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1.发明申请FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF 审中-公开四唑替代方法的形成及其选择性减少公开(公告)号：US20100041893A1
公开(公告)日：2010-02-18
申请号：US12603901
申请日：2009-10-22
申请人： KEVIN R. CAMPOS , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： KEVIN R. CAMPOS , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D211/72 , C07C233/00
CPC分类号： C07C231/18 , C07C253/14 , C07C309/73 , C07D213/64 , C07C255/56
摘要： The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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2.发明授权公开(公告)号：US07629470B2
公开(公告)日：2009-12-08
申请号：US11629005
申请日：2005-07-01
申请人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D213/63
CPC分类号： C07C231/18 , C07C253/14 , C07C309/73 , C07D213/64 , C07C255/56
摘要： The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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3.发明申请公开(公告)号：US20090018340A1
公开(公告)日：2009-01-15
申请号：US11629005
申请日：2005-07-01
申请人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： Kevin R. Campos , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D213/64 , C07C255/50
CPC分类号： C07C231/18 , C07C253/14 , C07C309/73 , C07D213/64 , C07C255/56
摘要： The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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公开(公告)号：US07579487B2
公开(公告)日：2009-08-25
申请号：US11578283
申请日：2005-05-06
IPC分类号： C07D309/06
CPC分类号： C07D315/00 , C07C303/40 , C07C2601/14 , C07D309/04 , C07D309/06 , C07D309/20 , C07C311/13 , C07C311/19 , C07C311/16 , C07C311/29
摘要： This invention relates to a process for preparing optically active α-amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene-sulfonamide acid or ester.
摘要翻译： 本发明涉及用于制备用于治疗炭疽的有效的致死因子（LF）抑制剂的光学活性α-氨基酸底物的方法。 本发明还涉及一种合成用于治疗炭疽的强效LF抑制剂的方法。 具体地，本发明涉及四取代的烯 - 磺酰胺酸或酯的新颖的高产率和高度对映选择性的不对称氢化反应。
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