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公开(公告)号：US08916701B2
公开(公告)日：2014-12-23
申请号：US13921145
申请日：2011-12-15
申请人： Daniel Robert Fandrick , Zhi-Hui Lu , Diana Reeves , Jonathan Reeves , Chris Hugh Senanayake , Jinhua Jeff Song , Yongda Zhang
发明人： Daniel Robert Fandrick , Zhi-Hui Lu , Diana Reeves , Jonathan Reeves , Chris Hugh Senanayake , Jinhua Jeff Song , Yongda Zhang
IPC分类号： C07D413/10 , C07D265/10 , C07D213/64
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。
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公开(公告)号：US20090264655A1
公开(公告)日：2009-10-22
申请号：US12487910
申请日：2009-06-19
IPC分类号： C07D403/04 , C07D209/18 , C07D403/12
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2,3,4-二取代吲哚化合物的方法，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。
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公开(公告)号：US07332610B2
公开(公告)日：2008-02-19
申请号：US11514141
申请日：2006-09-01
IPC分类号： C07D291/04
CPC分类号： C07D291/04 , C07B2200/07 , C07C209/52 , C07C249/02 , C07C303/34 , C07C2601/04 , C07D453/04 , C07C307/02 , C07C211/29 , C07C251/16
摘要： This invention provides intermediates useful in a method of preparing amine stereoisomers. It also provides a method of preparing sulfoxide and sulfinylamine stereoisomers using certain of the intermediates.
摘要翻译： 本发明提供了可用于制备胺立体异构体的方法的中间体。 它还提供了使用某些中间体制备亚砜和亚磺酰胺立体异构体的方法。
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公开(公告)号：US07064214B2
公开(公告)日：2006-06-20
申请号：US10120541
申请日：2002-04-12
申请人： Chris Hugh Senanayake , Zhengxu Han , Dhileepkumar Krishnamurthy , Derek Pflum , Harold Scott Wilkinson
发明人： Chris Hugh Senanayake , Zhengxu Han , Dhileepkumar Krishnamurthy , Derek Pflum , Harold Scott Wilkinson
IPC分类号： C07D213/02 , C07D235/04
CPC分类号： C07D291/04 , C07B2200/07 , C07C303/36 , C07C313/04 , C07C315/00 , C07C317/04 , C07C2602/08 , C07D235/28 , C07D291/08 , C07D401/12 , C07C317/14 , C07C311/03
摘要： This invention encompasses novel methods of preparing sulfinamides and sulfoxides, particularly stereomerically pure sulfinamides and sulfoxides. The invention further encompasses novel compounds from which sulfinamides and sulfoxides can be prepared.
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公开(公告)号：US6140529A
公开(公告)日：2000-10-31
申请号：US211646
申请日：1998-12-15
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： C07B57/00 , C07C51/43 , C07C51/487 , C07C59/11 , C07C59/54 , C07C67/12 , C07C69/732 , C07C69/96 , C07C213/06 , C07C219/20 , C07C229/36
CPC分类号： C07C69/96 , C07C213/06 , C07C219/20 , C07C229/36 , C07C51/487 , C07C67/12 , C07C68/02 , C07B2200/07 , C07C2101/14
摘要： A process for the preparation of optically active cyclohexylphenylglycolate 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环己基苯基甘醇酸酯的方法。 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。
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公开(公告)号：US06028224A
公开(公告)日：2000-02-22
申请号：US316095
申请日：1999-05-24
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.
摘要翻译： 公开了氟西汀的合成。 该方法开始于3-苯甲酰基丙酸的低级烷基酯，其在手性配体的存在下还原以产生相应的γ-羟基酯，并且酯被切割。 然后将游离酸与醇缩合形成γ-内酯，其用氨处理以提供γ-羟基酰胺。 酰胺进行霍夫曼重排以提供2-氧代-1,3-恶嗪，将其还原成3-（甲基氨基）-1-苯基-1-丙醇。 醇被去质子化并与4-氯或4-氟三氟甲苯反应，得到氟西汀游离碱。
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公开(公告)号：US6025177A
公开(公告)日：2000-02-15
申请号：US247731
申请日：1999-02-09
申请人： Chris Hugh Senanayake , Roger P. Bakale , Qun Kevin Fang , Paul Timothy Grover , Donald L. Heefner , Richard F. Rossi , Stephen Alan Wald
发明人： Chris Hugh Senanayake , Roger P. Bakale , Qun Kevin Fang , Paul Timothy Grover , Donald L. Heefner , Richard F. Rossi , Stephen Alan Wald
IPC分类号： C07C215/44 , C07C311/20 , C07D263/52 , C07D263/08
CPC分类号： C07D263/52 , C07C215/44 , C07C311/20 , C07C2101/14 , C07C2102/08 , Y02P20/582
摘要： Processes for preparing a single enantiomer of an .alpha.,.alpha.-disubstituted-.alpha.-hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. ##STR1## Intermediates useful in the process are also disclosed.
摘要翻译： 公开了制备α，α-二取代-α-羟基乙酸，特别是环己基苯基乙醇酸（CHPGA）的单一对映异构体的方法。 该方法通过形成恶唑烷的氨基醇或非对映体酰胺的非对映异构体酯，将环状1,2-氨基醇用作手性助剂。 还公开了在该方法中有用的中间体。
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公开(公告)号：US6013830A
公开(公告)日：2000-01-11
申请号：US050825
申请日：1998-03-30
申请人： Chris Hugh Senanayake , Roger P. Bakale , Qun Kevin Fang , Paul Timothy Grover , Donald L. Heefner , Richard F. Rossi , Stephen Alan Wald
发明人： Chris Hugh Senanayake , Roger P. Bakale , Qun Kevin Fang , Paul Timothy Grover , Donald L. Heefner , Richard F. Rossi , Stephen Alan Wald
IPC分类号： C07C215/44 , C07C311/20 , C07D263/52 , C07C69/76 , C07D263/54
CPC分类号： C07D263/52 , C07C215/44 , C07C311/20 , C07C2101/14 , C07C2102/08 , Y02P20/582
摘要： Processes for preparing a single enantiomer of an .alpha.,.alpha.-disubstituted-.alpha.-hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. ##STR1## Intermediates useful in the process are also disclosed.
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公开(公告)号：US07851625B2
公开(公告)日：2010-12-14
申请号：US12487910
申请日：2009-06-19
IPC分类号： C07D403/04 , C07D401/04 , C07D235/04 , C07D209/04
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2,3,4-二取代吲哚化合物的方法，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。
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公开(公告)号：US06780891B2
公开(公告)日：2004-08-24
申请号：US10308878
申请日：2002-12-02
IPC分类号： C07C21101
CPC分类号： C07C217/74 , C07C217/52 , C07C255/59 , C07C2601/02 , C07C2601/14
摘要： Compounds of formula I are effective in treating disorders modulated by opiate receptor activity and/or monoamine activity. In formula I, R1 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl; R2 is selected from hydrogen, hydroxy, cyano, haloalkyl, glycosyl, SO2R5, and OR5; R3 and R4 are independently selected from hydrogen and lower alkyl, or R3 and R4 taken together with nitrogen form a five- or six-membered heterocyclic or substituted heterocyclic ring; and R5 is selected from alkyl, aryl, alkylaryl, substituted alkyl, substituted aryl, and substituted alkylaryl.
摘要翻译： 式I化合物在治疗由阿片剂受体活性和/或单胺活性调节的病症中是有效的。在式I中，R 1选自烷基，芳基，烷基芳基，取代的烷基，取代的芳基和取代的烷基芳基; R 2选自氢，羟基，氰基，卤代烷基，糖基，SO 2 R 5和OR 5; R 3和R 4独立地选自氢和低级烷基，或R 3和R 4与氮一起形成五元或六元杂环或取代的杂环; R 5选自烷基，芳基，烷基芳基，取代的烷基，取代的芳基和取代的烷基芳基。
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