专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2009056077A2 A NEW METHOD OF MANUFACTURING 2-(6-(4-CHLOROPHENYL)-2,2-DIMETHYL-7-PHENYL-2,3-DIHYDRO-LH-PYRROLIZINE-5-YL)ACETIC ACID (LICOFELONE) 审中-公开
标题翻译：制备2-（6-（4-氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-4-羟基吡咯烷-5-基）乙酸（LICOFELONE）的新方法
公开(公告)号：WO2009056077A2
公开(公告)日：2009-05-07
申请号：PCT/CZ2008/000116
申请日：2008-09-29
申请人： ZENTIVA, A.S. , RADL, Stanislav , KLECAN, Ondrej
发明人： RADL, Stanislav , KLECAN, Ondrej
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A method of manufacturing 2-(6-(4-chlorophenyl)-2,2-dirnethyl-7-phenyl-2,3-dihydro-l H - pyrrolizine-5-yl)acetic acid of formula I, wherein 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl- 2,3-dihydro-l H -pyrrolizine of formula II is alkylated with a iodo derivative of formula VII, wherein A is either the cyano group CN or an ester group COOR, wherein R is an (un)branched C 1 -C 6 alkyl group, with the use of the Fenton reagent in the presence of a sulfoxide of formula R 1 -SO-R 2 , wherein R 1 is an (un)branched C 1 -C 12 alkyl group, R 2 is either an (un)branched C 1 -C 12 alkyl group, an aryl group or a substituted aryl group, or wherein R 1 , R 2 are independently (CΗ 2 ) m X(CΗ 2 ) n , wherein X = CH 2 , O, S, NR 3 , m = 1-3, n = 1-3 and R 3 is either an (un)branched C 1 -C 12 alkyl group, an aryl group or a substituted aryl group, the reaction being carried out in the environment of the sulfoxide used or in its mixture with suitable solvents at a temperature of O 0C to 80 °C, preferably at temperatures in the range of 10 to 40 °C, and the resulting ester of formula IV or nitrile of formula VIII is hydrolyzed to the desired product of formula I either directly or in the case of the nitrile via the amide of formula (IX).
摘要翻译：制备式I的2-（6-（4-（4-氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯嗪-5-基）乙酸的方法，其中6-（4 - 氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯嗪与式Ⅶ的碘衍生物烷基化，其中A为氰基CN或酯基COOR，其中R是（未）支化的C 1 -C 6烷基，在式R1-SO-R2的亚砜存在下使用芬顿试剂，其中R 1是（未）支化的C 1 -C 12烷基，R 2 是（未）支链C 1 -C 12烷基，芳基或取代芳基，或其中R 1，R 2独立地为（C 2）m X（C 2）n，其中X = CH 2，O，S ，NR 3，m = 1-3，n = 1-3，并且R 3是（未）支化的C 1 -C 12烷基，芳基或取代的芳基，所述反应在所用亚砜的环境中进行或在其合适的溶剂中，在0℃至80℃的温度下，优选在10℃的温度范围内将所得到的式IV的酯或式VIII的腈直接或通过式（IX）的酰胺直接或在腈的情况下水解成所需的式I的产物。

2. 发明申请

WO2011124190A3 METHOD OF PRODUCING 4-(2-(SUBSTITUTED)-1-(1-HYDROXYCYCLOHEXYL)ETHYL)PHENOLS BY O- DEMETHYLATION OF THEIR METHYLETHERS BY MEANS OF INODOROUS AROMATIC THIOLS 审中-公开
标题翻译：通过异构芳香硫醇通过其甲基酯的O-甲基化生产4-（2-（取代的）-1-（1-羟基环己基）乙基）苯酚的方法
公开(公告)号：WO2011124190A3
公开(公告)日：2011-12-01
申请号：PCT/CZ2011000032
申请日：2011-04-06
申请人： ZENTIVA K S , RADL STANISLAV , RIDVAN LUDEK , KLECAN ONDREJ , HRUBY PETR
发明人： RADL STANISLAV , RIDVAN LUDEK , KLECAN ONDREJ , HRUBY PETR
IPC分类号： C07C213/00 , C07C215/64
CPC分类号： C07C213/00 , C07C2601/14 , C07C215/64
摘要： A method of producing 4-(2-(substituted)-l-(l-hydroxycyclohexyl)ethyl)phenols of general formula (I), wherein the symbols R1 and R2 are hydrogen (H) or methyl (CH3), by demethylation of their methylethers of general formula (II), wherein symbols R1 and R2 have the same meaning as in formula (I), by heating to 100 to 220 °C with at least one equivalent of an aromatic thiol in the environment of solvents; the reaction is carried out with addition of a base and the aromatic thiol is non- stinking. The term non-stinking means that the stink is only perceptible in concentrations reached in a qualified chemical production in extreme situations only, i.e., for example, above an opened vessel containing the substance; the agent should lack extremely disagreeable "sulphur" character typical of low-molecular compounds containing thiol groups; and even in the above mentioned extreme situations its stink does not exceed intensity of commonly used organic solvents under similar conditions. (Formulae (I), (II)).
摘要翻译：一种制备通式（I）的4-（2-（取代的）-1-（1-羟基环己基）乙基）苯酚的方法，其中符号R1和R2是氢（H）或甲基（CH3），通过脱甲基其通式（II）的甲醚，其中符号R1和R2具有与式（I）中相同的含义，通过在溶剂环境中用至少一当量的芳族硫醇加热至100至220℃; 反应是通过加入碱进行的，而芳族硫醇是非臭的。非臭味这一术语意味着臭气只能在极端情况下，即在例如含有物质的开放容器之上的合格化学品生产中达到的浓度是可察觉的; 该试剂应缺乏含有硫醇基团的低分子化合物典型的极不理想的“硫”特征; 即使在上述极端情况下，在类似条件下，其臭气也不会超过常用有机溶剂的强度。（式（I），（II））。

3. 发明申请

WO2009056077A3 A NEW METHOD OF MANUFACTURING 2-(6-(4-CHLOROPHENYL)-2,2-DIMETHYL-7-PHENYL-2,3-DIHYDRO-LH-PYRROLIZINE-5-YL)ACETIC ACID (LICOFELONE) 审中-公开
标题翻译：制备2-（6-（4-氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-HR-吡咯烷-5-基）乙酸（Lofofelone）的新方法
公开(公告)号：WO2009056077A3
公开(公告)日：2009-06-18
申请号：PCT/CZ2008000116
申请日：2008-09-29
申请人： ZENTIVA AS , RADL STANISLAV , KLECAN ONDREJ
发明人： RADL STANISLAV , KLECAN ONDREJ
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A method of manufacturing 2-(6-(4-chlorophenyl)-2,2-dirnethyl-7-phenyl-2,3-dihydro-lH- pyrrolizine-5-yl)acetic acid of formula I, wherein 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl- 2,3-dihydro-lH-pyrrolizine of formula II is alkylated with a iodo derivative of formula VII, wherein A is either the cyano group CN or an ester group COOR, wherein R is an (un)branched C1-C6 alkyl group, with the use of the Fenton reagent in the presence of a sulfoxide of formula R1-SO-R2, wherein R1 is an (un)branched C1-C12 alkyl group, R2 is either an (un)branched C1-C12 alkyl group, an aryl group or a substituted aryl group, or wherein R1, R2 are independently (C?2)mX(C?2)n, wherein X = CH2, O, S, NR3, m = 1-3, n = 1-3 and R3 is either an (un)branched C1-C12 alkyl group, an aryl group or a substituted aryl group, the reaction being carried out in the environment of the sulfoxide used or in its mixture with suitable solvents at a temperature of O 0C to 80 °C, preferably at temperatures in the range of 10 to 40 °C, and the resulting ester of formula IV or nitrile of formula VIII is hydrolyzed to the desired product of formula I either directly or in the case of the nitrile via the amide of formula (IX).
摘要翻译：式I的2-（6-（4-氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯嗪-5-基）乙酸的制备方法，其中6-（4 - 氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯嗪用式VII的碘代衍生物进行烷基化，其中A是氰基CN或酯基COOR，其中R是（未）支化的C 1 -C 6烷基，使用Fenton试剂在式R 1 -SO-R 2的亚砜存在下进行，其中R 1是（非）支化的C 1 -C 12烷基，R 2 （未）支链C 1 -C 12烷基，芳基或取代芳基，或其中R 1，R 2独立地为（C 2）mX（C 2）n，其中X = CH 2，O，S ，NR 3，m = 1-3，n = 1-3和R 3是（非）支链C 1 -C 12烷基，芳基或取代芳基，反应在所用亚砜的环境中进行或者在其与适合的溶剂的混合物中，在0℃至80℃的温度下，优选在10℃的温度下进行将所得式IV的酯或式VIII的腈直接水解或在腈的情况下经由式（IX）的酰胺水解为所需的式I产物。

4. 发明申请

WO2005021535A2 A METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTING GROUP 审中-公开
标题翻译：一种去除三苯基甲烷保护基团的方法
公开(公告)号：WO2005021535A2
公开(公告)日：2005-03-10
申请号：PCT/CZ2004/000051
申请日：2004-08-26
申请人： ZENTIVA, a.s. , RADL, Stanislav , STACH, Jan , KLECAN, Ondrej
发明人： RADL, Stanislav , STACH, Jan , KLECAN, Ondrej
IPC分类号： C07D403/10
CPC分类号： C07D257/04 , C07D403/10 , Y02P20/55
摘要： A method of removing the triphenylmethane protecting group from 1-triphenylmethyl-5-(4'-subst. methyl-1,1‘-biphenyl-2-yl)-1 H -tetrazoles of general formula I wherein R represents the groups of formulae and where R 1 , R 2 and R 3 can be H, a halogen, an unbranched or branched C1-C5 alkyl, C1-C5 hydroxyalkyl, Cl-C5 alkoxy, C1-C5 alkoxymethyl or benzyl, or wherein R 2 and R 3 can form together a saturated or unsaturated C5-C7 ring, optionally an unsubstituted or substituted aromatic ring, is carried out by solvolysis in a simple anhydrous Cl to C5 alcohol in a neutral or slightly basic medium. The method is suitable for the preparation of drugs, such as the potassium salts of losartan, irbesartan or valsartan or candesartan cilexetil.
摘要翻译：从1-三苯甲基-5-（4'-烯基甲基-1,1'-联苯-2-基）-1H-苯并三唑基甲酸酯中除去三苯基甲烷保护基团的方法，通式I的四唑类，其中R代表下式的基团，并且其中R 1，R 2和R 3可以是H，卤素，直链或支链的C 1 -C 5烷基，C 1 -C 5羟基烷基，C 1 -C 5烷氧基，C 1 -C 5烷氧基甲基或苄基，或者其中R 2和R 3为氢，可以通过在简单的无水C1-C5醇中在中性或微碱性介质中进行溶剂分解而一起形成饱和或不饱和的C5-C7环，任选未取代或取代的芳环。该方法适用于制备药物，如氯沙坦，厄贝沙坦或缬沙坦或坎地沙坦西酯的钾盐。

5. 发明申请

WO2014023270A1 SALTS OR CO-CRYSTALS OF ETHYL N-[2-AMINO-4-[(4-FLUOROPHENYL)METHYLAMINO]-PHENYL]CARBAMATE 审中-公开
标题翻译：乙基N- [2-氨基-4- [[（4-氟苯基）甲基] - 苯基]碳酸酯的钠盐或共晶体
公开(公告)号：WO2014023270A1
公开(公告)日：2014-02-13
申请号：PCT/CZ2012/000077
申请日：2012-08-09
申请人： ZENTIVA, K.S. , RIDVAN, Ludek , KISS, Violetta , KLECAN, Ondrej , TKADLECOVA, Marcela , DAMMER, Ondrej , KREJCIK, Lukas
发明人： RIDVAN, Ludek , KISS, Violetta , KLECAN, Ondrej , TKADLECOVA, Marcela , DAMMER, Ondrej , KREJCIK, Lukas
IPC分类号： C07C271/28 , A61K31/325
CPC分类号： C07C269/08 , C07B2200/13 , C07C271/28
摘要： A salt or co-crystal of ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]- phenyl]carbamate and one acid selected from the group consisting of hydrobromic acid, hydrochloric acid, methanesulphonic acid, benzenesulphonic acid, fumaric acid and salicylic acid.
摘要翻译： N- [2-氨基-4 - [（4-氟苯基）甲基氨基] - 苯基]氨基甲酸乙酯和一种选自氢溴酸，盐酸，甲磺酸，苯磺酸，富马酸和水杨酸。

6. 发明申请

WO2011124190A2 METHOD OF PRODUCING 4-(2-(SUBSTITUTED)-1-(1-HYDROXYCYCLOHEXYL)ETHYL)PHENOLS BY O- DEMETHYLATION OF THEIR METHYLETHERS BY MEANS OF INODOROUS AROMATIC THIOLS 审中-公开
标题翻译：通过甲基醚的非离子型芳香族硫醇的O-甲基化制备4-（2-（取代的）-1-（1-羟基环己基）乙基）苯酚的方法
公开(公告)号：WO2011124190A2
公开(公告)日：2011-10-13
申请号：PCT/CZ2011/000032
申请日：2011-04-06
申请人： ZENTIVA, K.S. , RADL, Stanislav , RIDVAN, Ludek , KLECAN, Ondrej , HRUBY, Petr
发明人： RADL, Stanislav , RIDVAN, Ludek , KLECAN, Ondrej , HRUBY, Petr
IPC分类号： C07C213/00
CPC分类号： C07C213/00 , C07C2601/14 , C07C215/64
摘要： A method of producing 4-(2-(substituted)-l-(l-hydroxycyclohexyl)ethyl)phenols of general formula (I), wherein the symbols R 1 and R 2 are hydrogen (H) or methyl (CH 3 ), by demethylation of their methylethers of general formula (II), wherein symbols R 1 and R 2 have the same meaning as in formula (I), by heating to 100 to 220 °C with at least one equivalent of an aromatic thiol in the environment of solvents; the reaction is carried out with addition of a base and the aromatic thiol is non- stinking. The term non-stinking means that the stink is only perceptible in concentrations reached in a qualified chemical production in extreme situations only, i.e., for example, above an opened vessel containing the substance; the agent should lack extremely disagreeable "sulphur" character typical of low-molecular compounds containing thiol groups; and even in the above mentioned extreme situations its stink does not exceed intensity of commonly used organic solvents under similar conditions. (Formulae (I), (II)).
摘要翻译：制备通式（I）的4-（2-（取代）-1-（1-羟基环己基）乙基）酚的方法，其中符号R 1，和R 2是氢（H）或甲基（CH 3），通过其通式（II）的甲基醚的去甲基化，其中符号R 1， R 2和R 2具有与式（I）中相同的含义，通过在溶剂环境中用至少1当量的芳族硫醇加热至100至220℃; 该反应在加入碱的情况下进行并且芳族硫醇不发臭。术语“不发臭”是指只有在极端情况下合格的化学品生产达到的浓度才可以察觉臭味，例如，在含有该物质的开放容器上方; 试剂应该缺乏极度不愉快的“硫” 性质典型的含有巯基的低分子化合物; 即使在上述极端情况下，其臭味也不会超过类似条件下常用有机溶剂的强度。（式（I），（II））。

7. 发明申请

WO2005021535A3 A METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTING GROUP 审中-公开
标题翻译：一种去除三苯甲基保护基团的方法
公开(公告)号：WO2005021535A3
公开(公告)日：2005-06-09
申请号：PCT/CZ2004000051
申请日：2004-08-26
申请人： ZENTIVA AS , RADL STANISLAV , STACH JAN , KLECAN ONDREJ
发明人： RADL STANISLAV , STACH JAN , KLECAN ONDREJ
IPC分类号： C07D257/04 , C07D403/10
CPC分类号： C07D257/04 , C07D403/10 , Y02P20/55
摘要： A method of removing the triphenylmethane protecting group from 1-triphenylmethyl-5-(4'-subst. methyl-1,1'-biphenyl-2-yl)-1H-tetrazoles of general formula I wherein R represents the groups of formulae and where R , R and R can be H, a halogen, an unbranched or branched C1-C5 alkyl, C1-C5 hydroxyalkyl, Cl-C5 alkoxy, C1-C5 alkoxymethyl or benzyl, or wherein R and R can form together a saturated or unsaturated C5-C7 ring, optionally an unsubstituted or substituted aromatic ring, is carried out by solvolysis in a simple anhydrous Cl to C5 alcohol in a neutral or slightly basic medium. The method is suitable for the preparation of drugs, such as the potassium salts of losartan, irbesartan or valsartan or candesartan cilexetil.
摘要翻译：从通式I的1-三苯基甲基-5-（4'-取代甲基-1,1'-联苯-2-基）-1H-四唑中除去三苯基甲烷保护基的方法，其中R表示式的基团和其中R 1，R 2和R 3可以是H，卤素，无支链或支链C 1 -C 5烷基，C 1 -C 5羟烷基，C 1 -C 5烷氧基，C 1 -C 5烷氧基甲基或苄基，或其中 R 2和R 3可以一起形成饱和或不饱和的C 5 -C 7环，任选未取代或取代的芳环，通过在中性或微碱性介质中的简单的无水C1至C5醇中溶剂解来进行。该方法适用于制备药物，如氯沙坦，厄贝沙坦或缬沙坦或坎地沙坦酯的钾盐。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式