公开(公告)号：US5070022A

公开(公告)日：1991-12-03

申请号：US288216

申请日：1988-12-22

申请人： David L. Hughes ,  Paul J. Reider ,  Joseph S. Amato ,  James J. Bergan ,  Edward J. J. Grabowski

发明人： David L. Hughes ,  Paul J. Reider ,  Joseph S. Amato ,  James J. Bergan ,  Edward J. J. Grabowski

IPC分类号： C07D215/12 ,  C07D215/18 ,  C12P17/12 ,  C12P41/00

CPC分类号： C12P17/12 ,  C12P41/005

摘要： Disclosed is a process for preparing the R and S enantiomers of a compound of the formula; ##STR1## which comprises; (1) reacting an enzyme with a prochiral diester of the formula ##STR2## where M.sup.1 and M.sup.2 are the same, to produce a chiral monoester of the compound of formula II;(2) treating the chiral monoester product of step (1) with an amine and a trialkyl aluminum compound to produce the R enantiomer of the compound of formula I; or reacting the chiral monoester product of step (1) with an acid activating agent, an amine, and a base to produce the S enantiomer of the compound of formula I.In the alternative the R enantiomer of the compound of formula I may be synthesized by direct enzymatic hydrolysis of the racemic mixture of a compound having the formula ##STR3##

公开(公告)号：US4894450A

公开(公告)日：1990-01-16

申请号：US48341

申请日：1987-05-11

申请人： Edward J. J. Grabowski ,  David L. Hughes

发明人： Edward J. J. Grabowski ,  David L. Hughes

IPC分类号： C07D477/02 ,  C07F9/6561

CPC分类号： C07F9/65611 ,  C07D477/02

摘要： This invention relates to a process for preparing 2-(aminoalkylthio)carbapenems. In particular, this invention relates to a process in which a bis(substituted phenyl) phosphorohalidate is used to form an enol phosphate intermediate that can be converted to 2-(aminoalkylthio)carbapenems by reaction with suitable thioalkylamines.

公开(公告)号：US06994024B2

公开(公告)日：2006-02-07

申请号：US10667904

申请日：2003-09-16

申请人： Kevin L. Corcoran ,  David L. Hughes

发明人： Kevin L. Corcoran ,  David L. Hughes

IPC分类号： B31F1/07

CPC分类号： B31F1/07 ,  B31F2201/0702

摘要： Disclosed is an embossing system to be used with a die press. The embossing system includes a force transfer assembly, which comprises a first cover and an opposite second cover with the first and second covers being connected by a hinge. The force transfer assembly further includes a stencil and an opposing form positioned internal of the force transfer assembly. The stencil and the form are adapted to sandwich an embossing material, such as paper, between the stencil and the form. The embossing system further includes a layer of static vinyl that is located internally of one of the covers to secure the form to the internal side of one of the covers. The embossing system also utilizes an adhesive located on the cover opposite the cover with the vinyl to secure the stencil to the internal side of the opposite cover.

摘要翻译： 公开了一种与压模一起使用的压花系统。 压花系统包括力传递组件，其包括第一盖和相对的第二盖，其中第一和第二盖通过铰链连接。 力传递组件还包括位于力传递组件内部的模版和相对的形状。 模板和模板适于在模板和模板之间夹住诸如纸的压花材料。 压花系统还包括一层静电乙烯基，其位于一个盖的内部，以将形式固定在其中一个盖的内侧。 压花系统还使用位于盖子上的与乙烯基相反的盖子上的粘合剂将模板固定到相对的盖子的内侧。

公开(公告)号：US5340927A

公开(公告)日：1994-08-23

申请号：US846725

申请日：1992-03-02

申请人： David L. Hughes

发明人： David L. Hughes

IPC分类号： C07F7/18 ,  C07C245/18

CPC分类号： C07F7/188 ,  C07F7/1852

摘要： A novel process for preparing 2-diazo-3-trisubstituted silyloxy-3-butenoates, synthons useful in the conversion of 3-substituted-4-acetoxy azetidinones and penicillin to thienamycin, imipenem and other carbapenem antibiotic compounds is provided, comprising the reaction of the appropriate diazo acetoacetate with the substituted silane, base and salt.

摘要翻译： 提供了一种用于制备2-重氮-3-三取代的甲硅烷氧基-3-丁烯酸酯的新方法，可用于将3-取代-4-乙酰氧基氮杂环丁酮和青霉素转化成硫霉素，亚胺培南和其他碳青霉烯类抗生素化合物的合成物，其包括 适当的重氮乙酰乙酸酯与取代的硅烷，碱和盐。

公开(公告)号：US5126456A

公开(公告)日：1992-06-30

申请号：US777979

申请日：1991-10-17

申请人： Zhiguo Song ,  David L. Hughes

发明人： Zhiguo Song ,  David L. Hughes

IPC分类号： C07B61/00 ,  C07D215/18 ,  C07D215/50 ,  C07D217/02

CPC分类号： C07D215/18

摘要： An improved process is described which utilizes tetrachloro-1,4(or 1,2)-quinone as an oxidant in the Doebner-Miller synthesis of 7-chloroquinaldine, a starting material in the preparation of leukotriene antagonists. The process improves yield and eliminates the need of forming a ZnCl.sub.2 complex to isolate the end product.

公开(公告)号：US06333435B1

公开(公告)日：2001-12-25

申请号：US08443616

申请日：1995-05-18

申请人： Dongwei Cai ,  David L. Hughes ,  Sylvain Levac ,  Thomas R. Verhoeven

发明人： Dongwei Cai ,  David L. Hughes ,  Sylvain Levac ,  Thomas R. Verhoeven

IPC分类号： C07F902

CPC分类号： C07F9/5027

摘要： A process of synthesizing a compound of the formula 1: is disclosed, which comprises reacting a compound of the formula 2: with diphenylphosphine in the presence of an amine base and a nickel catalyst to produce a compound of formula 1.

摘要翻译： 公开了合成式1化合物的方法，其包括使式2化合物与二苯基膦在胺碱和镍催化剂的存在下反应以制备式1化合物。

公开(公告)号：US06262268B1

公开(公告)日：2001-07-17

申请号：US09709083

申请日：2000-11-09

申请人： Michael Palucki ,  David L. Hughes ,  Chunhua Yang ,  Nobuyoshi Yasuda

发明人： Michael Palucki ,  David L. Hughes ,  Chunhua Yang ,  Nobuyoshi Yasuda

IPC分类号： C07D21338

CPC分类号： C07D213/40 ,  C07D213/38 ,  C07D471/04

摘要： A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.

摘要翻译： 提供了一种制备3-（5,6,7,8-四氢 - [1,8] - 萘啶-2-基） - 丙胺的新方法，其可用于合成αphav整联蛋白受体拮抗剂。 还提供了从该方法获得的有用的中间体。

公开(公告)号：US4654433A

公开(公告)日：1987-03-31

申请号：US691086

申请日：1985-01-14

申请人： David L. Hughes

发明人： David L. Hughes

IPC分类号： A61K20060101 ,  C07C20060101 ,  C07C101/77

CPC分类号： C07C227/18

摘要： A simple single step process for preparing alkyl and substituted alkyl esters of amino acids is described. The products are bioactive compounds including compounds useful as antihypertensive agents.

摘要翻译： 描述了用于制备氨基酸的烷基和取代的烷基酯的简单的单步方法。 该产品是包括可用作抗高血压剂的化合物的生物活性化合物。

公开(公告)号：US5892082A

公开(公告)日：1999-04-06

申请号：US813193

申请日：1997-03-07

申请人： Dongwei Cai ,  Ian F. Cottrell ,  David L. Hughes ,  Joseph F. Payack

发明人： Dongwei Cai ,  Ian F. Cottrell ,  David L. Hughes ,  Joseph F. Payack

IPC分类号： B01J31/00 ,  B01J31/22 ,  C07F7/28 ,  C07F17/00 ,  C07F13/00

CPC分类号： B01J31/2295 ,  C07F17/00 ,  B01J2231/14 ,  B01J2231/4205 ,  B01J2531/46

摘要： The present invention is directed to a process for the preparation of the reagent dimethyl titanocene (Cp.sub.2 Ti(CH.sub.3).sub.2) from titanocene dichloride (Cp.sub.2 TiCl.sub.2) and a methyl magnesium halide, in particular, methyl magnesium chloride (CH.sub.3 MgCl). The instant process provides the desired reagent in a manner which is generally less hazardous and more economical than previous methods.

摘要翻译： 本发明涉及二氯二茂钛（Cp2TiCl2）和甲基卤化镁，特别是甲基氯化镁（CH3MgCl）制备试剂二甲基二茂钛（Cp2Ti（CH3）2）的方法。 本方法以通常危险性较低且比以前方法更经济的方式提供所需试剂。

公开(公告)号：US5552521A

公开(公告)日：1996-09-03

申请号：US386618

申请日：1995-02-10

申请人： Kevin M. Belyk ,  Dean R. Bender ,  Regina M. Black ,  David L. Hughes ,  William Leonard

发明人： Kevin M. Belyk ,  Dean R. Bender ,  Regina M. Black ,  David L. Hughes ,  William Leonard

IPC分类号： A61B17/04 ,  A61B17/06 ,  A61K38/00 ,  A61P31/04 ,  A61P31/12 ,  A61P37/04 ,  C07K1/06 ,  C07K1/107 ,  C07K7/56 ,  C07K7/64

CPC分类号： C07K7/56 ,  A61B17/06133 ,  A61B2017/06142 ,  Y10S930/27

摘要： There is disclosed a novel process for preparing aza cyclohexapeptides of the formula ##STR1## where all variables are defined herein.

摘要翻译： 公开了一种制备式（I）的氮杂环己肽的新方法，其中所有变量在本文中定义。