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1. 发明申请

US20110118460A1 PROCESS FOR THE SYNTHESIS OF QUETIAPINE 有权
标题翻译： QUETIAPINE合成方法
公开(公告)号：US20110118460A1
公开(公告)日：2011-05-19
申请号：US13001713
申请日：2009-01-30
申请人： Siro Serafini , Filippo Tomasi , Marco Galvagni
发明人： Siro Serafini , Filippo Tomasi , Marco Galvagni
IPC分类号： C07D417/04
CPC分类号： C07D281/14
摘要： The present invention relates to a process for the synthesis of quetiapine. In particular, a process is provided for the synthesis of quetiapine of formula (A) comprising reacting dibenzo[b,f][1,4]thiazepin-11(10H)-one, intermediate (I) with phosphorous oxychloride to give 11-chlorodibenzo[b,f][1,4]thiazepine, intermediate (II) wherein the said reaction of intermediate (I) to intermediate (II) is performed in an organic solvent in the presence of a mixture of an organic base together with an inorganic base.
摘要翻译：本发明涉及喹硫平的合成方法。特别地，提供了用于合成式（A）的喹硫平的方法，包括使二苯并[b，f] [1,4]硫杂吖庚因-11（10H） - 酮，中间体（I）与氯氧化磷反应，得到11- 氯二苯并[b，f] [1,4]硫氮杂，中间体（II），其中中间体（I）与中间体（II）的所述反应在有机溶剂中，在有机碱与无机碱。

2. 发明申请

US20110166364A1 SYNTHESIS OF 3--5-[2-(PHENYLSULFONYL)ETHYL]-1H-INDOLE 有权
标题翻译： 3- [2-（苯基磺酰基）乙基] -1H-吲哚的合成
公开(公告)号：US20110166364A1
公开(公告)日：2011-07-07
申请号：US12995390
申请日：2009-11-09
申请人： Siro Serafini , Andrea Castellin , Claudio Dal Santo
发明人： Siro Serafini , Andrea Castellin , Claudio Dal Santo
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.
摘要翻译：本发明涉及合成名为Eletriptan的3 - {[（2R）-1-甲基吡咯烷-2-基]甲基} -5- [2-（苯基磺酰基）乙基] -1H-吲哚，或其盐。特别地，本发明涉及一种合成埃曲普坦或其盐的方法，包括以下步骤：a）使用二羧酸使式（6）的中间体盐化得到衍生的盐; b）任选地，通过溶剂结晶纯化根据步骤a）获得的所述生盐，得到式（6）中间体的纯化盐; c）根据步骤a）将所述式（6）的中间体的盐或根据步骤b）的所述纯化盐转化成式（10）的中间体; d）将式（10）的中间体转化成Eletriptan或其盐。

3. 发明申请

US20090312557A1 PROCESS FOR THE PREPARATION OF EPSILON -ALKOXYCARBONYLLYSINES AND THEIR ANALOGUES 有权
标题翻译：制备EPSILON -ALKOXYCARBONYLLYSINES及其类似物的方法
公开(公告)号：US20090312557A1
公开(公告)日：2009-12-17
申请号：US12307687
申请日：2006-08-04
申请人： Siro Serafini , Riccardo Motterle , Elena Brasola
发明人： Siro Serafini , Riccardo Motterle , Elena Brasola
IPC分类号： C07D249/18 , C07C53/126 , C07C55/02
CPC分类号： C07C269/04 , C07D249/18 , C07C271/22
摘要： A process for the preparation of ω-alkoxycarbonylamino-α-aminoacids and α,ω orthogonally diprotected diaminoacids from α,ω-diaminoacids using 1-alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of ε-alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of ω-alkoxycarbonylamino-α-aminoacids with benzotriazoles are also disclosed.
摘要翻译：公开了使用1-烷氧基羰基苯并三唑作为保护剂从ω，ω-二氨基酸制备ω-烷氧基羰基氨基-α-氨基酸和α，ω正交二保护二氨基酸的方法。在替代实施方案中，使用在苯并三唑存在下的氨基甲酰化剂代替1-烷氧基羰基苯并三唑。该反应优选用于从赖氨酸制备ε-烷氧基羰基赖氨酸。还公开了制备叔丁氧基羰基苯并三唑的方法和ω-烷氧基羰基氨基-α-氨基酸与苯并三唑的新配合物。

4. 发明授权

US06632942B2 Asymmetric synthesis of piperazic acid and derivatives thereof 失效
标题翻译：哌嗪酸及其衍生物的不对称合成
公开(公告)号：US06632942B2
公开(公告)日：2003-10-14
申请号：US10168463
申请日：2002-06-14
申请人： Andrea L. C. Robidoux , Siro Serafini , Petra Dieterich , Stefania Leonardi , John Stibbard
发明人： Andrea L. C. Robidoux , Siro Serafini , Petra Dieterich , Stefania Leonardi , John Stibbard
IPC分类号： C07D23704
CPC分类号： C07D487/04 , C07D237/04
摘要： This invention provides a concise, asymmetric synthesis of piperazic acid and derivatives thereof, whereby either the (3S)- or (3R)-enantiomeric form may be obtained with high optical purity. (3S)-piperazic acid is derived from D-glutamic acid through an (R)-2,5-dihydroxyvalerate ester intermediate. After the hydroxy groups are converted to suitable leaving groups, such as mesylates, the ester is treated with a bis-protected hydrazine to provide the desired (3S)-piperazic acid derivative. The (3R) enantiomer of piperazic acid may be similarly obtained starting with L-glutamic acid. The method may also be used to obtain piperazic acid derivatives that have moderate optical purity or are racemic. By this method, piperazic acid derivatives may be obtained that are useful as intermediates for pharmacologically active compounds. For example, certain intermediates of this invention are useful for preparing caspase inhibitors, particularly inhibitors of ICE, through additional steps known in the art.
摘要翻译：本发明提供哌嗪酸及其衍生物的简明，不对称合成，由此可以以高光学纯度获得（3S） - 或（3R） - 对映体形式。（3S） - 哌嗪酸通过（R）-2,5-二羟基戊酸酯中间体衍生自D-谷氨酸。将羟基转化为合适的离去基团（如甲磺酸酯）后，用双 - 保护的肼处理酯，得到所需的（3S） - 哌嗪酸衍生物。哌嗪酸的（3R）对映异构体可以从L-谷氨酸开始类似地获得。该方法也可用于获得具有中等光学纯度或外消旋的哌嗪酸衍生物。通过该方法，可以得到可用作药理活性化合物的中间体的哌嗪酸衍生物。例如，通过本领域已知的附加步骤，本发明的某些中间体可用于制备胱天蛋白酶抑制剂，特别是ICE的抑制剂。

5. 发明授权

US08389716B2 Process for the synthesis of quetiapine 有权
标题翻译：喹硫平的合成方法
公开(公告)号：US08389716B2
公开(公告)日：2013-03-05
申请号：US13001713
申请日：2009-01-30
申请人： Siro Serafini , Filippo Tomasi , Marco Galvagni
发明人： Siro Serafini , Filippo Tomasi , Marco Galvagni
IPC分类号： C07D281/14
CPC分类号： C07D281/14
摘要： The present invention relates to a process for the synthesis of quetiapine. In particular, a process is provided for the synthesis of quetiapine of formula (A) comprising reacting dibenzo[b,f][1,4]thiazepin-11(10H)-one, intermediate (I) with phosphorous oxychloride to give 11-chlorodibenzo[b,f][1,4]thiazepine, intermediate (II) wherein the said reaction of intermediate (I) to intermediate (II) is performed in an organic solvent in the presence of a mixture of an organic base together with an inorganic base.
摘要翻译：本发明涉及喹硫平的合成方法。特别地，提供了用于合成式（A）的喹硫平的方法，包括使二苯并[b，f] [1,4]硫杂吖庚因-11（10H） - 酮，中间体（I）与氯氧化磷反应，得到11- 氯二苯并[b，f] [1,4]硫氮杂，中间体（II），其中中间体（I）与中间体（II）的所述反应在有机溶剂中，在有机碱与无机碱。

6. 发明授权

US4900859A Process for 4-dimethylamino-3,5-dimethoxybenzaldehyde 失效
标题翻译： 4-二甲基氨基-3,5-二甲氧基苯甲醛的方法
公开(公告)号：US4900859A
公开(公告)日：1990-02-13
申请号：US272366
申请日：1988-11-17
申请人： Siro Serafini , Giuseppe Zagotto
发明人： Siro Serafini , Giuseppe Zagotto
IPC分类号： B01J25/02 , B01J27/122 , C07B61/00 , C07C221/00 , C07C223/06 , C07C253/30 , C07C255/58 , C07C255/59
CPC分类号： C07C255/58 , C07C221/00 , C07C255/59
摘要： 4-Dimethylamino-3,5-dimethoxy-benzaldehyde, an intermediate for the preparation of the antibacterially active aditoprim (4-dimethylamino-3,5-dimethoxybenzoldehyde) a known antibacterially active compound, is obtained from 4-dimethylaminobenzonitrile by bromination or chlorination, replacement of the halogen by the methoxy group and reduction of the nitrile group.
摘要翻译：通过溴化或氯化从4-二甲基氨基苄腈得到4-二甲基氨基-3,5-二甲氧基 - 苯甲醛，其是制备已知抗菌活性化合物的抗菌活性阿维生丁（4-二甲氨基-3,5-二甲氧基苯甲醇）的中间体，用甲氧基代替卤素并还原腈基。

7. 发明授权

US08426612B2 Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole 有权
标题翻译： 3 - {[（2R）-1-甲基吡咯烷-2-基]甲基} -5 [2-（苯基磺酰基）乙基] -1H-吲哚
公开(公告)号：US08426612B2
公开(公告)日：2013-04-23
申请号：US12995390
申请日：2009-11-09
申请人： Siro Serafini , Andrea Castellin , Claudio Dal Santo
发明人： Siro Serafini , Andrea Castellin , Claudio Dal Santo
IPC分类号： C07D209/04
CPC分类号： C07D403/06
摘要： The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.
摘要翻译：本发明涉及合成名为Eletriptan的3 - {[（2R）-1-甲基吡咯烷-2-基]甲基} -5- [2-（苯基磺酰基）乙基] -1H-吲哚，或其盐。特别地，本发明涉及一种合成埃曲普坦或其盐的方法，包括以下步骤：a）使用二羧酸使式（6）的中间体盐化得到衍生的盐; b）任选地，通过溶剂结晶纯化根据步骤a）获得的所述生盐，得到式（6）中间体的纯化盐; c）根据步骤a）将所述式（6）的中间体的盐或根据步骤b）的所述纯化盐转化成式（10）的中间体; d）将式（10）的中间体转化成Eletriptan或其盐。

8. 发明授权

US08026372B2 Process for the preparation of ε-alkoxycarbonyllysines and their analogues 有权
标题翻译： - 烷氧基羰基赖氨酸及其类似物的制备方法
公开(公告)号：US08026372B2
公开(公告)日：2011-09-27
申请号：US12307687
申请日：2006-08-04
申请人： Siro Serafini , Riccardo Motterle , Elena Brasola
发明人： Siro Serafini , Riccardo Motterle , Elena Brasola
IPC分类号： C07D249/00
CPC分类号： C07C269/04 , C07D249/18 , C07C271/22
摘要： A process for the preparation of ω-alkoxycarbonylamino-α-aminoacids and α,ω orthogonally diprotected diaminoacids from α,ω-diaminoacids using 1-alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of ε-alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of ω-alkoxycarbonylamino-α-aminoacids with benzotriazoles are also disclosed.
摘要翻译：公开了使用1-烷氧基羰基苯并三唑作为保护剂从ω，ω-二氨基酸制备ω-烷氧基羰基氨基-α-氨基酸和α，ω正交二保护二氨基酸的方法。在替代实施方案中，使用在苯并三唑存在下的氨基甲酰化剂代替1-烷氧基羰基苯并三唑。该反应优选用于从赖氨酸制备的α-烷氧基羰基赖氨酸。还公开了制备叔丁氧基羰基苯并三唑的方法和ω-烷氧基羰基氨基-α-氨基酸与苯并三唑的新型络合物。

9. 发明授权

US5710321A Process for preparing the cyclohexylamine salt of (+) - threo-2-hydroxy-3-(2'-aminophenylthio) -3-(4"-methoxyphenyl) -propionic acid and of its (-) -antipode" 失效
标题翻译：制备（+） - 苏氨基-2-羟基-3-（2'-氨基苯硫基）-3-（4“ - 甲氧基苯基） - 丙酸及其（ - ） -
公开(公告)号：US5710321A
公开(公告)日：1998-01-20
申请号：US632077
申请日：1996-04-15
申请人： Roberto Bortolaso , Siro Serafini
发明人： Roberto Bortolaso , Siro Serafini
IPC分类号： C07B57/00 , C07C211/35 , C07C319/28 , C07C323/56 , C07C55/00
CPC分类号： C07B57/00 , C07C211/35 , C07C319/28 , C07B2200/07 , C07C2101/14
摘要： The present invention relates to a process for preparing the cyclohexylamine salt of (+)-threo-2-hydroxy-3-(2'-aminophenylthio)-3-(4"-methoxyphenyl)-propionic acid and of its optical (-)-antipode, by starting from the racemate acid by means of a first crystallization from a suitable chiral base and a second crystallization from a cyclohexylamine-containing solvent. Said salt is an intermediate in the synthesis of diltiazem, a well-known calcium-antagonist drug.
摘要翻译：本发明涉及（+） - 苏氨基-2-羟基-3-（2'-氨基苯硫基）-3-（4“ - 甲氧基苯基） - 丙酸的环己胺盐及其光学（ - ） - - 通过从合适的手性碱进行的第一次结晶和来自含环己胺的溶剂的第二次结晶从外消旋酸开始。所述盐是合成地尔硫卓（一种众所周知的钙拮抗剂药物）的中间体。

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