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1. 发明授权

US4701540A Process for carotenoid intermediates 失效
标题翻译：类胡萝卜素中间体的方法
公开(公告)号：US4701540A
公开(公告)日：1987-10-20
申请号：US588268
申请日：1984-03-12
申请人： Teodor Lukac , Milan Soukup , Erich Widmer
发明人： Teodor Lukac , Milan Soukup , Erich Widmer
IPC分类号： C07C47/20 , C07C27/00 , C07C29/00 , C07C29/09 , C07C33/12 , C07C35/02 , C07C35/06 , C07C45/00 , C07C45/42 , C07C45/71 , C07C49/587 , C07C67/00 , C07C401/00 , C07C403/00 , C07C403/08 , C07C403/10 , C07C403/14 , C07D317/72 , C07D317/20 , C07C37/00 , C07C43/184
CPC分类号： C07D317/72 , C07C403/08 , C07C403/14 , C07C45/71 , C07C2101/14 , C07C2101/16
摘要： A process for producing cycloketones of a 5 or 6 carbon chain length through which said ketones are known intermediates for producing carotenoids.
摘要翻译：一种制备5或6个碳链长度的环酮的方法，通过该方法所述酮是用于生产类胡萝卜素的已知中间体。

2. 发明授权

US4532358A Process for the manufacture of 3-hydroxy-2,6,6,-trimethyl-2 cyclohexen-1-one 失效
标题翻译： 3-羟基-2,6,6 - 三甲基-2环己烯-1-酮的制备方法
公开(公告)号：US4532358A
公开(公告)日：1985-07-30
申请号：US639544
申请日：1984-08-10
申请人： Teodor Lukac , Milan Soukup , Erich Widmer
发明人： Teodor Lukac , Milan Soukup , Erich Widmer
IPC分类号： C07C45/67 , B01J31/22 , B01J31/24 , C07B61/00 , C07C45/00 , C07C45/64 , C07C49/713 , C07C67/00 , C07C45/68
CPC分类号： C07C45/64
摘要： A process for the manufacture of 3-hydroxy-2,6,6,-trimethyl-2-cyclohexen-2-one, an intermediate in canthaxanthin synthesis, by isomerizing 1,1,3-trimethyl-7-oxabicyclo[4.1.0]heptan-2-one in the presence of a palladium(O) complex of an acetone derivative of the formula ##STR1## wherein R.sup.1 and R.sup.2 are aryl and R.sup.3 and R.sup.4 are hydrogen or monovalent hydrocarbon groups optionally carrying a carbonyl function, a bis-(diphenylphosphino) derivative of the formula(R.sup.5).sub.2 P--R.sup.6 --P(R.sup.5).sub.2wherein R.sup.5 is phenyl or tolyl and R.sup.6 is a C.sub.2 --C.sub.4 -alkylene group optionally substituted with one or more inert organic groups, and a triarylphosphine of the formulaP(R.sup.7).sub.3wherein R.sup.7 is an optionally alkyl-substituted phenyl group.
摘要翻译：通过使1,1,3-三甲基-7-氧杂双环[4.1.0]异构化制备3-羟基-2,6,6 - 三甲基-2-环己烯-2-酮，角黄素合成中间体的方法 ]庚-2-酮在式（III）的丙酮衍生物的钯（O）配合物存在下，其中R 1和R 2是芳基，R 3和R 4是氢或任选带有羰基官能团的一价烃基，式（R5）2P-R6-P（R5）2的双 - （二苯基膦基）衍生物其中R5是苯基或甲苯基，R6是任选被一个或多个惰性有机基团取代的C 2 -C 4亚烷基，和三芳基膦的式（R 7）3，其中R 7是任选的烷基取代的苯基。

3. 发明授权

US4661641A Substituted alkynes useful as intermediates in the synthesis of carotenoids 失效
标题翻译：用作合成类胡萝卜素的中间体的取代炔烃
公开(公告)号：US4661641A
公开(公告)日：1987-04-28
申请号：US614607
申请日：1984-05-29
申请人： Teodor Lukac , Milan Soukup , Erich Widmer
发明人： Teodor Lukac , Milan Soukup , Erich Widmer
IPC分类号： B01J31/02 , C07B61/00 , C07C29/60 , C07C31/135 , C07C33/14 , C07C35/18 , C07C403/00 , C07C31/20 , C07C53/134
CPC分类号： C07C403/10 , C07C29/60 , C07C33/14 , C07C35/18 , C07C403/08 , C07C403/14 , C07C403/16 , C12C11/02 , C07B2200/07 , C07C2101/14 , C07C2101/16 , Y02P20/55
摘要： Compounds of the formula ##STR1## wherein n is either 0 or 1; R.sup.1 and R.sup.2 is hydrogen and the other is hydrogen, hydroxy, oxo group, a protected hydroxy or protected oxo group; R.sup.3 is hydroxy oxo group, .dbd.CH--CH.sub.2 --OH, .dbd.CH--CHO or one of the foregoing groups where the hydroxy or oxo functions are protected; R.sup.4 is --CO--OR.sup.6, --CO--R.sup.6, --CO--NR.sup.6 R.sup.7, --CO--Cl or --SO.sub.2 --R.sup.6 ; R.sup.6 is saturated or aromatic hydrocarbon; and R.sup.7 is saturated or aromatic hydrocarbon or hydrogen,are converted by cleavage of R.sup.4 OH into corresponding cycloalkenes and protecting groups, if present, are hydrolyzed.The compounds obtained are valuable intermediates in carotenoid syntheses.
摘要翻译：式（Ⅰ）化合物其中n为0或1; R 1和R 2是氢，另一个是氢，羟基，氧代基，保护的羟基或被保护的氧代基; R3是羟基氧代基，= CH-CH2-OH，= CH-CHO或其中羟基或氧代官能团被保护的前述基团之一; R4是-CO-OR6，-CO-R6，-CO-NR6R7，-CO-C1或-SO2-R6; R6是饱和或芳烃; 并且R 7是饱和或芳族烃或氢，通过R 4 OH的裂解转化成相应的环烯烃，如果存在的话，保护基团被水解。所得化合物是类胡萝卜素合成中的有价值的中间体。

4. 发明授权

US5227507A Ethynylcyclohexene compounds and processes for manufacture thereof 失效
标题翻译：乙炔基环己烯化合物及其制备方法
公开(公告)号：US5227507A
公开(公告)日：1993-07-13
申请号：US498061
申请日：1990-03-23
申请人： Teodor Lukac , Milan Soukup
发明人： Teodor Lukac , Milan Soukup
IPC分类号： C07C35/17 , C07F7/08 , C07F9/54
CPC分类号： C07C403/24 , C07C35/17 , C07C403/08 , C07F9/5435 , C07B2200/07 , C07C2101/16
摘要： A process for the manufacture of compounds of the general formula ##STR1## wherein R.sup.1 signifies hydroxy or an etherified hydroxy group, and of zeaxanthin by converting a compound of the general formula ##STR2## wherein R.sup.1 has the above significance, in an inert organic solvent into the acetylenide and reacting this with methyl vinyl ketone, reducing the alcoholate obtained or the alcohol (obtained after hydrolysis of the alcoholate) of the general formula ##STR3## wherein R.sup.1 has the above significance, in an inert organic solvent with an aluminum hydride of the general formulaR.sub.x MAlH.sub.4-x IIIwherein M signifies alkali metal, R represents C.sub.1 -C.sub.10 -alkoxy or a group of the formula C.sub.n H.sub.2n+1 --O--C.sub.m H.sub.2m --O--, m and n each individually denote whole numbers of 1 to 7 and x stands for 0, 1, 2 or 3,and subsequently hydrolyzing to give the compound of formula IV and, if desired, converting the compound of formula IV obtained into zeaxanthin.
摘要翻译：制备其中R1表示羟基或醚化的羟基的化合物和玉米黄质的方法，其通过将惰性化合物转化成其中R 1具有上述含义的通式为I的化合物将有机溶剂倒入乙炔基中，并将其与甲基乙烯基酮反应，将所得的醇化物或醇（通过醇化物水解后得到）通式为其中R 1具有上述含义，在惰性有机溶剂中与通式为RxMAlH4-xIII的氢化铝，其中M表示碱金属，R表示C1-C10-烷氧基或式CnH2n + 1-O-CmH2m-O-基团，m和n各自表示1〜 7和x代表0,1,2或3，随后水解得到式Ⅳ化合物，如果需要，将得到的式Ⅳ化合物转化成玉米黄质。

5. 发明授权

US4952716A Ethynylcyclohexene compounds 失效
标题翻译：乙炔基环己烯化合物
公开(公告)号：US4952716A
公开(公告)日：1990-08-28
申请号：US164304
申请日：1988-03-04
申请人： Teodor Lukac , Milan Soukup
发明人： Teodor Lukac , Milan Soukup
IPC分类号： C07C43/188 , C07C27/00 , C07C35/17 , C07C35/18 , C07C35/46 , C07C41/00 , C07C43/18 , C07C43/196 , C07C43/303 , C07C67/00 , C07C401/00 , C07C403/00 , C07C403/02 , C07C403/08 , C07C403/10 , C07C403/24 , C07D309/06 , C07F7/18 , C07F9/54
CPC分类号： C07C403/24 , C07C35/17 , C07C403/08 , C07F9/5435 , C07C2101/16
摘要： A process for the manufacture of compounds of the general formula ##STR1## wherein R.sup.1 signifies hydroxy or an etherified hydroxy group, and of zeaxanthin by converting a compound of the general formula ##STR2## wherein R.sup.1 has the above significance, in an inert organic solvent into the acetylenide and reacting this with methyl vinyl ketone, reducing the alcoholate obtained or the alcohol (obtained after hydrolysis of the alcoholate) of the general formula ##STR3## wherein R.sup.1 has the above significance, and subsequently hydrolyzing to give the compound of formula IV and, if desired, converting the compound of formula IV obtained into zeaxanthin.
摘要翻译：制备其中R1表示羟基或醚化的羟基的化合物和玉米黄质的方法，其通过将惰性化合物转化成其中R 1具有上述含义的通式为I的化合物将有机溶剂倒入乙炔基中并与甲基乙烯基酮反应，还原得到的醇化物或醇（水解后得到的醇化物），其中R1具有上述含义，随后水解得到化合物并且如果需要，将获得的式IV化合物转化成玉米黄质。

6. 发明授权

US08703976B2 Manufacturing process for 8-aryloctanoic acids such as Aliskiren 失效
标题翻译： 8-阿糖辛酸如阿利吉仑的制备方法
公开(公告)号：US08703976B2
公开(公告)日：2014-04-22
申请号：US13337071
申请日：2011-12-24
申请人： Milan Soukup
发明人： Milan Soukup
IPC分类号： C07D307/00
CPC分类号： C07D307/33
摘要： The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compound such as Aliskiren.The invention describes preparation of enantiomerically pure 8-aryloctanoic acid of formula I from a chiral compound of formula IV. Friedel-Crafts reaction of this compound of formula IV with a compound of formula III provides compound of formula II which is converted reductively in a few steps into the compound of formula V, a know intermediate in the synthesis of compound of formula I. According to the disclosed process, Aliskiren can be now prepared from commercial starting materials (Guajacol or 2-bromoanisole, cis- or trans-1,4-dichloro-2-butene and 4(S)-benzyl-3-isovaleroyl-oxazolidin-2-one) in less than 8 process steps.
摘要翻译：本发明涉及可用于合成药物活性化合物如阿利吉仑的新型制备方法和新型中间体。本发明描述了由式IV的手性化合物制备式I的对映体纯的8-芳酸辛酸。该式IV化合物与式III化合物的Friedel-Crafts反应提供式II化合物，其在几步中还原转化成式V化合物，其是式I化合物合成中的已知中间体。根据所公开的方法，阿利吉仑现在可以由商业原料（Guajacol或2-溴苯甲醚，顺式或反式-1,4-二氯-2-丁烯和4（S） - 苄基-3-异戊酰基 - 恶唑烷-2-酮一个）在不到8个过程步骤。

7. 发明授权

US08680297B2 Manufacturing process for tiotropium bromide 失效
标题翻译：噻托溴铵的制造工艺
公开(公告)号：US08680297B2
公开(公告)日：2014-03-25
申请号：US13200975
申请日：2011-10-06
申请人： Milan Soukup
发明人： Milan Soukup
IPC分类号： C07D409/14
CPC分类号： C07D409/14 , C07D491/08
摘要： The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as a long-acting anticholinergic bronchodilator. Starting from oxalic acid derivative of formula III the invention describes preparation of a novel cyclic anhydride of formula II which is very efficient precursor in the synthesis of Tiotropium bromide (compound of formula I).
摘要翻译：本发明涉及用作长效抗胆碱能支气管扩张剂的式I的药学活性化合物的新型制造方法。从式III的草酸衍生物开始，本发明描述了制备式II的新型环状酸酐，其在合成噻托溴铵（式I化合物）中是非常有效的前体。

8. 发明授权

US07115643B2 Intermediate halophenyl derivatives and their use in a process for preparing azole derivatives 有权
标题翻译：中间卤代苯基衍生物及其在制备唑衍生物的方法中的用途
公开(公告)号：US07115643B2
公开(公告)日：2006-10-03
申请号：US10481654
申请日：2002-06-17
申请人： Milan Soukup
发明人： Milan Soukup
IPC分类号： A61K31/41 , C07D249/08
CPC分类号： C07D231/12 , C07C33/483 , C07D233/56 , C07D249/08
摘要： Novel halophenyl derivatives of the general formula (I), wherein R1 is halogen, a leaving group or 1H-1,2,4-triazol-1-yl and R2 is ethynyl or carboxy, X1 is halogen and X2 and X3 are each independently hydrogen or halogen, and their manufacture are described. They are intermediates for manufacturing azole derivatives of the general formula (V) which are valuable medicaments useful for treating systemic mycoses.
摘要翻译：通式（I）的新型卤代苯基衍生物，其中R 1是卤素，离去基团或1H-1,2,4-三唑-1-基和R 2 O >是乙炔基或羧基，X 1是卤素，X 2和X 3各自独立地是氢或卤素，并且描述了它们的制造。它们是制备通式（Ⅴ）的唑类衍生物的中间体，它们是可用于治疗全身性真菌病的有价值的药物。

9. 发明授权

US07064199B2 Process for the manufacture of 3-amino-pyrrolidine derivatives 失效
标题翻译： 3-氨基 - 吡咯烷衍生物的制备方法
公开(公告)号：US07064199B2
公开(公告)日：2006-06-20
申请号：US10743365
申请日：2003-12-22
申请人： Marc Muller , Milan Soukup
发明人： Marc Muller , Milan Soukup
IPC分类号： C07D501/24
CPC分类号： C07D207/14 , Y02P20/55
摘要： The invention is concerned with a process for the manufacture of vinylpyrrolidinone-cephalosporin derivatives from 3-amino-pyrrolidine derivatives of the formula wherein R1 signifies hydrogen or an amino protecting group; Z signifies hydrogen or an amino protecting group; and * represents a center of chirality.
摘要翻译：本发明涉及由下式的3-氨基 - 吡咯烷衍生物制备乙烯基吡咯烷酮 - 头孢菌素衍生物的方法：其中R 1表示氢或氨基保护基; Z表示氢或氨基保护基; *表示手性中心。

10. 发明授权

US08445708B2 Process for preparing chiral octenoic acid derivatives 失效
标题翻译：制备手性辛烯酸衍生物的方法
公开(公告)号：US08445708B2
公开(公告)日：2013-05-21
申请号：US12091795
申请日：2006-10-27
申请人： Milan Soukup , Karl Reuter , Florian Stolz , Viktor Meier , Jofzsef Balint , Mark Kantor
发明人： Milan Soukup , Karl Reuter , Florian Stolz , Viktor Meier , Jofzsef Balint , Mark Kantor
IPC分类号： C07C59/147 , C07C59/00 , C07C231/00
CPC分类号： C07C235/34 , C07B2200/07 , C07C51/377 , C07C57/13 , C07C57/66 , C07C59/64 , C07C59/90
摘要： The invention relates to a process for preparing chiral octenoic acid derivatives, which constitute important intermediates in the preparation of medicament active ingredients, and also to novel intermediates which are used in the process for preparing the octenoic acid derivatives mentioned.
摘要翻译：本发明涉及一种制备手性辛烯酸衍生物的方法，其在制备药物活性成分中构成重要的中间体，还涉及用于制备所述辛烯酸衍生物的方法中的新型中间体。

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