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21. 发明授权

US07642352B2 Process for preparing 2,3-disubstituted indoles 有权
标题翻译：制备2,3-二取代吲哚的方法
公开(公告)号：US07642352B2
公开(公告)日：2010-01-05
申请号：US11351411
申请日：2006-02-10
申请人： Ahmad Khodabocus , Zhi-Hui Lu , Chris Hugh Senanayake , Hanxun Wei , Yongda Zhang
发明人： Ahmad Khodabocus , Zhi-Hui Lu , Chris Hugh Senanayake , Hanxun Wei , Yongda Zhang
IPC分类号： C07D403/04
CPC分类号： C07D209/10 , C07D209/08 , C07D209/12 , C07D401/04 , C07D403/04 , C07D409/04
摘要： Disclosed are processes for making 2,3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence of a ligand, a palladium catalyst and a base to make a compound of general formula (ii); or alternatively reacting compound (i) with a trialkyl magnesiate reagent, followed by treatment with a borate; b) reacting the product of step a with a R2-Hal where R2-Hal is defined herein.
摘要翻译：公开了制备2,3二取代的吲哚化合物的方法，例如通式I的化合物，其包括以下步骤：a）在配体，钯催化剂和钯催化剂存在下使溴吲哚化合物（i）与二烷氧基C1-5硼烷反应，制备通式（ii）的化合物的碱; 或者使化合物（i）与三烷基氧化镁试剂反应，然后用硼酸盐处理; b）使步骤a的产物与本文定义R 2 Hal的R 2-Hal反应。

22. 发明授权

US06376684B1 Stereoselective process for alkyl phenylglycolic acids 有权
标题翻译：烷基苯基乙醇酸的立体选择性方法
公开(公告)号：US06376684B1
公开(公告)日：2002-04-23
申请号：US09711776
申请日：2000-11-13
申请人： Chris Hugh Senanayake , Paul T. Grover
发明人： Chris Hugh Senanayake , Paul T. Grover
IPC分类号： C07D30793
CPC分类号： C07D317/34 , C07C51/353 , C07C59/54
摘要： A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an &agr;-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.
摘要翻译：公开了一种制备烷基苯基乙醇酸的方法。它遵循将取代的乙醛与扁桃酸缩合的顺序，得到5-烷基酮或醛缩合的5-苯基-1,3-二氧戊环-4-酮，得到5-（1-羟基烷基）-5 - 苯基-1,3-二氧戊环-4-酮，将其脱水至5-（1-烯基）-5-苯基-1,3-二氧戊环-4-酮。可以将5-（1-烯基）-5-苯基-1,3-二氧戊环-4-酮水解并还原成α-烷基苯基乙醇酸，或者可以逆转水解和还原步骤。该方法能够生产环己基苯基乙醇酸（CHPGA）的单一对映异构体。公开了外消旋CHPGA的类似方法，其使用外消旋扁桃酸和丙酮。还公开了该方法中的新型中间体。

23. 发明授权

US06180823B2 Stereoselective process for alkyl phenylglycolic acids 失效
标题翻译：烷基苯基乙醇酸的立体选择性方法
公开(公告)号：US06180823B2
公开(公告)日：2001-01-30
申请号：US09187832
申请日：1998-11-06
申请人： Chris Hugh Senanayake , Paul T. Grover
发明人： Chris Hugh Senanayake , Paul T. Grover
IPC分类号： C07C5730
CPC分类号： C07D317/34 , C07C51/353 , C07C59/54
摘要： A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an &agr;-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.
摘要翻译：公开了一种制备烷基苯基乙醇酸的方法。它遵循将取代的乙醛与扁桃酸缩合的顺序，得到5-烷基酮或醛缩合的5-苯基-1,3-二氧戊环-4-酮，得到5-（1-羟基烷基）-5 - 苯基-1,3-二氧戊环-4-酮，将其脱水至5-（1-烯基）-5-苯基-1,3-二氧戊环-4-酮。可以将5-（1-烯基）-5-苯基-1,3-二氧戊环-4-酮水解并还原成α-烷基苯基乙醇酸，或者可以逆转水解和还原步骤。该方法能够生产环己基苯基乙醇酸（CHPGA）的单一对映异构体。公开了外消旋CHPGA的类似方法，其使用外消旋扁桃酸和丙酮。还公开了该方法中的新型中间体。

24. 发明授权

US6090971A Resolution process for cyclohexylphenyl glycolic acid 有权
标题翻译：环己基苯基乙醇酸的拆分方法
公开(公告)号：US6090971A
公开(公告)日：2000-07-18
申请号：US344654
申请日：1999-06-25
申请人： Roger P. Bakale , Jorge L. Lopez , Francis X. McConville , Charles P. Vandenbossche , Chris Hugh Senanayake
发明人： Roger P. Bakale , Jorge L. Lopez , Francis X. McConville , Charles P. Vandenbossche , Chris Hugh Senanayake
IPC分类号： C07C51/487 , C07C67/12 , C07C69/96 , C07C213/06 , C07C219/20 , C07C229/36 , C07B57/00
CPC分类号： C07C213/06 , C07C51/487 , C07C67/12 , C07C69/96 , C07B2200/07 , C07C2101/14
摘要： A process for the preparation of optically active phenylcyclohexylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)-- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described. In addition, a resolution process employing tyrosine methyl ester enantiomers for preparing a single enantiomer of CHPGA from racemic CHPGA is disclosed.
摘要翻译：描述了制备光学活性苯基环己基甘醇酸酯的方法。该方法利用羧酸活化将（R） - 或（S） - 环己基苯基乙醇酸（CHPGA）与4-N，N-二乙基氨基丁醇或其它炔丙醇衍生物偶联。还描述了盐酸盐的制备。此外，公开了一种使用酪氨酸甲酯对映异构体从外消旋CHPGA制备CHPGA的单一对映异构体的拆分方法。

25. 发明授权

US5936124A Fluoxetine process from benzoylpropionic acid 失效
公开(公告)号：US5936124A
公开(公告)日：1999-08-10
申请号：US102418
申请日：1998-06-22
申请人： James Wallace Hilborn , Alex Roger Jurgens , Chris Hugh Senanayake
发明人： James Wallace Hilborn , Alex Roger Jurgens , Chris Hugh Senanayake
IPC分类号： C07C213/00 , C07C213/06 , C07C215/30 , C07C217/48
CPC分类号： C07C213/06 , C07C213/00 , C07B2200/07
摘要： A synthesis of fluoxetine is disclosed. The process begins with a lower alkyl ester of 3-benzoylpropionic acid, which is reduced in the presence of a chiral ligand to produce the corresponding .gamma.-hydroxy ester, and the ester is cleaved. The free acid is then condensed with the alcohol to form a .gamma.-lactone, which is treated with ammonia to provide the .gamma.-hydroxy amide. The amide undergoes a Hoffman rearrangement to provide a 2-oxo-1,3 oxazine, which is reduced to 3-(methylamino)-1-phenyl-1-propanol. The alcohol is deprotonated and reacted with a 4-chloro- or 4-fluoro benzotrifluoride to provide fluoxetine free base.

26. 发明申请

US20140171692A1 PROCESS FOR ASYMETRIC METHYLALLYLATION IN THE PRESENCE OF A 2,2'-SUBSTITUTED 1,1'-BI -2-NAPHTHOL CATALYST 有权
标题翻译：在2,2'-取代的1,1'-二-2-萘基催化剂存在下进行异亚甲基化的方法
公开(公告)号：US20140171692A1
公开(公告)日：2014-06-19
申请号：US14003248
申请日：2012-03-06
申请人： Wenjie Li , Zhi-Hui Lu , Chris Hugh Senanayake , Yongda Zhang
发明人： Wenjie Li , Zhi-Hui Lu , Chris Hugh Senanayake , Yongda Zhang
IPC分类号： C07C39/14 , C07C37/62 , C07C29/143
CPC分类号： C07C39/14 , C07B2200/07 , C07C29/143 , C07C29/38 , C07C37/055 , C07C37/62 , C07C39/38 , C07C41/48 , C07C43/313 , C07C33/483
摘要： Disclosed are a process and catalysts useful for carrying out asymmetric methlyallylations. The catalysts used in the invention have the formula (IV): wherein X1, X2, R3 and R4 are as defined herein. Compounds made by the process of the invention can be used to prepare pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors including 1,3-disubstituted oxazinan-2-ones.
摘要翻译：公开了用于进行不对称甲基化反应的方法和催化剂。用于本发明的催化剂具有式（Ⅳ）：其中X 1，X 2，R 3和R 4如本文所定义。通过本发明的方法制备的化合物可用于制备药物活性化合物，例如11-＆bgr-羟基类固醇氢化酶1型（11-＆amp; bgr-HSD1）抑制剂，包括1,3-二取代的恶嗪烷-2-酮。

27. 发明申请

US20080293972A1 Process for Preparing Substituted Anisidines 有权
标题翻译：制备取代苯胺的方法
公开(公告)号：US20080293972A1
公开(公告)日：2008-11-27
申请号：US12092454
申请日：2006-11-01
申请人： Fabrice Gallou , Heewon Lee , Chris Hugh Senanayake , Jinhua J. Song , Zhulin Tan , Jinghua Xu , Nathan K. Yee
发明人： Fabrice Gallou , Heewon Lee , Chris Hugh Senanayake , Jinhua J. Song , Zhulin Tan , Jinghua Xu , Nathan K. Yee
IPC分类号： C07C213/02 , C07C251/44
CPC分类号： C07C213/02 , C07C249/08 , C07C251/44 , C07C2601/16 , C07C217/84
摘要： Disclosed is a process for preparing substituted anisidines of formula I starting from substituted cyclic hydroxy-ketones II via aromatization through a substituted oxime intermediate IV in which R is C1-C6 alkyl or halogen, and Alk is C1-C6 alkyl. The substituted anisidines of formula I have been found to be useful as intermediates in the preparation of agents for the treatment of hepatitis C viral (HCV) infections.
摘要翻译：公开了通过芳族化通过其中R是C 1 -C 6烷基或卤素的取代的肟中间体IV和Alk是C 1 -C 6烷基的取代的环状羟基酮II制备取代的茴香胺的方法。已经发现式I的取代的茴香醚可用作制备用于治疗丙型肝炎病毒（HCV）感染的药剂的中间体。

28. 发明授权

US07126009B2 Palladium catalyzed indolization of 2-bromo or chloroanilines 有权
标题翻译：钯催化的2-溴或氯代苯胺的吲哚化
公开(公告)号：US07126009B2
公开(公告)日：2006-10-24
申请号：US11079636
申请日：2005-03-14
申请人： Guisheng Li , Jianxiu Liu , Zhi-Hui Lu , Frank Roschangar , Chris Hugh Senanayake , Ming Shen
发明人： Guisheng Li , Jianxiu Liu , Zhi-Hui Lu , Frank Roschangar , Chris Hugh Senanayake , Ming Shen
IPC分类号： C07D209/04 , C07D209/08 , C07D209/12 , C07D209/24 , C07F7/10
CPC分类号： C07C237/38 , C07C2601/04 , C07D209/12 , C07D401/04
摘要： The present invention provides a method for making substituted indole compounds of general formula III comprising the step of:(a) reacting a 2-bromoaniline or 2-chloroaniline of general formula (I) (I) wherein: X, R and R1 are defined herein with a substituted acetylene of formula (II) wherein R2 and R3 are defined herein in the presence of a palladium catalyst, a ligand, and a base in a solvent at a suitable temperature to give a compound of formula (III);
摘要翻译：本发明提供了制备通式III的取代的吲哚化合物的方法，其包括以下步骤：（a）使通式（I）（I）的2-溴苯胺或2-氯苯胺反应其中：X，R和R

29. 发明授权

US6147217A Synthesis of terfenadine and derivatives 有权
标题翻译：特非那定和衍生物的合成
公开(公告)号：US6147217A
公开(公告)日：2000-11-14
申请号：US316104
申请日：1999-05-24
申请人： Chris Hugh Senanayake , Qun Kevin Fang , Scott Harold Wilkinson
发明人： Chris Hugh Senanayake , Qun Kevin Fang , Scott Harold Wilkinson
IPC分类号： A61P37/08 , C07C69/716 , C07C69/76 , C07D211/22 , C07D211/34 , C07D307/20 , C07D317/20 , C07D317/22 , C07D317/26 , C07D317/30
CPC分类号： C07D317/20 , C07C69/76 , C07D211/22 , C07D211/34 , C07D307/20 , C07D317/22 , C07D317/30
摘要： Processes for preparing compounds having the general formula: ##STR1## wherein R.sup.1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of the general formula IV ##STR2## wherein R.sup.1 and R.sup.2 are as defined in the specification.
摘要翻译：公开了制备具有以下通式的化合物的方法：其中R1a被保护的羧基，羧基，羟甲基，被保护的羟甲基或甲基。本发明的方法开始于通式IV的起始原料，其中R 1和R 2如说明书中所定义。

30. 发明授权

US6071971A Desformoterol compositions useful for inducing bronchodilation 有权
标题翻译：用于诱导支气管扩张的曲美托洛尔组合物
公开(公告)号：US6071971A
公开(公告)日：2000-06-06
申请号：US305534
申请日：1999-05-05
申请人： Chris Hugh Senanayake
发明人： Chris Hugh Senanayake
IPC分类号： A61P11/08 , A61K31/137 , C07B61/00 , C07C213/02 , C07C213/04 , C07C215/78 , C07C217/60 , C07C217/70 , A61K31/135
CPC分类号： C07C213/04 , C07C217/60 , C07B2200/07
摘要： The (R,R)-, (S,S)-, (R,S)-, (R,S)-isomers of 3-amino-4-hydroxy-.alpha.-[[[2-(4-methoxyphenyl)-1-methylethyl]amino]methyl]-benzenemethanol (D) ##STR1## are disclosed, as well as an efficient method for their stereoselective synthesis. A method and composition are also disclosed utilizing desformoterol (D) as a bronchodilator, having high selectivity for .beta..sub.2 receptors.
摘要翻译： 3-氨基-4-羟基-α - [[[2-（4-甲氧基苯基） - 苯基] - （R，R） - ，（S，S） - ，（R，S） -1-甲基乙基]氨基]甲基] - 苯甲醇（D），以及其立体选择性合成的有效方法。还公开了一种方法和组合物，其使用作为支气管扩张剂的曲美托洛尔（D），对β2受体具有高选择性。

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