公开(公告)号：US08617864B2

公开(公告)日：2013-12-31

申请号：US13571248

申请日：2012-08-09

Applicant: Lorraine Joan Giver ,  Lisa Marie Newman ,  Emily Mundorff ,  Gjalt W. Huisman ,  Stephane J. Jenne ,  Jun Zhu ,  Behnaz Behrouzian ,  John H. Grate ,  James Lalonde

Inventor： Lorraine Joan Giver ,  Lisa Marie Newman ,  Emily Mundorff ,  Gjalt W. Huisman ,  Stephane J. Jenne ,  Jun Zhu ,  Behnaz Behrouzian ,  John H. Grate ,  James Lalonde

IPC: C12P1/00 ,  C12P7/62 ,  C12N9/02 ,  C12N9/04 ,  C12N1/20 ,  C07H21/04

CPC classification number: C12P13/002 ,  C07C253/30 ,  C12N9/0008 ,  C12P7/42 ,  C12P7/62 ,  C07C255/20

Abstract: The present disclosure provides ketoreductase enzymes having improved properties as compared to a naturally occurring wild-type ketoreductase enzyme. Also provided are polynucleotides encoding the engineered ketoreductase enzymes, host cells capable of expressing the engineered ketoreductase enzymes, method of using the engineered ketoreductase enzymes to synthesize a variety of chirally pure compounds, and the chirally pure compounds prepared therewith.

Abstract translation: 本公开提供与天然存在的野生型酮还原酶相比具有改善的性质的酮还原酶。 还提供了编码工程化酮还原酶的多核苷酸，能够表达工程化酮还原酶的宿主细胞，使用工程化酮还原酶合成各种手性纯化合物的方法，以及用其制备的手性纯化合物。

公开(公告)号：US20040006231A1

公开(公告)日：2004-01-08

申请号：US10411886

申请日：2003-04-11

Inventor： Robert Lee Bosch ,  Richard Joseph McCabe ,  Thomas Norman Nanninga ,  Robert Joseph Stahl

IPC: C07D215/12 ,  C07D209/04 ,  C07D27/416 ,  C07C255/11

CPC classification number: C07D207/416 ,  C07B41/02 ,  C07B2200/07 ,  C07C253/30 ,  C07C255/20 ,  C07C255/21 ,  C07D207/34 ,  Y02P20/55

Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.

Abstract translation: 描述了制备顺式-1,3-二醇的改进方法，其中用三烷基硼烷或二烷基烷氧基硼烷或三烷基硼烷和二烷基烷氧基硼烷的混合物处理β-羟基酮，然后回收和再利用烷基硼烷物质以转化另外的β 羟基酮与顺式-1,3-二醇反应。

公开(公告)号：US06344569B1

公开(公告)日：2002-02-05

申请号：US09674178

申请日：2001-01-02

Applicant: Masaru Mitsuda ,  Makoto Miyazaki ,  Kenji Inoue

Inventor： Masaru Mitsuda ,  Makoto Miyazaki ,  Kenji Inoue

IPC: C07D31906

CPC classification number: C07D319/06 ,  C07C253/14 ,  C07C255/20

Abstract: The present invention provides a process which can produce an important intermediate for the production of the HMG coenzyme A reductase inhibitor atrovastatin, 6-cyanomethyl-1,3-dioxane-4-acetic acid derivatives, with ease industrially and in good yields, wherein a 3,5-dihydroxy-6-halohexanoic acid derivative is used as the starting material, and which comprises cyanation by reaction with a cyanating agent for substitution of a cyano group for the halogen atom and an acetal formation reaction of the diol moiety with an acetal forming reagent in the presence of an acid catalyst.

Abstract translation: 本发明提供了一种能够在工业上以良好的产率生产HMG辅酶A还原酶抑制剂阿曲伐他汀，6-氰基甲基-1,3-二恶烷-4-乙酸衍生物的重要中间体的方法，其中a 使用3,5-二羟基-6-卤代己酸衍生物作为原料，其中包括通过与氰化剂反应以氰基取代卤素原子进行氰化和二醇部分与缩醛的缩醛形成反应 在酸催化剂存在下形成试剂。

公开(公告)号：US2730543A

公开(公告)日：1956-01-10

申请号：US16333150

申请日：1950-05-20

Applicant: MINNESOTA MINING & MFG

Inventor： RENDALL JOHN L ,  WILBUR PEARLSON

CPC classification number: C07C255/10 ,  C07C253/20 ,  C07C255/20

公开(公告)号：US2710302A

公开(公告)日：1955-06-07

申请号：US42143654

申请日：1954-04-06

Applicant: DU PONT

Inventor： HYSON ARCHIBALD M

IPC: C07B35/04 ,  C07C49/16

CPC classification number: C07C253/00 ,  C07C2601/14 ,  C07C255/20 ,  C07C255/46 ,  C07C255/17

公开(公告)号：US20080227635A1

公开(公告)日：2008-09-18

申请号：US11997224

申请日：2006-07-27

Applicant: Michael Hofmann ,  Henricus Maria Martinus Bastiaans ,  Jurgen Langewald ,  Hassan Oloumi-Sadeghi ,  Deborah L. Culbertson

Inventor： Michael Hofmann ,  Henricus Maria Martinus Bastiaans ,  Jurgen Langewald ,  Hassan Oloumi-Sadeghi ,  Deborah L. Culbertson

IPC: A01N25/34 ,  C07C233/00 ,  A01P7/04 ,  A01P5/00 ,  A01P7/02 ,  A01N37/18

CPC classification number: A01N37/34 ,  C07C255/19 ,  C07C255/20 ,  C07C255/21 ,  C07C317/44

Abstract: Dicyano alkanoic acid amides of formula (I), wherein R1 is H, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, or haloalkynyl; R2 is H, CN, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, alkoxy, or haloalkoxy; R3 and R4 are H, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, cycloalkenyl, halocycloalkenyl, or R3 and R4 together can be alkylene, haloalkylene, alkenylene or haloalkenylene; X is O or S; R5 and R6 are H, alkyl, optionally substituted with 1 to 3 groups CN, NO2, OH, NR7R8, alkoxy, haloalkoxy, alkylthio, haloalkylthio, cycloalkyl, halocycloalkyl and optionally substituted phenyl; or haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, NR7R8, alkoxycarbonyl, haloalkoxycarbonyl, alkenyloxycarbonyl, haloalkenyloxycarbonyl, alkylcarbonyl, haloalkylcarbonyl, R7R8N—C(═O)—, phenylcarbonyl, benzylcarbonyl or phenyl wherein phenylcarbonyl, benzylcarbonyl and phenyl are optionally substituted; or R5 and R6 are a saturated, partially unsaturated or unsaturated 5- to 6-membered heterocyclic radical which may contain 1 to 4 heteroatoms selected from oxygen, nitrogen and sulfur and which radical may be bonded via a carbonyl (C(═O)) linkage, and which radical is optionally substituted; R7, R8 are H, alkyl, haloalkyl, alkylcarbonyl, haloalkylcarbonyl, benzyl, phenyl, phenylcarbonyl, alkylsulfonyl, or haloalkylsulfonyl; or the enantiomers or diastereomers or salts thereof, processes for the preparation of compounds of formula (I), use of compounds of formula (I) for combating insects, acarids, or nematodes, and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites using compounds of formula (I).

公开(公告)号：US07034165B2

公开(公告)日：2006-04-25

申请号：US10211236

申请日：2002-08-05

Applicant: Jurgen Westermann ,  Johannes Platzek ,  Orlin Petrov

Inventor： Jurgen Westermann ,  Johannes Platzek ,  Orlin Petrov

IPC: C07D319/06 ,  C07F7/10 ,  C07C255/03

CPC classification number: C12P13/004 ,  C07C253/30 ,  C07C255/12 ,  C07C255/13 ,  C07C255/20 ,  C07D319/06 ,  C07F7/1804 ,  C12P41/004 ,  Y02P20/55

Abstract: The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothilone derivatives.

公开(公告)号：US20050197500A1

公开(公告)日：2005-09-08

申请号：US11119151

申请日：2005-04-29

Applicant: Robert Bosch ,  Richard McCabe ,  Thomas Nanninga ,  Robert Stahl

Inventor： Robert Bosch ,  Richard McCabe ,  Thomas Nanninga ,  Robert Stahl

IPC: C07B31/00 ,  C07B41/02 ,  C07C29/143 ,  C07C253/30 ,  C07C255/20 ,  C07C255/21 ,  C07D207/34 ,  C07D207/40 ,  C07D207/416 ,  C07D215/16 ,  C07D311/96

CPC classification number: C07D207/416 ,  C07B41/02 ,  C07B2200/07 ,  C07C253/30 ,  C07C255/20 ,  C07C255/21 ,  C07D207/34 ,  Y02P20/55

Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.

公开(公告)号：US20040259946A1

公开(公告)日：2004-12-23

申请号：US10483479

申请日：2004-08-12

Inventor： Tom Thomas Puthiaparampil ,  Acharya Poornaprajna ,  Chandrashekar Aswathanarayanappa ,  Madhavan Sridharan ,  Sambasivam Ganesh

IPC: A61K031/275 ,  A61K031/255 ,  C07C059/285 ,  C07C253/30

CPC classification number: C07F7/1892 ,  C07C67/31 ,  C07C253/30 ,  Y02P20/55 ,  C07C255/20 ,  C07C69/734

Abstract: In one aspect, the invention provides a process for the preparation of compounds of Formula I 1 wherein R1 is nullCN, nullOP, alkyl, aryl or heteroaryl; wherein P represents any suitable protecting group; and R2 is alkyl or aryl; by reacting a compound of Formula II 2 wherein R1 is nullCN, nullOP, alkyl, aryl or heteroaryl; wherein P represents any suitable protecting group; and R2 is alkyl or aryl; with a reducing agent (e.g. sodium borohydride) in the presence of a metal halid (e.g. CeCl3) or a metal alkoxid (e.g. Ti(OiPr)4).

Abstract translation: 一方面，本发明提供了制备式I化合物的方法，其中R 1是-CN，-OP，烷基，芳基或杂芳基; 其中P表示任何合适的保护基; R2是烷基或芳基; 其中R 1是-CN，-OP，烷基，芳基或杂芳基的式II化合物; 其中P表示任何合适的保护基; R2是烷基或芳基; 在金属卤化物（例如CeCl 3）或金属烷氧基（例如Ti（OiPr）4）的存在下还原剂（例如硼氢化钠）。

公开(公告)号：US20040063987A1

公开(公告)日：2004-04-01

申请号：US10673988

申请日：2003-09-30

Inventor： Johannes Bartek ,  Rudolf Fuchs ,  Stefan Hildbrand

IPC: C07C253/20

CPC classification number: C07C253/20 ,  C07C255/13 ,  C07C255/20

Abstract: A process for preparing 2-cyno-2-alkoxyacetamides of the formula: 1 where R1 is C1-16-alkyl or halogen-substituted C1-16-alkyl, wherein appropriate alkoxymalonamides of the general formula: 2 where R1 is as defined above, are reacted with a dehydrating agent and the reaction is stopped before the reaction continues to 2-cyano-2-alkoxyacetamides (I).

Abstract translation: 制备下式的2-噌啉-2-烷氧基乙酰胺的方法：其中R 1是C 1-6 - 烷基或卤素取代的C 1-6 - 烷基，其中适当的烷氧基丙二酰胺，其中R 1是 如上所述，与脱水剂反应，并且在反应继续进行2-氰基-2-烷氧基乙酰胺（I）之前停止反应。