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1. 发明授权

US08318960B2 Diarylphosphine- and dialkylphosphine-containing compounds, processes of preparing same and uses thereof as tridentate ligands 有权
标题翻译：含二芳基膦和二烷基膦的化合物，其制备方法和用途作为三齿配体
公开(公告)号：US08318960B2
公开(公告)日：2012-11-27
申请号：US12779093
申请日：2010-05-13
申请人： Mark Gandelman , Elaine Melissa Schuster , Gennady Nisnevich
发明人： Mark Gandelman , Elaine Melissa Schuster , Gennady Nisnevich
IPC分类号： C07F9/02
CPC分类号： C07D249/04 , B01J31/189 , B01J31/226 , B01J2231/4261 , B01J2531/0244 , B01J2531/824 , B01J2531/828 , C07F9/5013 , C07F9/5304 , C07F9/6518 , C07F9/65583 , C07F15/006 , C40B30/08 , C40B40/04 , C40B40/16
摘要： A novel process of preparing tridentate ligands containing one or more of a diarylphosphine and/or dialkylphosphine electron donating groups are disclosed. Use of this process for preparing a combinatorial library of such tridentate ligands and of organometallic complexes containing same is also disclosed. Further disclosed are novel diarylphosphine-containing and dialkylphosphine-containing compounds that can serve as tridentate ligands (e.g., pincer ligands), combinatorial libraries of such tridentate ligands, organometallic complexes containing these ligands (e.g., pincer complexes), and combinatorial libraries of such complexes. Methods utilizing these libraries for screening for candidate organometallic catalysts are also disclosed. Novel precursor molecules useful for preparing the tridentate ligands and processes of preparing same are also disclosed.
摘要翻译：公开了一种制备含有一个或多个二芳基膦和/或二烷基膦给电子基团的三齿配体的新方法。还公开了该方法用于制备这种三齿配体的组合文库和含有它们的有机金属络合物的用途。还公开了可以用作三齿配体（例如夹心配体）的新型含二芳基膦和含二烷基膦的化合物，这种三齿配体的组合文库，含有这些配体的有机金属配合物（例如夹心络合物）和这种配合物的组合文库。还公开了利用这些文库筛选候选有机金属催化剂的方法。还公开了可用于制备三齿配体的新型前体分子及其制备方法。

2. 发明申请

US20100292084A1 NOVEL DIARYLPHOSPHINE- AND DIALKYLPHOSPHINE-CONTAINING COMPOUNDS, PROCESSES OF PREPARING SAME AND USES THEREOF AS TRIDENTATE LIGANDS 有权
标题翻译：新型二硫代磷酸和含二氢吡啶鎓的化合物，其制备方法及其作为三氯乙烯配位体的用途
公开(公告)号：US20100292084A1
公开(公告)日：2010-11-18
申请号：US12779093
申请日：2010-05-13
申请人： Mark GANDELMAN , Elaine Melissa Schuster , Gennady Nisnevich
发明人： Mark GANDELMAN , Elaine Melissa Schuster , Gennady Nisnevich
IPC分类号： C40B20/00 , C07F9/28 , C07D249/04 , C40B40/04 , C07F15/00 , C40B40/16 , C07C247/02 , C07F9/53
CPC分类号： C07D249/04 , B01J31/189 , B01J31/226 , B01J2231/4261 , B01J2531/0244 , B01J2531/824 , B01J2531/828 , C07F9/5013 , C07F9/5304 , C07F9/6518 , C07F9/65583 , C07F15/006 , C40B30/08 , C40B40/04 , C40B40/16
摘要： A novel process of preparing tridentate ligands containing one or more of a diarylphosphine and/or dialkylphosphine electron donating groups are disclosed. Use of this process for preparing a combinatorial library of such tridentate ligands and of organometallic complexes containing same is also disclosed. Further disclosed are novel diarylphosphine-containing and dialkylphosphine-containing compounds that can serve as tridentate ligands (e.g., pincer ligands), combinatorial libraries of such tridentate ligands, organometallic complexes containing these ligands (e.g., pincer complexes), and combinatorial libraries of such complexes. Methods utilizing these libraries for screening for candidate organometallic catalysts are also disclosed. Novel precursor molecules useful for preparing the tridentate ligands and processes of preparing same are also disclosed.
摘要翻译：公开了一种制备含有一个或多个二芳基膦和/或二烷基膦给电子基团的三齿配体的新方法。还公开了该方法用于制备这种三齿配体的组合文库和含有它们的有机金属络合物的用途。还公开了可以用作三齿配体（例如夹心配体）的新型含二芳基膦和含二烷基膦的化合物，这种三齿配体的组合文库，含有这些配体的有机金属配合物（例如夹心络合物）和这种配合物的组合文库。还公开了利用这些文库筛选候选有机金属催化剂的方法。还公开了可用于制备三齿配体的新型前体分子及其制备方法。

3. 发明授权

US08822516B2 Process for the preparation of iodides 有权
标题翻译：制备碘化物的方法
公开(公告)号：US08822516B2
公开(公告)日：2014-09-02
申请号：US13703183
申请日：2011-06-09
申请人： Gennady Nisnevich , Mark Gandelman , Kseniya Kulbitski
发明人： Gennady Nisnevich , Mark Gandelman , Kseniya Kulbitski
IPC分类号： A01N43/76 , A61K31/42 , C07D205/04 , C07D263/00 , C07C67/32 , C07C22/00 , C07J9/00
CPC分类号： C07C17/093 , C07C41/22 , C07C67/32 , C07C201/12 , C07C269/06 , C07C2601/02 , C07C2601/04 , C07C2603/62 , C07C2603/90 , C07D205/04 , C07D211/38 , C07J9/00 , C07J9/005 , C07C19/075 , C07C22/04 , C07C25/22 , C07C25/18 , C07C22/00 , C07C19/07 , C07C25/02 , C07C23/46 , C07C43/225 , C07C69/753 , C07C69/74 , C07C69/76 , C07C205/11 , C07C271/22
摘要： This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.
摘要翻译：本发明涉及使用N-碘酰胺从其相应的羧酸制备高产率烷基或芳基碘的方法。

4. 发明申请

US20130165658A1 PROCESS FOR THE PREPARATION OF IODIDES 有权
标题翻译：制备碘化物的方法
公开(公告)号：US20130165658A1
公开(公告)日：2013-06-27
申请号：US13703183
申请日：2011-06-09
申请人： Gennady Nisnevich , Mark Gandelman , Kseniya Kulbitski
发明人： Gennady Nisnevich , Mark Gandelman , Kseniya Kulbitski
IPC分类号： C07C17/093 , C07D205/04 , C07C201/12 , C07C41/22 , C07D211/18 , C07C67/32 , C07J9/00 , C07D211/38 , C07C269/06
CPC分类号： C07C17/093 , C07C41/22 , C07C67/32 , C07C201/12 , C07C269/06 , C07C2601/02 , C07C2601/04 , C07C2603/62 , C07C2603/90 , C07D205/04 , C07D211/38 , C07J9/00 , C07J9/005 , C07C19/075 , C07C22/04 , C07C25/22 , C07C25/18 , C07C22/00 , C07C19/07 , C07C25/02 , C07C23/46 , C07C43/225 , C07C69/753 , C07C69/74 , C07C69/76 , C07C205/11 , C07C271/22
摘要： This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.
摘要翻译：本发明涉及使用N-碘酰胺从其相应的羧酸制备高产率烷基或芳基碘的方法。

5. 发明授权

US07247730B2 Process for the preparation of dexmethylphenidate hydrochloride 失效
标题翻译：盐酸右哌甲酯制备方法
公开(公告)号：US07247730B2
公开(公告)日：2007-07-24
申请号：US10793080
申请日：2004-03-04
申请人： Arie Gutman , Igor Zaltsman , Anton Shalimov , Maxim Sotrihin , Gennady Nisnevich , Lev Yudovich , Irina Fedotev
发明人： Arie Gutman , Igor Zaltsman , Anton Shalimov , Maxim Sotrihin , Gennady Nisnevich , Lev Yudovich , Irina Fedotev
IPC分类号： C07D211/22
CPC分类号： C07D211/34
摘要： The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising: (a) reacting a solution of threo-N-Boc-ritalinic acid with (S)-1-phenylethylamine, separating precipitated solid salt of (R,R)-enriched N-Boc-ritalinic acid with (S)-1-phenylethylamnine from the reaction mixture and recrystallizing, reslurring and/or trituring of said salt; (b) mixing the solid salt of (R,R)-N-Boc-ritalinic acid and (S)-1-phenylethylamine obtained in step (a) with aqueous acid and separating (R,R)-N-Boc-ritalinic acid from the mixture; and (c) reacting the (R,R)-N-Boc-ritalinic acid prepared in step (b) with hydrogen chloride and methanol to give dexmethylphenidate hydrochloride with optical purity of at least 99% ee. The present invention further provides salt of (R,R)-N-Boc-ritalinic acid with (S)-1-phenylethylamine as new intermediate in the preparation of dexmethylphenidate hydrochloride.
摘要翻译：本发明提供了一种用于制备具有高光学纯度的右哌醋酸盐酸盐的新型和有效的方法，该方法包括：（a）使苏氨酸-N-Boc-色氨酸与（S）-1-苯基乙胺的溶液，分离（R，R）富含N-Boc-异戊酸的沉淀固体盐与（S）-1-苯乙基胺在反应混合物中的沉淀，并重结晶，再沉淀和/或研磨所述盐; （b）将步骤（a）中得到的（R，R）-N-Boc-异戊酸和（S）-1-苯基乙胺的固体盐与酸水溶液和（R，R）-N-Boc-活化后酸从混合物中; 和（c）使步骤（b）中制备的（R，R）-N-Boc-异戊酸与氯化氢和甲醇反应，得到光学纯度为至少99％ee的盐酸偏苯甲酸酯。本发明进一步提供（R，R）-N-Boc-异戊酸与（S）-1-苯基乙胺的盐作为制备右哌甲酯盐酸盐的新中间体。

6. 发明申请

US20060135780A1 Novel synthesis of irbesartan 失效
公开(公告)号：US20060135780A1
公开(公告)日：2006-06-22
申请号：US11349360
申请日：2006-02-06
申请人： Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov , Ben-Zion Dolitzky
发明人： Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov , Ben-Zion Dolitzky
IPC分类号： C07F5/02
CPC分类号： C07D235/02 , C07D403/10
摘要： Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4′-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.

7. 发明申请

US20050176794A1 Novel synthesis of irbesartan 审中-公开
标题翻译：厄贝沙坦的新型合成
公开(公告)号：US20050176794A1
公开(公告)日：2005-08-11
申请号：US10621623
申请日：2003-07-16
申请人： Ben-Zion Dolitzky , Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov
发明人： Ben-Zion Dolitzky , Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov
IPC分类号： C07D403/10 , A61K31/41
CPC分类号： C07D403/10
摘要： Provided is a novel synthesis of irbesartan employing a phase transfer catalyst. Also provided is irbesartan having a fine particle size.
摘要翻译：提供使用相转移催化剂的厄贝沙坦的新型合成。还提供了具有细粒度的厄贝沙坦。

8. 发明申请

US20050043329A1 Crystalline forms of valacyclovir hydrochloride 审中-公开
标题翻译：盐酸伐昔洛韦的结晶形式
公开(公告)号：US20050043329A1
公开(公告)日：2005-02-24
申请号：US10791451
申请日：2004-03-01
申请人： Shlomit Wizel , Judith Aronhime , Valerie Niddam-Hildesheim , Ben-Zion Dolitzky , Marina Etinger , Michael Yuzefovich , Gennady Nisnevich , Boris Pertsikov , Boris Tishin , Dina Blasberger
发明人： Shlomit Wizel , Judith Aronhime , Valerie Niddam-Hildesheim , Ben-Zion Dolitzky , Marina Etinger , Michael Yuzefovich , Gennady Nisnevich , Boris Pertsikov , Boris Tishin , Dina Blasberger
IPC分类号： A61K31/522 , C07D473/00 , C07D473/18
CPC分类号： A61K31/522 , C07D473/00 , C07D473/18
摘要： Provided are novel crystalline forms of valacyclovir hydrochloride, in particular a novel hydrated form of valacyclovir hydrochloride having about 6% to about 10% by weight water. Also provided are methods for making the novel crystalline forms.
摘要翻译：提供盐酸伐昔洛韦的新型结晶形式，特别是具有约6％至约10％重量水的新型水合形式的盐酸伐昔洛韦。还提供了制备新型结晶形式的方法。

9. 发明授权

US07332612B2 Amorphous and crystalline forms of losartan potassium and process for their preparation 失效
标题翻译：氯沙坦钾的无定形和结晶形式及其制备方法
公开(公告)号：US07332612B2
公开(公告)日：2008-02-19
申请号：US10293820
申请日：2002-11-13
申请人： Ben Zion Dolitzky , Shlomit Wizel , Gennady Nisnevich , Igor Rukhman , Julia Kaftanov
发明人： Ben Zion Dolitzky , Shlomit Wizel , Gennady Nisnevich , Igor Rukhman , Julia Kaftanov
IPC分类号： C07D403/10
CPC分类号： C07D403/10
摘要： This invention relates to novel amorphous losartan potassium, novel losartan potassium in a crystalline form that is a hydrate, novel crystalline losartan potassium Form IV and solvates thereof, novel crystalline losartan potassium Form V and solvates thereof, to processes for their preparation, to compositions containing them and to their use in medicine. This invention further relates to a novel process for preparing crystalline losartan potassium Form I and Form II.
摘要翻译：本发明涉及新型无定形洛沙坦钾，结晶形式的新型氯沙坦钾，其为水合物，新型结晶氯沙坦钾形式IV及其溶剂合物，新型结晶氯沙坦钾V型及其溶剂化物，其制备方法，含有他们和他们在医学中的使用。本发明还涉及一种制备结晶氯沙坦钾I型和II型的新方法。

10. 发明申请

US20070213539A1 Novel synthesis of irbesartan 失效
标题翻译：厄贝沙坦的新型合成
公开(公告)号：US20070213539A1
公开(公告)日：2007-09-13
申请号：US11800332
申请日：2007-05-04
申请人： Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov , Ben-Zion Dolitzky
发明人： Gennady Nisnevich , Igor Rukhman , Boris Pertsikov , Julia Kaftanov , Ben-Zion Dolitzky
IPC分类号： C07D403/02
CPC分类号： C07D235/02 , C07D403/10
摘要： Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4′-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.
摘要翻译：提供通过Suzuki偶联反应制备厄贝沙坦的方法和新的中间体2-丁基-3-（4'-溴苄基）-1,3-二氮杂螺[4.4]壬-1-烯-4-酮的方法处理。该新方法包括使这种中间体与受保护的咪唑苯基硼酸反应的步骤。

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