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1. 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

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

JP2011046751A Synthesis of himbacine analog 审中-公开
标题翻译：生物素类似物的合成
公开(公告)号：JP2011046751A
公开(公告)日：2011-03-10
申请号：JP2010275168
申请日：2010-12-09
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 , WANG TAO , LIAO JING , CHIU JOHN S , TSAI DAVID J S , LEE HONG-CHAN , WU WENXUE , FU XIAOYONG
IPC分类号： C07D405/06 , A61K31/4525 , A61P43/00 , C07D307/33
CPC分类号： C07D307/77 , C07D307/885 , C07D307/92 , C07D405/06
摘要： PROBLEM TO BE SOLVED: To provide a new method for preparing himbacine analogs useful as thrombin receptor antagonists.
SOLUTION: An improved method for preparing himbacine analogs from compound 2A is provided. The improved method may allow for at least one of, easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供一种制备可用作凝血酶受体拮抗剂的十一碳烯类似物的新方法。提供了一种从化合物2A制备烟肼类似物的改进方法。改进的方法可以允许至少一种，通过结晶进行更容易的纯化，更容易的伸缩性和提高所需对映异构体的方法产率。版权所有（C）2011，JPO＆INPIT

5. 发明专利

JP2010189425A Crystalline polymorph of bisulfate salt of thrombin receptor antagonist 审中-公开
标题翻译：硫蛋白受体拮抗剂双磷酸盐的结晶多糖
公开(公告)号：JP2010189425A
公开(公告)日：2010-09-02
申请号：JP2010100422
申请日：2010-04-23
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 , WU WENXUE , WANG TAO , CHIU JOHN S , BOGDANOWICH-KNIPP SUSAN , PAVLOVSKY ANASTASIA , GREENLEE WILLIAM J , GRAZIANO MICHAEL P , KOSOGLOU TEDDY , CHINTALA MADHU , CHACKALAMANNIL SAMUEL
IPC分类号： C07D405/06 , A61K31/443 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/12 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D405/14 , C07D413/14 , C07D417/14 , C07D521/00
CPC分类号： C07D417/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06 , C07D405/14 , C07D413/14
摘要： PROBLEM TO BE SOLVED: To provide a crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist.
SOLUTION: A compound 2 which is the crystalline polymorph of the bisulfate salt can be obtained from a thrombin receptor antagonist compound 1 according to a process represented by formula (A). The compound 2 has higher stability than that of the compound 1. The compound can be used as a pharmaceutical composition for treating thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, myocardial infarction, glomerulonephropathy, thrombotic stroke, thromboembolic cerebral stroke, peripheral vascular disease, inflammatory lesion, cerebral ischemia or cancer.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供凝血酶受体拮抗剂的硫酸氢盐的结晶多晶型物。解决方案：根据由式（A）表示的方法，可以从凝血酶受体拮抗剂化合物1获得作为硫酸氢盐结晶多晶型物的化合物2。化合物2具有比化合物1更高的稳定性。该化合物可以用作治疗血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭，心肌梗塞，肾小球肾炎，血栓形成中风，血栓栓塞大脑的药物组合物中风，外周血管疾病，炎症性病变，脑缺血或癌症。版权所有（C）2010，JPO＆INPIT

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