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1. 发明专利

JP2005060399A Hydrogenation method 有权
标题翻译：氢化方法
公开(公告)号：JP2005060399A
公开(公告)日：2005-03-10
申请号：JP2004237823
申请日：2004-08-18
申请人： Merck Patent Gmbh , メルクパテントゲゼルシャフトミットベシュレンクテルハフトングMerck Patent Gesellschaft mit beschraenkter Haftung
发明人： KRALIK JOACHIM , MUERMANN CHRISTOPH , LEHMANN STEFAN , POETSCH EIKE DR , MEYER VOLKER , WERNER BINDER
IPC分类号： B01J31/24 , C07B53/00 , C07B61/00 , C07C41/20 , C07C43/225 , C07D309/04 , C07D309/06 , C07D309/08 , C07D309/20 , C07D309/22 , C07D309/28
CPC分类号： C07C41/20 , B01J31/24 , C07B2200/07 , C07C2601/14 , C07D309/04 , C07D309/06 , C07D309/08 , C07D309/20 , C07D309/22 , C07D309/28 , C07C43/225
摘要： PROBLEM TO BE SOLVED: To provide a production method of a 1,4-disubstituted cyclohexane derivative and a 2,5-disubstituted tetrahydropyran derivative, whereby a target trans-isomer can be more easily obtained, especially with a high selectivity in a high overall yield.
SOLUTION: The production method is for producing e.g. a compound of formula 2, e.g. by hydrogenating a compound of formula 1 in the presence of a transition metal complex which is stabilized by one or more phosphine ligands which are identical to or different from each other.
COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：要解决的问题：提供1,4-二取代的环己烷衍生物和2,5-二取代的四氢吡喃衍生物的制备方法，由此可以更容易地获得目标反式异构体，特别是以高选择性总产量很高。解决方案：制备方法用于制备例如式2的化合物，例如在通过一个或多个彼此相同或不同的膦配体稳定的过渡金属络合物的存在下氢化式1的化合物。版权所有（C）2005，JPO＆NCIPI

2. 发明专利

AU2016316436B2 Method for the production of praziquantel and precursors thereof 未知
公开(公告)号：AU2016316436B2
公开(公告)日：2021-04-29
申请号：AU2016316436
申请日：2016-08-10
申请人： MERCK PATENT GMBH
发明人： EBERHARDT LUC , WAECHTLER ANDREAS , MAILLARD DAVID , LEHMANN STEFAN
IPC分类号： C07D217/14 , C07B53/00
摘要： The present invention provides methods of preparing Praziquantel, in particular (R)-Praziquantel and analogues thereof in a stereoselective manner. One method involves asymmetric hydrogenation of the following intermediate compound (I) and subsequent cyclization.

3. 发明专利

AU9545301A Method for hydrogenating c-c double bonds 未知
公开(公告)号：AU9545301A
公开(公告)日：2002-03-22
申请号：AU9545301
申请日：2001-08-09
申请人： MERCK PATENT GMBH
发明人： LEHMANN STEFAN , KOPPE THOMAS
IPC分类号： C07B61/00 , C07D495/04 , C07C5/02 , C07D333/00 , C07D235/00
摘要： The present invention relates to a gentle process for catalytic hydrogenation and to a process for the preparation of biotin using the hydrogenation step. The process according to the invention for the selective, catalytic hydrogenation of a C-C double bond on a thiazole ring system having at least one functional group which can be converted into a salt under basic conditions is characterised in that the hydrogenation is carried out in a protic solvent is a pH>7.

4. 发明专利

DE10135681A1 未知
公开(公告)号：DE10135681A1
公开(公告)日：2002-03-14
申请号：DE10135681
申请日：2001-07-21
申请人： MERCK PATENT GMBH
发明人： LEHMANN STEFAN , KOPPE THOMAS
IPC分类号： C07D495/04 , C07B35/02
摘要： The invention relates to a mild catalytic hydrogenation method and to a method for producing biotin, using the hydrogenation step. The inventive method for the selective, catalytic hydrogenation of a C-C double bond on a thiazole ring system, comprising at least one functional group that can be salinized in an alkaline manner, is characterized in that the hydrogenation is carried out in a protic solvent at a pH value > 7.

5. 发明专利

CA2996813A1 METHOD FOR THE PRODUCTION OF PRAZIQUANTEL AND PRECURSORS THEREOF 未知
公开(公告)号：CA2996813A1
公开(公告)日：2017-03-09
申请号：CA2996813
申请日：2016-08-10
申请人： MERCK PATENT GMBH
发明人： EBERHARDT LUC , WAECHTLER ANDREAS , MAILLARD DAVID , LEHMANN STEFAN
IPC分类号： C07D217/14 , C07B53/00
摘要： The present invention provides methods of preparing Praziquantel, in particular (R)-Praziquantel and analogues thereof in a stereoselective manner. One method involves asymmetric hydrogenation of the following intermediate compound (I) and subsequent cyclization.

6. 发明专利

DE102004036068A1 Disubstituted cyclohexane or tetrahydropyran derivative preparation, for use e.g. in liquid crystals, by trans-selective hydrogenation of cyclohexene or dihydropyran derivative over transition metal phosphine complex 未知
公开(公告)号：DE102004036068A1
公开(公告)日：2005-03-10
申请号：DE102004036068
申请日：2004-07-24
申请人： MERCK PATENT GMBH
发明人： KRALIK JOACHIM , MUERMANN CHRISTOPH , LEHMANN STEFAN , POETSCH EIKE , MEYER VOLKER , BINDER WERNER
IPC分类号： B01J31/24 , C07B53/00 , C07B61/00 , C07C41/20 , C07C43/225 , C07D309/04 , C07D309/06 , C07D309/08 , C07D309/20 , C07D309/22 , C07D309/28 , C07B35/02
摘要： Production of 1,4-disubstituted cyclohexane or 2,5-disubstituted tetrahydropyran derivatives (I) involves hydrogenating a corresponding cyclohexene or dihydropyran derivative (II) in presence of a transition metal complex (III) stabilized by one or more same or different phosphine ligands. Production of cyclohexane or tetrahydropyran derivatives (I) of formula (IA) or (IB) involves hydrogenating a corresponding cyclohexene or dihydropyran derivative (II) of formula (IIA) or (IIB) in presence of a transition metal complex (III) stabilized by one or more same or different phosphine ligands. [Image] [Image] W : O or CH 2; a - e and f - j : 0 or 1, provided that e and j = 1 if W = CH 2; A 1>1>- A 1>5>, A 2>1>- A 2>5>1,4-cyclohexylene (in which 1 or 2 non-adjacent CH 2groups are optionally replaced by O and/or S), 1,4-phenylene (in which 1 or 2 non-adjacent CH groups are optionally replaced by N), naphthalene-2,6-diyl or 1,2,3,4-tetrahydronaphthalene-2,6-diyl (all optionally substituted (os) by one or more of halo or CN); or 1,3-cyclobutylene, piperidine-1,4-diyl or decahydronaphthalene-2,6-diyl; R 1>1>H or 1-15C alkyl (os and optionally having one or more CH 2groups replaced by CC, S, O, CO, COO, OCO or OCOO, provided that heteroatoms are not directly linked), provided that R 1>1>is not H if a = b = 0 and Z 1>2>= direct bond; R 2>1>H or 1-15C alkyl (os and optionally having one or more CH 2groups replaced by CH=CH, CC, S, O, CO, COO, OCO or OCOO, provided that heteroatoms are not directly linked), provided that R 2>1>is not H if f = g = 0 and Z 2>2>= direct bond; Y 1>1>H, halo, NCS, SCN, SF 6or CN; or 1-15C alkyl (os by one or more of halo or CN) or 7-16C aralkyl (os by one or more of halo, NO 2, alkanoyl, alkoxy, NH 2or dialkanoylamino) (both optionally having one or more CH 2groups replaced by CC, S, SO, SO 2, O, CO, COO, OCO or OCOO, provided that heteroatoms are not directly linked); Y 2>1>H, halo, NCS, SCN, SF 6or CN; or os 1-15C alkyl or 7-16C aralkyl (both optionally having one or more CH 2groups replaced by CH=CH, CC, S, SO, SO 2, O, CO, COO, OCO or OCOO, provided that heteroatoms are not directly linked); Z 1>1>, Z 1>3>- Z 1>5>direct bond, CH 2CH 2, CF 2CF 2, CHCF 2, CF 2CH 2, CHFCHF, CC, CH 2O, OCH 2, CF 2O, OCF 2, COO or OCO; Z 2>1>, Z 2>3>- Z 2>5>direct bond, CH=CH, CH 2CH 2, CF 2CF 2, CHCF 2, CF 2CH 2, CHFCHF, CC, CH 2O, OCH 2, CF 2O, OCF 2, COO or OCO; Z 1>2>direct bond, CH 2CH 2, CC, CH 2O, OCH 2, COO or OCO; Z 2>2>direct bond, CH=CH, CH 2CH 2, CC, CH 2O, OCH 2, COO or OCO. An independent claim is included for compositions comprising a compound (II) and at least one of the stabilized complexes (III).

7. 发明专利

BR112018002881B1 Métodos para produção de praziquantel e de seus precursores 未知
公开(公告)号：BR112018002881B1
公开(公告)日：2022-06-07
申请号：BR112018002881
申请日：2016-08-10
申请人： MERCK PATENT GMBH
发明人： WAECHTLER ANDREAS , MAILLARD DAVID , EBERHARDT LUC , LEHMANN STEFAN
IPC分类号： C07B53/00 , C07D217/14
摘要： método para produção de prazi-quantel e precursores do mesmo. a presente invenção refere-se a métodos de preparação de praziquantel, em particular (r)-praziquantel, e análogos do mesmo de uma maneira estereosseletiva. um método envolve hidrogenação assimétrica do composto (i) intermediário que segue e ciclização subsequente.

8. 发明专利

IL257814A Method for the production of praziquantel 未知
公开(公告)号：IL257814A
公开(公告)日：2021-03-25
申请号：IL25781418
申请日：2018-03-01
申请人： MERCK PATENT GMBH , WAECHTLER ANDREAS , MAILLARD DAVID , EBERHARDT LUC , LEHMANN STEFAN
发明人： WAECHTLER ANDREAS , MAILLARD DAVID , EBERHARDT LUC , LEHMANN STEFAN
IPC分类号： B01J31/12 , B01J31/24 , C07B53/00
摘要： and subsequent cyclization.

9. 发明专利

AU2016316436A1 Method for the production of praziquantel and precursors thereof 未知
公开(公告)号：AU2016316436A1
公开(公告)日：2018-04-26
申请号：AU2016316436
申请日：2016-08-10
申请人： MERCK PATENT GMBH
发明人： EBERHARDT LUC , WAECHTLER ANDREAS , MAILLARD DAVID , LEHMANN STEFAN
IPC分类号： C07D217/14 , C07B53/00
摘要： The present invention provides methods of preparing Praziquantel, in particular (R)-Praziquantel and analogues thereof in a stereoselective manner. One method involves asymmetric hydrogenation of the following intermediate compound (I) and subsequent cyclization.

10. 发明专利

ES2811271T3 Método para la producción de praziquantel y sus precursores 未知
公开(公告)号：ES2811271T3
公开(公告)日：2021-03-11
申请号：ES16750623
申请日：2016-08-10
申请人： MERCK PATENT GMBH
发明人： EBERHARDT LUC , WAECHTLER ANDREAS , MAILLARD DAVID , LEHMANN STEFAN
IPC分类号： C07D217/14 , C07B53/00
摘要： Un metodo de preparacion de (i) un compuesto opticamente activo segun la siguiente formula (X1) **(Ver fórmula)** o (ii) un compuesto opticamente activo segun la siguiente formula (X2) **(Ver fórmula)** o (iii) una mezcla de los dos, donde R se selecciona entre alquilo C1-C8, cicloalquilo C3-C8, y arilo sustituido o no sustituido, que comprende: someter a un compuesto segun la siguiente formula (Y) **(Ver fórmula)** con R como anteriormente, a una etapa de hidrogenacion, donde la mezcla comprende el compuesto segun la formula (X1) o el compuesto segun la formula (X2) en exceso y donde la etapa de hidrogenacion es una etapa de hidrogenacion asimetrica en presencia de un catalizador.

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