公开(公告)号：US20090018332A1

公开(公告)日：2009-01-15

申请号：US12144733

申请日：2008-06-24

申请人： Kenneth Alfred Martin Kremer ,  Lalitha Krishnan ,  Aranapakam Mudumbai Venkatesan ,  Mellard Norman Jennings ,  Joseph Zeldis ,  Takao Abe ,  Tarek Suhayl Mansour ,  Henry Lee Strong

发明人： Kenneth Alfred Martin Kremer ,  Lalitha Krishnan ,  Aranapakam Mudumbai Venkatesan ,  Mellard Norman Jennings ,  Joseph Zeldis ,  Takao Abe ,  Tarek Suhayl Mansour ,  Henry Lee Strong

IPC分类号： C07D498/04

CPC分类号： C07C47/277 ,  C07C43/303 ,  C07C45/513 ,  C07C45/71 ,  C07C47/263 ,  C07C69/716 ,  C07C257/14 ,  C07D265/30 ,  C07D498/04 ,  C07D519/00

摘要： The invention relates to processes for the preparation of the bicyclic oxazine carboxaldehyde Compound 1: The invention also relates to the use of Compound 1 in the preparation of □-lactamase inhibitors.

摘要翻译： 本发明涉及制备双环恶嗪甲醛的方法化合物1：本发明还涉及化合物1在制备β-内酰胺酶抑制剂中的用途。

公开(公告)号：US07276611B2

公开(公告)日：2007-10-02

申请号：US10844243

申请日：2004-05-12

申请人： Michael William Winkley ,  Anita Wai-Yin Chan ,  Ivo L. Jirkovsky ,  Kenneth Alfred Martin Kremer ,  Joseph Zeldis ,  Antonia Aristotelevna Nikitenko ,  Henry Lee Strong ,  Tarek Mansour ,  Gulnaz Khafizova ,  Aranapakam M. Venkatesan

发明人： Michael William Winkley ,  Anita Wai-Yin Chan ,  Ivo L. Jirkovsky ,  Kenneth Alfred Martin Kremer ,  Joseph Zeldis ,  Antonia Aristotelevna Nikitenko ,  Henry Lee Strong ,  Tarek Mansour ,  Gulnaz Khafizova ,  Aranapakam M. Venkatesan

IPC分类号： C07D231/54

CPC分类号： C07D498/04 ,  C07D487/04

摘要： There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.

摘要翻译： 提供了一种制备具有结构式I的双环杂芳基羧醛的方法，其中X和Y在说明书中定义。双环杂芳基羧醛可用作制备β-内酰胺酶抑制剂的中间体。

公开(公告)号：US07297795B2

公开(公告)日：2007-11-20

申请号：US10918947

申请日：2004-08-16

申请人： Karen Wiggins Sutherland ,  Gregg Brian Feigelson ,  Diane Harris Boschelli ,  David Michael Blum ,  Henry Lee Strong

发明人： Karen Wiggins Sutherland ,  Gregg Brian Feigelson ,  Diane Harris Boschelli ,  David Michael Blum ,  Henry Lee Strong

IPC分类号： C07D215/44

CPC分类号： C07D405/04 ,  C07D215/54 ,  C07D495/04

摘要： This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.

摘要翻译： 本发明公开了一种制备4-氨基-3-喹啉甲腈的方法，包括将胺化合物与氰基乙酸和酸催化剂混合以产生氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺在醇溶剂和三烷基原甲酸酯中缩合，得到3-氨基-2-氰基丙烯酰胺; 任选在催化剂存在下，将3-氨基-2-氰基丙烯酰胺与三氯氧化磷在乙腈，丁腈，甲苯或二甲苯中的混合，得到4-氨基-3-喹啉腈，并公开了制备7-氨基-2-氰基丙烯酰胺的方法， 氨基 - 噻吩并[3,2-b]吡啶-6-甲腈，其包括在醇溶剂中组合二取代的3-氨基噻吩与氰基乙酰胺和三烷基酯，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯和乙腈，丁腈，甲苯或二甲苯组合，任选在催化剂存在下，得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈和 还公开了通过将胺化合物与氰基乙酸和肽偶联剂组合以制备悬浮液来制备4-氨基-3-喹啉腈的方法; 过滤悬浮液，得到氰基乙酰胺; 将氰基乙酰胺与任选的高达四取代的苯胺，醇溶剂和原甲酸三乙酯缩合，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯组合，得到4-氨基-3-喹啉腈。