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1. 发明授权

US06376685B1 Process for producing optically active threo-3-amino-1,2-epoxy compounds 失效
标题翻译：光学活性苏氨酸-3-氨基-1,2-环氧化合物的制备方法
公开(公告)号：US06376685B1
公开(公告)日：2002-04-23
申请号：US09600215
申请日：2000-07-12
申请人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
发明人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
IPC分类号： C07D30102
CPC分类号： C07C303/28 , C07D303/36 , C07C309/66
摘要： Highly pure optically active threo-3-amino-1,2-epoxy compounds appropriate for materials for manufacturing drugs and a process for producing the same on an industrial scale. An optically active threo-3-amino-1,2-diol derivative is subjected in an organic solvent in the presence of a base to alkylsufonylation or arylsulfonylation to thereby give the corresponding optically active threo-3-amino-2-hydroxy-1-sulfonyloxy compound. Next, the resultant product is subjected to epoxidation in the presence of a base to give the corresponding optically active threo-3-amino-1,2-epoxy compound. The thus obtained epoxy compound is purified by using an organic solvent and water, thus giving a highly pure epoxy compound.
摘要翻译：适用于制造药物的材料的高纯度旋光活性苏氨酸-3-氨基-1,2-环氧化合物及其制备方法。光学活性的苏氨酸-3-氨基-1,2-二醇衍生物在碱的存在下在有机溶剂中进行烷基磺酰化或芳基磺酰化，得到相应的光学活性的苏氨酸-3-氨基-2-羟基-1- 磺酰氧基化合物。接着，将所得产物在碱的存在下进行环氧化，得到相应的光学活性的苏氨酸-3-氨基-1,2-环氧化合物。由此获得的环氧化合物通过使用有机溶剂和水进行纯化，从而得到高纯度的环氧化合物。

2. 发明授权

US06693205B2 Process for preparing optically active epoxides 失效
标题翻译：光学活性环氧化物的制备方法
公开(公告)号：US06693205B2
公开(公告)日：2004-02-17
申请号：US10332608
申请日：2003-01-10
申请人： David Edward Justice
发明人： David Edward Justice
IPC分类号： C07D30102
CPC分类号： C07D301/24 , C07D303/36
摘要： The invention concerns a process for the production of optically active epoxides useful as pharmaceutical intermediates, particularly in the field of HIV protease inhibitors. The optically active epoxides are produced in commercially acceptable yields from an optically active alcohols by a Mitsunobu reaction and a cyclisation step, preferably comprising an intermediate re-crystallisation step. The stereochemistry of the alcohol is inverted during the Mitsunobu reaction to produce the desired epoxide.
摘要翻译：本发明涉及生产用作药物中间体的光学活性环氧化物的方法，特别是在HIV蛋白酶抑制剂领域。光学活性环氧化物以光学活性醇的商业上可接受的产率通过Mitsunobu反应和环化步骤制备，优选包括中间重结晶步骤。在Mitsunobu反应期间醇的立体化学反转以产生所需的环氧化物。

3. 发明授权

US06509485B2 Preparation of epoxides from alkanes using lanthanide-promoted silver catalysts 失效
公开(公告)号：US06509485B2
公开(公告)日：2003-01-21
申请号：US09792390
申请日：2001-02-22
申请人： Guido Mul , Marianna F. Asaro , Albert S. Hirschon , Robert B. Wilson, Jr.
发明人： Guido Mul , Marianna F. Asaro , Albert S. Hirschon , Robert B. Wilson, Jr.
IPC分类号： C07D30102
CPC分类号： C07D301/22 , B01J23/002 , B01J23/66 , B01J23/685
摘要： A process is provided for use in the conversion of alkanes into alkylene oxides, having particular utility in the conversion of propane to form propylene oxide, using a lanthanide-promoted, supported, silver catalyst prepared via precipitation. A preferred embodiment uses silver nitrate and lanthanum nitrate to form the catalyst on a BaCO3 support.

4. 发明授权

US06399793B1 Process for the preparation of &agr;' chloroketones 有权
公开(公告)号：US06399793B1
公开(公告)日：2002-06-04
申请号：US09908516
申请日：2001-07-18
申请人： David Kronenthal , Mark D. Schwinden
发明人： David Kronenthal , Mark D. Schwinden
IPC分类号： C07D30102
CPC分类号： C07C269/06 , C07C221/00 , C07D303/36 , C07C271/18
摘要： The present invention relates to a process for the preparation of &agr;′ chloroketones, such as 4-phenyl-3-t-butyloxy-carbonylamino)-2-keto-1-chlorobutane by reacting certain aryl amino acid esters, e.g. N-(2-t-butoxycarbonyl)-L-phenylalanine-4-nitrophenyl ester, with a sulfur ylide compound to form the corresponding keto ylide compound which is then treated with a source of chloride and an organic acid.

5. 发明授权

US06812357B2 Method for producing epoxides by oxidizing olefins 失效
标题翻译：通过氧化烯烃生产环氧化物的方法
公开(公告)号：US06812357B2
公开(公告)日：2004-11-02
申请号：US10363170
申请日：2003-09-05
申请人： Torsten Berndt , Olaf Boege , Jost Heintzenberg
发明人： Torsten Berndt , Olaf Boege , Jost Heintzenberg
IPC分类号： C07D30102
CPC分类号： C07D301/14 , C07D301/12
摘要： The invention relates to a new method for producing epoxides by oxidizing olefins in a homogeneous gas phase reaction, wherein ozone and NO2 and/or NO are reacted with the desired olefin under mild reaction conditions and without a catalyst. The inventive method can be carried out as a continuous, one-step method in a reactor according to FIG. 1, and requires very little technical input. Monoolefins having 2 to 16 carbon atoms and diolefins having 4 to 16 carbon atoms can be epoxidized.
摘要翻译：本发明涉及一种通过在均匀气相反应中氧化烯烃来生产环氧化物的新方法，其中在温和的反应条件下和无催化剂下，臭氧和NO 2和/或NO与所需的烯烃反应。本发明的方法可以作为连续的一步法在根据图1的反应器中进行。 1，需要很少的技术投入。具有2至16个碳原子的单烯烃和具有4至16个碳原子的二烯烃可以被环氧化。

6. 发明授权

US06559323B1 Process for the preparation of an oxirane, aziridine or cyclopropane 失效
标题翻译：制备环氧乙烷，氮丙啶或环丙烷的方法
公开(公告)号：US06559323B1
公开(公告)日：2003-05-06
申请号：US09423428
申请日：2000-02-28
申请人： John Richard Studley , Varinder Kumar Aggarwal
发明人： John Richard Studley , Varinder Kumar Aggarwal
IPC分类号： C07D30102
CPC分类号： C07D303/22 , C07D203/02 , C07D301/02 , C07D303/04 , C07D303/08 , C07D303/46 , C07D327/06 , C07D333/54 , C07D333/78 , C07D405/04 , C07D495/08 , Y10S436/903
摘要： A process for the preparation of an oxirane, aziridine or cyclopropane of formula (I), wherein X is oxygen, NR4 or CHR5; R1 is hydrogen, alkyl, aryl, heteroaromatic, heterocyclic or cycloalkyl; R2 is hydrogen, alkyl, aryl, heteroaromatic, CO2R8, CHR14NHR13, heterocyclic or cycloalkyl; or R1 and R2 join together to form a cycloalkyl ring; R3 and R10 are, independently, hydrogen, alkyl, aryl, heteroaromatic, CO2R8, R83Sn, CONR8R9, trialkylsilyl or triarylsilyl; R4 is an electron withdrawing group; R5 is alkyl, cycloalkyl, aryl, heteroaromatic, SO2R8, SO3R8, COR8, CO2R8, CONR8R9, PO(R8)2, PO(OR8)2 or CN; R8 and R9 are independently alkyl or aryl; and R13 and R14 are independently hydrogen, alkyl or aryl is provided. The process comprises degrading a compound of formula (II), (IIa), (IIb) or (IIc): wherein R3 and R10 are as defined above; Y is a cation; depending on the nature of Y, r is 1 or 2; and L is a suitable leaving group, to form a diazo compound. The diazo compound is reacted with a suitable transition metal catalyst, and the product thereof reacted with a sulphide of formula SR6R7, wherein R6 and R7 are independently alkyl, aryl or heteroaromatic, or R6 and R7 join together to form an optionally substituted ring which optionally includes an additional heteroatom. This product is then reacted with an aldehyde, ketone, imine or alkene.
摘要翻译：制备式（I）的环氧乙烷，氮丙啶或环丙烷的方法，其中X是氧，NR 4或CHR 5; R 1是氢，烷基，芳基，杂芳族，杂环或环烷基; R2是氢，烷基，芳基，杂芳族，CO2R8，CHR14NHR13，杂环或环烷基; 或R 1和R 2连接在一起形成环烷基环; R 3和R 10独立地是氢，烷基，芳基，杂芳族，CO 2 R 8，R 83 Sn，CONR 8 R 9，三烷基甲硅烷基或三芳基甲硅烷基; R4是吸电子基团; R5是烷基，环烷基，芳基，杂芳族，SO2R8，SO3R8，COR8，CO2R8，CONR8R9，PO（R8）2，PO（OR8）2或CN; R8和R9独立地是烷基或芳基; R 13和R 14独立地为氢，提供烷基或芳基。该方法包括降解式（II），（IIa），（IIb）或（IIc）化合物：其中R 3和R 10如上所定义; Y是阳离子; 取决于Y的性质，r为1或2; 并且L是合适的离去基团，以形成重氮化合物。将重氮化合物与合适的过渡金属催化剂反应，其产物与式SR6R7的硫化物反应，其中R 6和R 7独立地为烷基，芳基或杂芳族，或R 6和R 7连接在一起形成任选取代的环，包括另外的杂原子。然后将该产物与醛，酮，亚胺或烯烃反应。

7. 发明授权

US06353122B1 Method for epoxidation of 3-methylenecyclopropanes 失效
标题翻译： 3-亚甲基环丙烷的环氧化方法
公开(公告)号：US06353122B1
公开(公告)日：2002-03-05
申请号：US09018425
申请日：1998-02-04
申请人： Paul R. Brodfuehrer , Thomas R. Sattleberg, Sr.
发明人： Paul R. Brodfuehrer , Thomas R. Sattleberg, Sr.
IPC分类号： C07D30102
CPC分类号： C07F7/1892 , C07C67/293 , C07D301/02 , C07D303/16 , C07F7/1804 , C07C69/78
摘要： The present invention provides a process for the expoxidation of a protected 3-methylene-(trans)-1,2,-hydroxymethylcyclopropane with cyclohexanone and potassium peroxymonosulfate and subsequent rearrangement to provide the corresponding cyclobutanone.
摘要翻译：本发明提供了用环己酮和过氧化硫酸钾过氧化被保护的3-亚甲基 - （反）-1,2 - 羟甲基环丙烷的方法，随后重排以提供相应的环丁酮。

8. 发明授权

US06570027B2 Method of preparing intermediates useful in synthesis of retroviral protease inhibitors 失效
公开(公告)号：US06570027B2
公开(公告)日：2003-05-27
申请号：US10114313
申请日：2002-04-03
申请人： John S Ng , Claire A. Przybyla , Richard A Mueller , Michael L Vazquez , Daniel P Getman
发明人： John S Ng , Claire A. Przybyla , Richard A Mueller , Michael L Vazquez , Daniel P Getman
IPC分类号： C07D30102
CPC分类号： C07K5/06191 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/216 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C04B35/632 , C07B2200/07 , C07C213/00 , C07C213/02 , C07C213/08 , C07C269/06 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D303/36 , C07D307/85 , C07D401/12 , C07K5/0207 , C07K5/021 , C07K5/06026 , C07K5/06139 , C07C215/08 , C07C215/28 , C07C271/16
摘要： A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.

9. 发明授权

US06409769B1 Kinetic resolution of olefins 失效
标题翻译：烯烃的动力学拆分
公开(公告)号：US06409769B1
公开(公告)日：2002-06-25
申请号：US09673335
申请日：2000-12-04
申请人： Yian Shi
发明人： Yian Shi
IPC分类号： C07D30102
CPC分类号： C07D303/22 , C07B53/00 , C07B57/00 , C07B2200/07 , C07D301/14 , C07D303/04 , C07D303/16 , C07D303/40 , C07H9/04
摘要： A method for kinetically resolving a stereoisomer mixture of compounds using asymmetric epoxidation is provided. Compounds contain an olefin moiety providing one stereoisomer to be epoxidized at a higher rate than the other stereoisomer using a chiral ketone and an oxidizing agent.
摘要翻译：提供了使用不对称环氧化反应动力学拆分化合物的立体异构体混合物的方法。化合物含有使用手性酮和氧化剂以比其它立体异构体更高的速率环氧化的一种立体异构体的烯烃部分。

10. 发明授权

US06344572B1 Processes for the preparation of threo-1,2-epoxy-3-amino-4-phenylbutane derivatives 有权
标题翻译：制备苏式-1,2-环氧-3-氨基-4-苯基丁烷衍生物的方法
公开(公告)号：US06344572B1
公开(公告)日：2002-02-05
申请号：US09647340
申请日：2000-11-17
申请人： Katsuji Maehara , Yukinori Tokuda , Hiroshi Murao , Yasuyoshi Ueda
发明人： Katsuji Maehara , Yukinori Tokuda , Hiroshi Murao , Yasuyoshi Ueda
IPC分类号： C07D30102
CPC分类号： C07D301/26 , C07D303/36
摘要： The present invention provides a production method of high quality threo-1,2-epoxy-3-amino-4-phenylbutane derivatives (1) on a commercial scale in a simple, easy and efficient manner and with very high productivity, which comprises treating a threo-1-halo-2-hydroxy-3-amino-4-phenylbutane derivative (2) with a base in a polar organic solvent or a solvent composed of a polar organic solvent and water, and adding the resulting reaction mixture to water to thereby cause the resulting threo-1,2-epoxy-3-amino-4-phenylbutane derivative (1) to crystallize out.
摘要翻译：本发明以简单，容易和有效的方式以非常高的生产率提供了高质量的threo-1,2-epoxy-3-氨基-4-苯基丁烷衍生物（1）的制备方法，其包括处理在极性有机溶剂或由极性有机溶剂和水组成的溶剂中的碱，将苏-1-卤代-2-羟基-3-氨基-4-苯基丁烷衍生物（2）与碱反应，并将得到的反应混合物加入到水从而使得到的所述苏-12-环氧-3-氨基-4-苯基丁烷衍生物（1）结晶出来。

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