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1. 发明专利

JP2010053139A Synthesis of 2-hydroxy-n,n-dimethyl-3-[[2-[[1(r)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobutene-1-yl]amino]benzamide 有权
标题翻译：合成2-羟基-N，N-二甲基-3 - [[2 - [[1（R） - （5-甲基-2-呋喃基）丙基]氨基] -3,4-二氧代-1-环己基-1 基]氨基]苯甲酰胺
公开(公告)号：JP2010053139A
公开(公告)日：2010-03-11
申请号：JP2009273993
申请日：2009-12-01
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： YIN JIANGUO , FU XIAOYONG , ZHANG SHUYI , MCALLISTER TIMOTHY L , KIM-MEADE AGNES S , WINTERS JASON L , SUDHAKAR ANANTHA , SCHUMACHER DORIS P
IPC分类号： C07D307/52 , C07B53/00 , C07B61/00 , C07C235/60
CPC分类号： C07D307/52 , C07C235/60
摘要： PROBLEM TO BE SOLVED: To produce an antagonist which binds to a CXC chemokine receptor. SOLUTION: The process for producing the compound of formula (I) (2-hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobutene-1-yl]amino]benzamide) using compounds of formulas (II), (Q), and (XI) or (XII), (II) is disclosed. Here, A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R is 1-10C alkyl. Intermediate compounds produced in the process are also disclosed. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：产生结合CXC趋化因子受体的拮抗剂。解决方案：制备式（I）化合物的方法（2-羟基-N，N-二甲基-3 - [[2 - [[1（R） - （5-甲基-2-呋喃基）丙基公开了使用式（II），（Q）和（XI）或（XII），（II）的化合物的氨基] -3,4-二氧代-1-环丁烯-1-基]氨基]苯甲酰胺。这里，A选自Br，Cl和I（优选Br）; R为1-10C烷基。还公开了在该方法中生产的中间体化合物。版权所有（C）2010，JPO＆INPIT

2. 发明专利

JP2012036224A Process for synthesis of azetidinones 审中-公开
标题翻译：合成AZETIDINONES的方法
公开(公告)号：JP2012036224A
公开(公告)日：2012-02-23
申请号：JP2011252865
申请日：2011-11-18
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： THIRUVETTIPURAM THIRUVENGADAM K , CHIU JOHN S , FU XIAOYONG , MCALLISTER TIMOTHY L
IPC分类号： C07D205/08 , C07D201/02
CPC分类号： C07D205/08 , C07H17/02
摘要： PROBLEM TO BE SOLVED: To provide a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents.SOLUTION: The process includes reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent. The cyclizing agent is selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride.
摘要翻译：要解决的问题：提供一种制备可用作半乳聚糖和低胆固醇血症药的中间体的氮杂环丁酮的方法。解决方案：该方法包括使β-（取代氨基）酰胺，β-（取代氨基）酸酯或β-（取代氨基）硫代碳酸酯与甲硅烷基化剂和环化剂。环化剂选自碱金属羧酸盐，季铵羧酸盐，季铵氢氧化物，季铵醇盐，季铵芳氧化物及其水合物，或其反应产物：（i）至少一种季铵卤化物和至少一种碱金属羧酸盐; 或（ii）至少一种季铵氯化物，季铵溴化物或季铵碘化物和至少一种碱金属氟化物。版权所有（C）2012，JPO＆INPIT

3. 发明专利

JP2011016841A Process for synthesizing azetidinone 审中-公开
标题翻译：合成AZETIDINONE的方法
公开(公告)号：JP2011016841A
公开(公告)日：2011-01-27
申请号：JP2010216153
申请日：2010-09-27
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： THIRUVENGADAM TIRUVETTIPURAM K , FU XIAOYONG , TANN CHOU-HONG , MCALLISTER TIMOTHY L , CHIU JOHN S , COLON CESAR
IPC分类号： C07D205/08 , B01J31/02 , C07B61/00 , C07D263/20 , C07F7/18
CPC分类号： C07D205/08 , C07F7/1852 , C07F7/1856 , C07F7/1892 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a simple and improved process for preparing hypocholesterolemic agent, azetidinone, having formula I in a high yield.SOLUTION: The process for preparing a hypocholesterolemic compound (I) is provided. The process includes following steps: (a) a step for preparing a ketone of formula (IV) by reacting p-fluorobenzoyl lactic acid with pivaloyl chloride and acylating the resultant product with a chiral auxiliary; (b) a step for reducing the ketone of formula (IV) to an alcohol in the presence of a chiral catalyst; (c) a step for preparing β-(substituted amino)amide of formula (VII) by reacting the chiral alcohol of the step (b), an imine and a silyl protective agent, subsequently condensing the protected compound; and (d) a step for preparing a protected lactam of formula (VIII) by cyclizing the β-(substituted amino)amide of formula (VII) with a silylating agent and a fluoride ion catalyst.
摘要翻译：要解决的问题：提供一种用于制备具有式I的低胆固醇血症药物氮杂环丁酮的简单和改进的方法，其产率高。提供了制备低胆固醇血症化合物（I）的方法。该方法包括以下步骤：（a）通过使对氟苯甲酰乳酸与新戊酰氯反应制备式（Ⅳ）的酮并用手性助剂酰化所得产物的步骤; （b）在手性催化剂存在下将式（Ⅳ）的酮还原成醇的步骤; （c）通过使步骤（b）的手性醇与亚胺和甲硅烷基保护剂反应，随后使被保护的化合物冷凝，从而制备式（Ⅶ）的β-（取代的氨基）酰胺的步骤; 和（d）通过使甲硅烷基化剂和氟离子催化剂环化式（VII）的β-（取代的氨基）酰胺来制备式（VIII）的受保护内酰胺的步骤。

4. 发明专利

JP2010111684A Stereoselective alkylation of chiral 2-methyl-4-protected piperazine 审中-公开
标题翻译： 2甲基-4保护的哌嗪的立体选择性烷基化
公开(公告)号：JP2010111684A
公开(公告)日：2010-05-20
申请号：JP2009291493
申请日：2009-12-22
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： WU WENXUE , LIAO HONGBIAO , TSAI DAVID J , ANDREWS DAVID R , GALA DINESH , LEE GARY M , SCHWARTZ MARTIN LAWRENCE , MCALLISTER TIMOTHY L , FU XIAOYONG , MALONEY DONAL , THIRUVENGADAM T K , TANN CHOU-HANG
IPC分类号： C07D241/04 , C07B51/00 , C07B53/00 , C07B61/00 , C07C45/51 , C07C303/28 , C07C309/73 , C07D295/084 , C07D295/088 , C07D295/185 , C07D295/192 , C07D295/205
CPC分类号： C07D295/185 , C07B2200/07 , C07C45/512 , C07C67/343 , C07C309/73 , C07D295/088 , C07D295/092 , C07D295/192 , C07D295/205 , C07C49/255 , C07C69/734 , C07C49/84
摘要： PROBLEM TO BE SOLVED: To provide stereoselective alkylation of chiral 2-methyl-4-protected piperazines. SOLUTION: There is provided the synthesis of a compound VIII with high stereochemical purity by a stereoselective alkylation process of 2-methyl-4-protected piperazines and using an inorganic base, wherein X is a substituent on the aromatic ring; n is an integer indicating the number of the same or different X moiety and in a range of 1-5; each X is independently selected from the group consisting of alkyl, halogen, halogenated alkyl, alkoxy, aryl, aryloxy, and heteroaryl; and Z is selected from the group consisting of alkyl, alkoxyalkyl, aryl, heteroaryl, heteroarylalkyl and arylalkyl. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供手性2-甲基-4-保护的哌嗪的立体选择性烷基化。解决方案：通过2-甲基-4-保护的哌嗪的立体选择性烷基化方法和使用无机碱（其中X是芳环上的取代基），提供具有高立体化学纯度的化合物VIII的合成; n表示相同或不同的X部分的数目，在1-5的范围内的整数; 每个X独立地选自烷基，卤素，卤代烷基，烷氧基，芳基，芳氧基和杂芳基; 并且Z选自烷基，烷氧基烷基，芳基，杂芳基，杂芳基烷基和芳基烷基。版权所有（C）2010，JPO＆INPIT

5. 发明专利

JP2005053931A Process for synthesis of azetidinone 有权
标题翻译：合成AZETIDINONE的方法
公开(公告)号：JP2005053931A
公开(公告)日：2005-03-03
申请号：JP2004325744
申请日：2004-11-09
申请人： Schering Plough Corp , シェーリングコーポレイションSchering Corporation
发明人： THIRUVENGADAM TIRUVETTIPURAM K , FU XIAOYONG , TANN CHOU-HONG , MCALLISTER TIMOTHY L , CHIU JOHN S , COLON CESAR
IPC分类号： C07D205/08 , C07B61/00 , C07F7/18
CPC分类号： C07D205/08 , C07F7/1852 , C07F7/1856 , C07F7/1892 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide an improved, simple and high yield process for producing a hypocholesterolemic agent azetidinone having formula I.
SOLUTION: The process for preparing the hypocholesterolemic compound I is provided, wherein the process comprises (a) a step for reacting p-fluorobenzoylbutyric acid with pivaloyl chloride and acylating the product with a chiral auxiliary to obtain a ketone of formula IV, (b) a step for reducing the ketone of formula IV in the presence of a chiral catalyst to an alcohol, (c) a step for reacting the chiral alcohol of step (b), an imine and a silyl protecting agent, then condensing the protected compounds to obtain a β-(substituted-amino)amide of formula VII and (d) a step for cyclizing the β-(substituted-amino)amide of formula VII with a silylating agent and a fluoride ion catalyst to obtain a protected lactam of formula VIII. The intermediates of formulas VII and VIII are also claimed.
COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：解决方案：提供一种用于制备具有式I的低胆固醇血症药物氮杂环丁酮的改进的，简单且高产率的方法。解决方案：提供制备低胆固醇血症化合物I的方法，其中该方法包括（a ）使对氟苯甲酰基丁酸与新戊酰氯反应并用手性助剂酰化产物以获得式IV的酮的步骤，（b）在手性催化剂存在下将式IV的酮还原为醇的步骤，（c）使步骤（b）的手性醇与亚胺和甲硅烷基保护剂反应的步骤，然后使被保护的化合物缩合得到式VII的β-（取代的 - 氨基）酰胺和（d）步骤用甲硅烷基化剂和氟离子催化剂使式VII的β-（取代氨基）酰胺环化，得到受保护的式VIII的内酰胺。还要求保护式VII和VIII的中间体。版权所有（C）2005，JPO＆NCIPI

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