    Applicant: Nabil M. Lawandy ,  Charles M. Zepp ,  Kenneth S. Norland

    Inventor： Nabil M. Lawandy ,  Charles M. Zepp ,  Kenneth S. Norland

    IPC: G11B370

    CPC classification number: G11B20/00086 ,  G11B7/252 ,  G11B7/2534 ,  G11B7/2542 ,  G11B7/2575 ,  G11B7/2585 ,  G11B20/00797 ,  G11B23/282 ,  G11B23/505 ,  Y10S430/146

    Abstract: Methods and apparatus are provided for making an optically readable media unreadable. The method includes steps of (a) providing the media with an optically activated mechanism that degrades the reflectivity of a surface wherein information is encoded; (b) exposing the media to optical radiation for reading out the information; and, during the step of exposing, (c) initiating the operation of the optically activated mechanism. In this embodiment the step of initiating includes steps of (d) generating singlet oxygen in a layer disposed on the media; and (e) reacting the singlet oxygen with a metal-containing layer for oxidizing the surface of the metal-containing layer, thereby degrading the reflectivity of the surface. In a further aspect the optically activated mechanism causes a defocusing of a readout beam, thereby degrading reflection of the readout beam from a surface wherein information is encoded. In another embodiment the method deforms a surface of the layer resulting in readout beam aberration or in an inability to correctly stay on track. In another embodiment a portion of the surface is removed to the atmosphere, such as by evaporation of sublimation. In this embodiment a layer of the media is comprised of a volatile component and at least one other component. Removing at least some of volatile component by evaporation or sublimation causes an increase in at least one of photoabsorption or scattering or surface roughness with the remaining component, thereby rendering at least a portion of encoded information of the media unreadable, or affecting the tracking operation.

    Abstract translation: 提供了用于使光可读介质不可读的方法和装置。 该方法包括以下步骤：（a）向介质提供光学激活机制，其降低其中信息被编码的表面的反射率; （b）将介质暴露于光学辐射以读出信息; 并且在曝光步骤期间，（c）启动光学激活机构的操作。 在该实施方案中，起始步骤包括（d）在设置在介质上的层中产生单线态氧的步骤; 和（e）使单线态氧与含金属层反应，以使含金属层的表面氧化，从而降低表面的反射率。 在另一方面，光学激活的机构导致读出光束的散焦，从而降低读出光束从其中信息被编码的表面的反射。 在另一个实施例中，该方法使层的表面变形，导致读出光束像差或不能正确地保持轨道。 在另一个实施例中，表面的一部分被移除到大气中，例如通过蒸发升华。 在该实施例中，介质层由挥发性组分和至少一种其它组分组成。 通过蒸发或升华去除至少一些挥发性组分导致与剩余组分的光吸收或散射或表面粗糙度中的至少一种的增加，从而使得介质的编码信息的至少一部分不可读或影响跟踪操作。

    Method for membrane reactor resolution of stereoisomers
    10.
    发明授权
    Method for membrane reactor resolution of stereoisomers 失效
    立体异构体的膜反应器拆分方法

    公开(公告)号：US5077217A

    公开(公告)日：1991-12-31

    申请号：US178743

    申请日：1988-04-07

    Applicant: Stephen L. Matson ,  Stephen A. Wald ,  Charles M. Zepp ,  David R. Dodds

    Inventor： Stephen L. Matson ,  Stephen A. Wald ,  Charles M. Zepp ,  David R. Dodds

    IPC: B01J19/24 ,  C07C219/10 ,  C07C305/04 ,  C07C305/10 ,  C07C309/65 ,  C07C309/66 ,  C07C327/32 ,  C07F9/09 ,  C12M1/40 ,  C12N11/02 ,  C12N11/08 ,  C12P1/00 ,  C12P7/40 ,  C12P7/64 ,  C12P13/06 ,  C12P17/12 ,  C12P41/00

    CPC classification number: C12N11/02 ,  B01J19/2475 ,  C07C219/10 ,  C07C305/04 ,  C07C305/10 ,  C07C309/65 ,  C07C309/66 ,  C07C327/32 ,  C07F9/091 ,  C12M21/18 ,  C12M25/02 ,  C12M29/04 ,  C12M29/16 ,  C12N11/08 ,  C12P1/00 ,  C12P41/00 ,  C12P41/005 ,  C12P7/40 ,  B01J2219/00159 ,  B01J2219/00162 ,  B01J2219/00177

    Abstract: This invention relates to novel methods for facilitating the enzymatic resolution of racemic mixtures of esters, which are derivatized with groups which enhance the esters' aqueous solubility, in an extractive member reactor where the enzyme is placed alternatively either (1) in the aqueous phase, (2) in association with the membrane, or (3) in the aqueous phase and in association with the membrane, wherein the aqueous ester phase is contacted with one side of the membrane, and where an organic extractive phase is contacted with the other side of the membrane, wherein the extractive phase serves to remove the resolving reaction product. Of particular significance regarding this invention is its use of water soluble esters that are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment. Novel methods were utilized to prepare these esters, for use in this invention's methods for enzymatically resolving the racemic mixtures of the esters, to produce the separate chiral isomers of the racemic mixture. The importance of the resolution of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities.

    Abstract translation: 本发明涉及用于促进酯的外消旋混合物的酶拆分的新方法，其在提取成分反应器中被提取酯水溶性的基团衍生化，其中酶在水相中置换为（1） （2）与膜结合，或（3）在水相中并与膜结合，其中酯水相与膜的一侧接触，并且其中有机萃取相与另一侧接触 的膜，其中萃取相用于除去拆分的反应产物。 对于本发明具有特别意义的是其使用水溶性酯，其用增强其水溶性的基团衍生化，并且它们与在水性环境中介导的酶拆分方法的反应性。 使用新的方法制备这些酯，用于本发明的用于酶拆分酯的外消旋混合物的方法，以产生外消旋混合物的分离的手性异构体。 拆分外消旋混合物的单独手性异构体的重要性在于分离经常具有不同生物活性的异构体。

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