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1. 发明授权

US08282793B2 Continuous process for preparing neral in pure or enriched form 有权
标题翻译：用于制备纯净或富集形式的连续方法
公开(公告)号：US08282793B2
公开(公告)日：2012-10-09
申请号：US12666478
申请日：2008-06-09
申请人： Gunnar Heydrich , Nawid Kashani-Shirazi , Christoph Jäkel , Joachim Schmidt-Leithoff
发明人： Gunnar Heydrich , Nawid Kashani-Shirazi , Christoph Jäkel , Joachim Schmidt-Leithoff
IPC分类号： B01D3/00
CPC分类号： B01D3/143 , B01D3/14 , B01D3/141 , C07C45/83 , C07C47/21
摘要： The present invention relates to a continuous process for preparing neral (cis-citral) in pure or enriched form by distillatively separating neral from substance mixtures comprising essentially neral and geranial (trans-citral). This distillative separation is performed in a dividing wall column or in a connection of two distillation columns in the form of a thermal coupling.
摘要翻译：本发明涉及通过从包含基本上和野生（反 - 柠檬醛）的物质混合物中蒸馏分离出来的来制备纯的或富集形式的盐酸（顺 - 柠檬醛）的连续方法。这种蒸馏分离在分隔壁塔中或以热耦合形式的两个蒸馏塔的连接中进行。

2. 发明申请

US20100249467A1 METHOD FOR PRODUCING OPTICALLY ACTIVE, RACEMIC MENTHOL 有权
标题翻译：用于生产光学活性的，法定的MENTHOL的方法
公开(公告)号：US20100249467A1
公开(公告)日：2010-09-30
申请号：US12744110
申请日：2008-11-13
申请人： Gunnar Heydrich , Gabriele Gralla , Matthias Rauls , Joachim Schmidt-Leithoff , Klaus Ebel , Wolfgang Krause , Steffen Oehlenschläger , Christoph Jäkel , Marko Friedrich , Eike Johannes Bergner , Nawid Kashani-Shirazi , Rocco Paciello
发明人： Gunnar Heydrich , Gabriele Gralla , Matthias Rauls , Joachim Schmidt-Leithoff , Klaus Ebel , Wolfgang Krause , Steffen Oehlenschläger , Christoph Jäkel , Marko Friedrich , Eike Johannes Bergner , Nawid Kashani-Shirazi , Rocco Paciello
IPC分类号： C07C35/12
CPC分类号： C07C29/56 , C07B2200/07 , C07C29/172 , C07C29/78 , C07C45/62 , C07C45/82 , C07C2601/14 , C07C2601/16 , C07C47/21 , C07C35/12 , C07C35/17
摘要： The present invention relates to a particularly economic overall method for producing menthol, specifically for producing optically active, essentially enantiomerically and diastereomerically pure L-menthol and racemic menthol, starting from the starting material citral which is available inexpensively on an industrial scale. The method comprises the following stepsa.1) catalytic hydrogenation of neral and/or geranial to give citronellal, b.1) cyclization of citronellal to isopulegol in the presence of an acidic catalyst, c.1) purification of isopulegol by crystallization and d.1) catalytic hydrogenation of isopulegol to give menthol.
摘要翻译：本发明涉及一种特别经济的制备薄荷醇的总体方法，特别用于制备光学活性的，基本上是对映异构体和非对映异构体纯的L-薄荷醇和外消旋薄荷醇，其原料柠檬醛以工业规模廉价地得到。该方法包括以下步骤a.1）在酸性催化剂的存在下，将柠檬醛和/或香叶醇进行催化氢化以产生香茅醛，b.1）将香茅醛环化成异胡仑醇，c.1）通过结晶和d进行异丙醇的纯化 .1）异丙醇的催化氢化得到薄荷醇。

3. 发明申请

US20130046118A1 METHOD FOR PRODUCING OPTICALLY ACTIVE, RACEMIC MENTHOL 审中-公开
标题翻译：用于生产光学活性的，法定的MENTHOL的方法
公开(公告)号：US20130046118A1
公开(公告)日：2013-02-21
申请号：US13658003
申请日：2012-10-23
申请人： Gunnar Heydrich , Gabriele Gralla , Matthias Rauls , Joachim Schmidt-Leithoff , Klaus Ebel , Wolfgang Krause , Steffen Oehlenschläger , Christoph Jäkel , Marko Friedrich , Eike Johannes Bergner , Nawid Kashani-Shirazi , Rocco Paciello
发明人： Gunnar Heydrich , Gabriele Gralla , Matthias Rauls , Joachim Schmidt-Leithoff , Klaus Ebel , Wolfgang Krause , Steffen Oehlenschläger , Christoph Jäkel , Marko Friedrich , Eike Johannes Bergner , Nawid Kashani-Shirazi , Rocco Paciello
IPC分类号： C07C29/17
CPC分类号： C07C29/56 , C07B2200/07 , C07C29/172 , C07C29/78 , C07C45/62 , C07C45/82 , C07C2601/14 , C07C2601/16 , C07C47/21 , C07C35/12 , C07C35/17
摘要： The present invention relates to a particularly economic overall method for producing menthol, specifically for producing optically active, essentially enantiomerically and diastereomerically pure L-menthol and racemic menthol, starting from the starting material citral which is available inexpensively on an industrial scale. The method comprises the following steps a.1) catalytic hydrogenation of neral and/or geranial to give citronellal, b.1) cyclization of citronellal to isopulegol in the presence of an acidic catalyst, c.1) purification of isopulegol by crystallization and d.1) catalytic hydrogenation of isopulegol to give menthol.
摘要翻译：本发明涉及一种特别经济的制备薄荷醇的总体方法，特别用于制备光学活性的，基本上是对映异构体和非对映异构体纯的L-薄荷醇和外消旋薄荷醇，其原料柠檬醛以工业规模廉价地得到。该方法包括以下步骤a.1）在酸性催化剂的存在下，将柠檬醛和/或香叶醇进行催化氢化以产生香茅醛，b.1）将香茅醛环化成异胡仑醇，c.1）通过结晶和d进行异丙醇的纯化 .1）异丙醇的催化氢化得到薄荷醇。

4. 发明申请

US20100193348A1 CONTINUOUS PROCESS FOR PREPARING NERAL IN PURE OR ENRICHED FORM 有权
标题翻译：用于准备纯粹或加强形式的NERAL的连续过程
公开(公告)号：US20100193348A1
公开(公告)日：2010-08-05
申请号：US12666478
申请日：2008-06-09
申请人： Gunnar Heydrich , Nawid Kashani-Shirazi , Christoph Jäkel , Joachim Schmidt-Leithoff
发明人： Gunnar Heydrich , Nawid Kashani-Shirazi , Christoph Jäkel , Joachim Schmidt-Leithoff
IPC分类号： B01D3/14
CPC分类号： B01D3/143 , B01D3/14 , B01D3/141 , C07C45/83 , C07C47/21
摘要： The present invention relates to a continuous process for preparing neral (cis-citral) in pure or enriched form by distillatively separating neral from substance mixtures comprising essentially neral and geranial (trans-citral). This distillative separation is performed in a dividing wall column or in a connection of two distillation columns in the form of a thermal coupling.
摘要翻译：本发明涉及通过从包含基本上和野生（反 - 柠檬醛）的物质混合物中蒸馏分离出来的来制备纯的或富集形式的盐酸（顺 - 柠檬醛）的连续方法。这种蒸馏分离在分隔壁塔中或以热耦合形式的两个蒸馏塔的连接中进行。

5. 发明授权

US08318985B2 Method for producing optically active, racemic menthol 有权
标题翻译：光学活性外消旋薄荷醇的制备方法
公开(公告)号：US08318985B2
公开(公告)日：2012-11-27
申请号：US12744110
申请日：2008-11-13
申请人： Gunnar Heydrich , Gabriele Gralla , Matthias Rauls , Joachim Schmidt-Leithoff , Klaus Ebel , Wolfgang Krause , Steffen Oehlenschläger , Christoph Jäkal , Marko Friedrich , Eike Johannes Bergner , Nawid Kashani-Shirazi , Rocco Paciello
发明人： Gunnar Heydrich , Gabriele Gralla , Matthias Rauls , Joachim Schmidt-Leithoff , Klaus Ebel , Wolfgang Krause , Steffen Oehlenschläger , Christoph Jäkal , Marko Friedrich , Eike Johannes Bergner , Nawid Kashani-Shirazi , Rocco Paciello
IPC分类号： C07C29/17
CPC分类号： C07C29/56 , C07B2200/07 , C07C29/172 , C07C29/78 , C07C45/62 , C07C45/82 , C07C2601/14 , C07C2601/16 , C07C47/21 , C07C35/12 , C07C35/17
摘要： The present invention relates to a particularly economic overall method for producing menthol, specifically for producing optically active, essentially enantiomerically and diastereomerically pure L-menthol and racemic menthol, starting from the starting material citral which is available inexpensively on an industrial scale. The method comprises the following stepsa) catalytic hydrogenation of neral and/or geranial to give citronellal,b) cyclization of citronellal to isopulegol in the presence of an acidic catalyst,c) purification of isopulegol by crystallization andd) catalytic hydrogenation of isopulegol to give menthol.
摘要翻译：本发明涉及一种特别经济的制备薄荷醇的总体方法，特别用于制备光学活性的，基本上是对映异构体和非对映异构体纯的L-薄荷醇和外消旋薄荷醇，其原料柠檬醛以工业规模廉价地得到。该方法包括以下步骤：a）在酸性催化剂存在下，通过催化氢化醛和/或香叶醇以产生香茅醛，b）在酸性催化剂的存在下将香茅醛环化成异葎草醇，c）通过结晶纯化异丙醇钾，和d）将异丙醇的催化氢化至给薄荷脑

6. 发明授权

US07973198B2 Method for synthesizing optically active carbonyl compounds 有权
标题翻译：光学活性羰基化合物的合成方法
公开(公告)号：US07973198B2
公开(公告)日：2011-07-05
申请号：US12597025
申请日：2008-04-17
申请人： Joachim Schmidt-Leithoff , Christoph Jäkel , Rocco Paciello
发明人： Joachim Schmidt-Leithoff , Christoph Jäkel , Rocco Paciello
IPC分类号： C07C45/62
CPC分类号： C07C29/172 , C07B53/00 , C07B2200/07 , C07C29/56 , C07C45/62 , C07C2601/14 , C07C35/12 , C07C35/17 , C07C47/21
摘要： The present invention relates to a process for preparing optically active carbonyl compounds by asymmetrically hydrogenating α,β-unsaturated carbonyl compounds in the presence of optically active transition metal catalysts which are soluble in the reaction mixture and have at least one carbon monoxide ligand, the optically active catalyst which has at least one carbon monoxide ligand and is to be used in each case being prepared by pretreating a catalyst precursor with a gas mixture comprising carbon monoxide and hydrogen and the asymmetric hydrogenation being performed in the presence of carbon monoxide supplied additionally to the reaction mixture.
摘要翻译：本发明涉及一种通过在光学活性的过渡金属催化剂的存在下不对称氢化α，β-不饱和羰基化合物来制备光学活性的羰基化合物的方法，其可溶于反应混合物并具有至少一种一氧化碳配体，具有至少一种一氧化碳配体并且在每种情况下使用的光学活性催化剂通过用包含一氧化碳和氢气的气体混合物预处理催化剂前体而制备，并且在另外提供的一氧化碳的存在下进行不对称氢化反应混合物。

7. 发明申请

US20100152494A1 METHOD FOR SYNTHESIZING OPTICALLY ACTIVE CARBONYL COMPOUNDS 有权
标题翻译：用于合成光学活性碳化合物的方法
公开(公告)号：US20100152494A1
公开(公告)日：2010-06-17
申请号：US12597025
申请日：2008-04-17
申请人： Joachim Schmidt-Leithoff , Christoph Jäkel , Rocco Paciello
发明人： Joachim Schmidt-Leithoff , Christoph Jäkel , Rocco Paciello
IPC分类号： C07C45/00 , C07C35/12
CPC分类号： C07C29/172 , C07B53/00 , C07B2200/07 , C07C29/56 , C07C45/62 , C07C2601/14 , C07C35/12 , C07C35/17 , C07C47/21
摘要： The present invention relates to a process for preparing optically active carbonyl compounds by asymmetrically hydrogenating α,β-unsaturated carbonyl compounds in the presence of optically active transition metal catalysts which are soluble in the reaction mixture and have at least one carbon monoxide ligand, the optically active catalyst which has at least one carbon monoxide ligand and is to be used in each case being prepared by pretreating a catalyst precursor with a gas mixture comprising carbon monoxide and hydrogen and the asymmetric hydrogenation being performed in the presence of carbon monoxide supplied additionally to the reaction mixture.
摘要翻译：本发明涉及一种通过在光学活性的过渡金属催化剂的存在下不对称氢化α，β-不饱和羰基化合物来制备光学活性的羰基化合物的方法，其可溶于反应混合物并具有至少一种一氧化碳配体，具有至少一种一氧化碳配体并且在每种情况下使用的光学活性催化剂通过用包含一氧化碳和氢气的气体混合物预处理催化剂前体而制备，并且在另外提供的一氧化碳的存在下进行不对称氢化反应混合物。

8. 发明授权

US08153820B2 Method for the production of N-substituted (3-dihalomethyl-1-methylpyrazol-4-yl) carboxamides 有权
标题翻译：制备N-取代的（3-二卤代甲基-1-甲基吡唑-4-基）甲酰胺的方法
公开(公告)号：US08153820B2
公开(公告)日：2012-04-10
申请号：US12601966
申请日：2008-05-30
申请人： Thomas Zierke , Joachim Rheinheimer , Michael Rack , Sebastian Peer Smidt , Ansgar Gereon Altenhoff , Joachim Schmidt-Leithoff , Nina Challand
发明人： Thomas Zierke , Joachim Rheinheimer , Michael Rack , Sebastian Peer Smidt , Ansgar Gereon Altenhoff , Joachim Schmidt-Leithoff , Nina Challand
IPC分类号： C07D231/10
CPC分类号： C07D231/14
摘要： The present invention relates to a process for preparing N-substituted (3-dihalomethylpyrazol-4-yl)carboxamides of the formula (I) in which R1 is optionally substituted phenyl or C3-C7-cycloalkyl, R1a is hydrogen or fluorine, or R1a together with R1 is optionally substituted C3-C5-alkanediyl or C5-C7-cycloalkanediyl, R2 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C4-alkoxy-C1-C2-alkyl, X is F or Cl and n is 0, 1, 2 or 3; which comprises A) providing a compound of the formula (II) in which X is F or Cl, Y is Cl or Br and R2 has one of the meanings given above and B) reacting a compound of the formula (II) with carbon monoxide and a compound of the formula (III) in which R1, R1a and n have one of the meanings given above; in the presence of a palladium catalyst; to intermediates used for the preparation according to the process according to the invention, and also to processes for their preparation.
摘要翻译：本发明涉及式（I）的N-取代的（3-二卤代甲基吡唑-4-基）甲酰胺的制备方法，其中R 1为任选取代的苯基或C 3 -C 7 - 环烷基，R 1a为氢或氟，或R 1a R 1是C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基或C 1 -C 4 - 烷氧基-C 1 -C 2 - 烷基，其中R 1是任选取代的C 3 -C 5 - 烷二基或C 5 -C 7 - 环烷二基， X是F或Cl，n是0,1,2或3; 其包括A）提供其中X为F或Cl，Y为Cl或Br的式（II）化合物，R 2具有上述含义之一，B）使式（II）化合物与一氧化碳和其中R1，R1a和n具有上述含义之一的式（III）化合物; 在钯催化剂的存在下; 用于根据本发明的方法制备的中间体，以及其制备方法。

9. 发明申请

US20110105766A1 Method for Producing Substituted Biphenyls 有权
标题翻译：生产取代联苯的方法
公开(公告)号：US20110105766A1
公开(公告)日：2011-05-05
申请号：US13001070
申请日：2009-06-22
申请人： Sebastian Peer Smidt , Volker Maywald , Kathrin Wissel-Stoll , Joachim Schmidt-Leithoff , Ansgar Gereon Altenhoff , Michael Keil
发明人： Sebastian Peer Smidt , Volker Maywald , Kathrin Wissel-Stoll , Joachim Schmidt-Leithoff , Ansgar Gereon Altenhoff , Michael Keil
IPC分类号： C07D231/10 , C07C205/06 , C07C211/43
CPC分类号： C07C205/11 , C07C201/12
摘要： A process for preparing substituted biphenyls of the formula I where R1=nitro or amino, R2=cyano, halogen, C1-C4-haloalkyl, C1-C4-haloalkoxy or C1-C4-haloalkylthio, n=from 0 to 3, and R3=hydrogen, cyano or halogen, which comprises reacting a halobenzene of the formula II in which Hal is chlorine or bromine, in the presence of a base and of a palladium catalyst which consists of palladium and a bidentate phosphorus ligand of the formula III where Ar is phenyl which is substituted if desired and R4 and R5 are each C1-C8-alkyl or C3-C6-cycloalkyl or together form a 2- to 7-membered bridge which may, if desired, bear a C1-C6-alkyl substituent, in a solvent or diluent, with a phenylboronic acid IVa a diphenylborinic acid IVb or a mixture of IVa and IVb.
摘要翻译：制备式I的取代的联苯的方法，其中R 1 =硝基或氨基，R 2 =氰基，卤素，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基或C 1 -C 4卤代烷硫基，n = 0至3， =氢，氰基或卤素，其包括在碱的存在下使Hal为氯或溴的式II的卤代苯与由式III的二齿磷配体组成的钯催化剂反应，其中Ar 是如果需要被取代的苯基，并且R 4和R 5各自是C 1 -C 8 - 烷基或C 3 -C 6 - 环烷基或一起形成2-7元桥，如果需要，其可以具有C 1 -C 6烷基取代基，在溶剂或稀释剂中与苯基硼酸IVa为二苯基硼酸IVb或IVa和IVb的混合物。

10. 发明授权

US08703992B2 Method for producing aromatic and heteroaromatic carboxylic acids, carboxylic acid esters and carboxylic acid amides 有权
标题翻译：芳族和杂芳族羧酸，羧酸酯和羧酸酰胺的制备方法
公开(公告)号：US08703992B2
公开(公告)日：2014-04-22
申请号：US12994271
申请日：2009-05-25
申请人： Nina Challand , Ansgar Gereon Altenhoff , Joachim Schmidt-Leithoff , Kathrin Wissel-Stoll , Michael Rack , Joachim Rheinheimer
发明人： Nina Challand , Ansgar Gereon Altenhoff , Joachim Schmidt-Leithoff , Kathrin Wissel-Stoll , Michael Rack , Joachim Rheinheimer
IPC分类号： C07C67/36
CPC分类号： C07C231/10 , C07C51/10 , C07C67/36 , C07C63/04 , C07C69/76 , C07C235/84
摘要： Process for the preparation of aromatic and heteroaromatic carboxylic acids, carboxylic acid esters and carboxamides by the reaction of aromatic or heteroaromatic halides R—Xn, in which n=integer from 1 to 6, R=substituted or unsubstituted and aromatic or heteroaromatic radical and X=chlorine, bromine or iodine atom, with carbon monoxide and water, ammonia, alcohols or amines in the presence of bases and zero-valent or divalent palladium compounds and bidentate diphosphanes or complexes of zero-valent or divalent palladium with bidentate diphosphanes, in which use is made of bidentate diphosphanes (R1—)(R2—)P—Y—P(—R3)(—R4) in which R1 to R4=unsubstituted aryl radicals or aryl radicals substituted with at least one radical exhibiting a positive resonance effect or a positive inductive effect, or unsubstituted or substituted cycloalkyl radicals, and Y=hydrocarbon group with a total of 2 to 20 carbon atoms, in which at least one of the carbon atoms carries only one or no hydrogen atom as substituent; except for the reaction of 4-bromo-3-difluoromethyl-1-methylpyrazole with 2-(3,4,5-trifluorophenyl)aniline and carbon monoxide to give N-[2-(3,4,5-trifluorophenyl)phenyl]-3-difluoromethyl-1-methylpyrazole-4-carboxamide.
摘要翻译：通过芳族或杂芳族卤化物R-Xn的反应制备芳族和杂芳族羧酸，羧酸酯和羧酰胺的方法，其中n = 1至6的整数，R =取代或未取代的芳族或杂芳族基团和X 在碱和零价或二价钯化合物和二价二膦或零价或二价钯与二齿二膦的配合物存在下，用一氧化碳和水，氨，醇或胺进行氯，溴或碘原子，其中使用二价二膦（R1 - ）（R2-）P-Y-P（-R3）（ - R4），其中R1至R4 =未取代的芳基或被至少一个表现出正共振效应的基团取代的芳基或正电感效应，或未取代或取代的环烷基，Y =总共2至20个碳原子的烃基，其中至少一个碳原子仅携带一个或不具有氢原子原子作为取代基; 除了4-溴-3-二氟甲基-1-甲基吡唑与2-（3,4,5-三氟苯基）苯胺和一氧化碳反应，得到N- [2-（3,4,5-三氟苯基）苯基] -3-二氟甲基-1-甲基吡唑-4-甲酰胺。

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