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1. 发明申请

US20110263844A1 METHOD FOR PREPARING MACROCYCLES 审中-公开
标题翻译：制备大分子的方法
公开(公告)号：US20110263844A1
公开(公告)日：2011-10-27
申请号：US12991238
申请日：2009-05-05
申请人： Chutian Shu , Chris Hugh Senanayake , Zhulin Tan , Nathan Yee , Xingzhong Zeng
发明人： Chutian Shu , Chris Hugh Senanayake , Zhulin Tan , Nathan Yee , Xingzhong Zeng
IPC分类号： C07D487/04 , C07D403/12
CPC分类号： C07K5/0804 , C07K1/107
摘要： The present invention is directed to a method for the preparation of macrocyclic compounds of formula (I), comprising the step of cyclizing a diene of formula (II), in the presence of a catalyst, wherein R1-R6, A, W and V are as defined herein. The present invention is also directed to intermediate compounds of formula II.
摘要翻译：本发明涉及一种制备式（I）的大环化合物的方法，包括在催化剂存在下使式（II）的二烯环化的步骤，其中R 1 -R 6，A，W和V 如本文所定义。本发明还涉及式II的中间体化合物。

2. 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。

3. 发明授权

US07884246B2 Process for preparing substituted anisidines 有权
标题翻译：制备取代的茴香胺的方法
公开(公告)号：US07884246B2
公开(公告)日：2011-02-08
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： C07C259/00
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。

4. 发明授权

US07179919B2 Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 有权
标题翻译：某些三氟甲基取代的醇的立体选择性合成
公开(公告)号：US07179919B2
公开(公告)日：2007-02-20
申请号：US11070462
申请日：2005-03-02
申请人： Jinhua J. Song , Zhulin Tan , Nathan K. Yee , Chris Hugh Senanayake , Jinghua Xu , Fabrice Gallou
发明人： Jinhua J. Song , Zhulin Tan , Nathan K. Yee , Chris Hugh Senanayake , Jinghua Xu , Fabrice Gallou
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07B2200/07
摘要： A process for stereoselective synthesis of a compound of Formula (I) wherein R1, R2, R3, R4, and R5 are as described herein.
摘要翻译：用于立体选择性合成式（I）的化合物的方法，其中R 1，R 2，R 3，R 4， / SUP>和R 5 5如本文所述。

5. 发明授权

US07265222B2 Process of making di-aryl urea compounds 有权
标题翻译：制备二芳基脲化合物的方法
公开(公告)号：US07265222B2
公开(公告)日：2007-09-04
申请号：US10881589
申请日：2004-06-30
申请人： Nizar Haddad , Xudong Wei , Chris Hugh Senanayake , Jinghua Xu , Nathan Yee
发明人： Nizar Haddad , Xudong Wei , Chris Hugh Senanayake , Jinghua Xu , Nathan Yee
IPC分类号： C07D239/34
CPC分类号： C07D239/47 , C07C275/34 , C07D239/545
摘要： Disclosed is a process of making compounds of formula(I): wherein R1, R2, R3, R4 and Ra of formula(I) are defined herein. The product compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation. Also disclosed are intermediates useful in making such compounds.
摘要翻译：公开了制备式（I）化合物的方法：其中R 1，R 2，R 3，R 4，（I）的R a和R A在本文中定义。产物化合物抑制涉及炎症过程的细胞因子的产生，因此可用于治疗涉及炎症的疾病和病理状况。还公开了可用于制备这些化合物的中间体。

6. 发明申请

US20140135493A1 METHODS OF MAKING DIASTEREOMERIC ORGANIC COMPOUNDS 有权
标题翻译：制备二酯有机化合物的方法
公开(公告)号：US20140135493A1
公开(公告)日：2014-05-15
申请号：US13921145
申请日：2011-12-15
申请人： Daniel Robert Fandrick , Zhi-Hui Lu , Diana Crimhilda Reeves , Jonathan Timothy Reeves , Chris Hugh Senanayake , Jinhua J. Song , Yongda Zhang
发明人： Daniel Robert Fandrick , Zhi-Hui Lu , Diana Crimhilda Reeves , Jonathan Timothy Reeves , Chris Hugh Senanayake , Jinhua J. Song , Yongda Zhang
IPC分类号： C07D413/10 , C07D213/64 , C07C271/48 , C07D265/10
CPC分类号： C07D413/10 , C07C271/48 , C07D213/64 , C07D265/10
摘要： Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.
摘要翻译：公开了制备式（I）的非对映体化合物的方法：其中m，n和R 1至R 4如本文所定义。本发明的方法以高产率提供式（I）化合物，基本上不含相应的非对映异构体。通过本发明的方法制备的式（I）化合物可用于制备药学活性化合物，例如11-羟基类固醇类氢化酶1型（11-＆amp; -HSD1）抑制剂。

7. 发明授权

US08017771B2 Process for preparing acyclic HCV protease inhibitors 有权
标题翻译：制备无环HCV蛋白酶抑制剂的方法
公开(公告)号：US08017771B2
公开(公告)日：2011-09-13
申请号：US12355157
申请日：2009-01-16
申请人： Carl Alan Busacca , Rogelio Perez Frutos , Nizar Haddad , Suresh R. Kapadia , Jon Charles Lorenz , Anjan Saha , Chris Hugh Senanayake , Xudong Wei
发明人： Carl Alan Busacca , Rogelio Perez Frutos , Nizar Haddad , Suresh R. Kapadia , Jon Charles Lorenz , Anjan Saha , Chris Hugh Senanayake , Xudong Wei
IPC分类号： C07D239/26 , C07D241/04 , C07D241/12 , C07D231/12 , C07D295/10 , C07D277/24 , C07C211/52
CPC分类号： C07K5/0808 , C07C225/22 , C07D417/14
摘要： Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.
摘要翻译：公开了用于制备式（I）化合物的高度收敛的方法，该化合物是用于治疗丙型肝炎病毒（HCV）感染的有效活性剂：所公开的方法使用具有羟丙基部分的肽化合物之间的SNAr-型偶联反应以下公式：卤代或磺化溴喹啉化合物。

8. 发明申请

US20110130563A1 SYNTHESIS IF DIHYDROTHIENO[3,2-D]PYRIMIDINE DIOLS 有权
标题翻译：如果DIHYDROTHIENO [3,2-D]吡咯烷酮合成
公开(公告)号：US20110130563A1
公开(公告)日：2011-06-02
申请号：US12989575
申请日：2009-05-07
申请人： Rogelio Perez Frutos , Thomas G. Tampone , Jason Alan Mulder , Dhileepkumar Krishnamurthy , Chris Hugh Senanayake
发明人： Rogelio Perez Frutos , Thomas G. Tampone , Jason Alan Mulder , Dhileepkumar Krishnamurthy , Chris Hugh Senanayake
IPC分类号： C07D239/00
CPC分类号： C07D495/04 , C07D239/70
摘要： The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers.
摘要翻译：本发明涉及制备二氢噻吩并[3,2-d]嘧啶二醇和类似的嘧啶二醇的改进方法，其是有效的，高产的，并且不需要昂贵和潜在的不稳定的中间体。二醇用作合成抑制PDE4的嘧啶化合物的中间体，因此可用于治疗呼吸道或胃肠道疾病和投诉，外周或中枢神经系统疾病和病症，炎症状况和癌症。

9. 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。

10. 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。

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