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1. 发明申请

US20120277443A1 PROCESS FOR THE PURIFICATION OF RUFINAMIDE 有权
标题翻译：净化呋喃胺的方法
公开(公告)号：US20120277443A1
公开(公告)日：2012-11-01
申请号：US13451651
申请日：2012-04-20
申请人： Pietro ALLEGRINI , Dario PASTORELLO , Gabriele RAZZETTI
发明人： Pietro ALLEGRINI , Dario PASTORELLO , Gabriele RAZZETTI
IPC分类号： C07D249/04
CPC分类号： C07D249/04
摘要： A process for purifying Rufinamide, comprising:a) providing a dispersion of crude 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxamide in a solvent mixture containing at least a carboxylic acid, and dissolving it;b) slowly cooling the solution to precipitate Rufinamide crystalline form A; andc) recovering the solid.
摘要翻译：一种用于纯化Rufinamide的方法，包括：a）提供粗制的1 - [（2,6-二氟苯基）甲基] -1H-1,2,3-三唑-4-甲酰胺在含有至少一种羧酸酸，并溶解; b）缓慢冷却溶液以沉淀Ruformamide结晶形式A; 和c）回收固体。

2. 发明授权

US08193386B2 Crystalline form of (S)-1-phenylethylammonium (R)-diphenylmethanesulphinyl-acetate 失效
标题翻译：（S）-1-苯基乙基铵（R） - 二苯基甲酰亚氨基乙酸酯的结晶形式
公开(公告)号：US08193386B2
公开(公告)日：2012-06-05
申请号：US12264502
申请日：2008-11-04
申请人： Giuseppe Barreca , Pietro Allegrini , Gabriele Razzetti
发明人： Giuseppe Barreca , Pietro Allegrini , Gabriele Razzetti
IPC分类号： C07C323/00 , C07C231/00
CPC分类号： C07C317/44 , C07C315/04
摘要： Novel crystalline hydrate form of (S)-1-phenylethylammonium (R)-diphenyl-methanesulphinyl-acetate and its use in a process for the preparation of (R)-benzhydrylsulphinylacetamide.
摘要翻译：（S）-1-苯基乙基铵（R） - 二苯基 - 甲基亚磺酰基 - 乙酸酯的新型结晶水合物形式及其在制备（R） - 二苯甲基亚磺酰基乙酰胺的方法中的用途。

3. 发明授权

US07790891B2 Process for the preparation of pyridine-methylsulfinyl compounds 失效
标题翻译：吡啶 - 甲基亚磺酰基化合物的制备方法
公开(公告)号：US07790891B2
公开(公告)日：2010-09-07
申请号：US11927009
申请日：2007-10-29
申请人： Pietro Allegrini , Marcello Rasparini , Gabriele Razzetti , Simone Mantegazza , Vittorio Lucchini , Alberto Bologna
发明人： Pietro Allegrini , Marcello Rasparini , Gabriele Razzetti , Simone Mantegazza , Vittorio Lucchini , Alberto Bologna
IPC分类号： C07D471/02 , C07D401/12
CPC分类号： C07D401/12 , C07D471/04
摘要： A process for the preparation of a compound of formula (I), or a salt thereof, wherein Q is ═CR8— or ═N—; and R1-R8 are as herein defined; comprising the reaction of a compound of formula (II), or a salt thereof, wherein Q, R1-R7 are as herein defined; with a reducing agent selected from a trivalent phosphorous compound, an oxidizable solvent and a sulfonic acid chloride; and, if desired, the conversion of a compound of formula (I) to another compound of formula (I) or a salt thereof.
摘要翻译：一种制备式（I）化合物或其盐的方法，其中Q为= CR8-或= N-; 和R 1 -R 8如本文所定义; 包括式（II）化合物或其盐的反应，其中Q，R 1 -R 7如本文所定义; 与选自三价磷化合物，可氧化溶剂和磺酰氯的还原剂反应; 如果需要，式（I）化合物转化为另一种式（I）化合物或其盐。

4. 发明授权

US07750177B2 Process for the preparation of entacapone 失效
标题翻译：恩他卡朋的制备方法
公开(公告)号：US07750177B2
公开(公告)日：2010-07-06
申请号：US11958778
申请日：2007-12-18
申请人： Simone Mantegazza , Pietro Allegrini , Gabriele Razzetti
发明人： Simone Mantegazza , Pietro Allegrini , Gabriele Razzetti
IPC分类号： C07C255/23
CPC分类号： C07C253/30 , C07C255/41
摘要： A process for the preparation of entacapone, in particular as the polymorphic form A, comprising the preparation of a compound of formula (V), wherein R is C1-C6 alkyl, by condensation of N,N-diethyl-cyano-acetamide with a compound of formula (IV), wherein R is C1-C6 alkyl, in the presence of a strong basic agent; the dealkylation of the compound of formula (V) to obtain entacapone, and the crystallization thereof from methyl ethyl ketone is performed to yield the polymorphic form A. The polymorphic form A of entacapone may be used to treat Parkinson's disease and/or to enhance effectiveness of muscle control.
摘要翻译：恩替卡宾的制备方法，特别是多晶型A，其包括通过N，N-二乙基 - 氰基 - 乙酰胺与一种或多种式I化合物的缩合制备其中R为C1-C6烷基的式（Ⅴ）化合物式（Ⅳ）化合物，其中R为C1-C6烷基，在强碱性试剂存在下; 进行式（V）化合物的脱烷基化以获得恩他卡朋，并从甲基乙基酮中进行结晶，得到多晶型A.恩他卡朋的多晶型A可用于治疗帕金森病和/或增强有效性的肌肉控制。

5. 发明申请

US20090286996A1 PROCESS FOR THE PREPARATION OF ZILEUTON 审中-公开
标题翻译：制备ZILEUTON的方法
公开(公告)号：US20090286996A1
公开(公告)日：2009-11-19
申请号：US12423122
申请日：2009-04-14
申请人： Emanuele ATTOLINA , Gianmaria Dell'Anna , Roberto Rossi , Pietro Allegrini , Gabriele Razzetti
发明人： Emanuele ATTOLINA , Gianmaria Dell'Anna , Roberto Rossi , Pietro Allegrini , Gabriele Razzetti
IPC分类号： C07D333/58 , C07D333/60 , C07F7/10
CPC分类号： C07D333/56 , C07D333/58 , C07F7/1804 , Y02P20/55
摘要： Process for preparing a compound of formula (I), or a salt thereof, comprising reacting of a compound of formula (II) wherein X and R are as herein defined; with a compound of formula (III) NH2OZ (III) wherein Z is a hydroxy protecting group, in presence of a catalyst, to obtain a compound of formula (IV), or a salt thereof, removing the hydroxyl protecting group to obtain a compound of formula (V), or a salt thereof; converting a compound of formula (V), or a salt thereof, into a compound of formula (I), or a salt thereof; and, if desired, converting a compound of formula (I) into a salt thereof, or vice versa.
摘要翻译：制备式（I）化合物或其盐的方法，包括其中X和R如本文所定义的式（II）化合物的反应; 与式（III）化合物（其中Z为羟基保护基）在催化剂存在下反应，得到式（Ⅳ）化合物或其盐，除去羟基保护基，得到化合物式（Ⅴ）化合物或其盐; 将式（Ⅴ）化合物或其盐转化为式（I）化合物或其盐; 如果需要，将式（I）化合物转化为其盐，反之亦然。

6. 发明申请

US20090203915A1 Process for the preparation of solifenacin 审中-公开
标题翻译：索非那新的制备方法
公开(公告)号：US20090203915A1
公开(公告)日：2009-08-13
申请号：US12362506
申请日：2009-01-30
申请人： Pietro Allegrini , Lino Colombo , Marco Brusasca , Chiara Vladiskovic , Gabriele Razzetti , Emanuele Attolino
发明人： Pietro Allegrini , Lino Colombo , Marco Brusasca , Chiara Vladiskovic , Gabriele Razzetti , Emanuele Attolino
IPC分类号： C07D401/12
CPC分类号： C07D453/02
摘要： A process for the preparation of (1S,3′R)-quiniclidin-3′-yl-1-phenyl-3,4-dihydro-1H-isoquinolin-2-carboxylate, namely solifenacin, comprising the reaction of a compound of formula (IV) with a compound of formula (V), as herein defined, and the subsequent reaction with 3-quinuclidinol.
摘要翻译：制备（1S，3'R） - 奎宁环-3'-基-1-苯基-3,4-二氢-1H-异喹啉-2-羧酸酯的方法，即solifenacin，其包括式（Ⅳ）与本文定义的式（Ⅴ）化合物反应，随后与3-奎宁环醇反应。

7. 发明授权

US07385062B2 Process for the preparation of phenyltetrazole derivatives 失效
标题翻译：苯基四唑衍生物的制备方法
公开(公告)号：US07385062B2
公开(公告)日：2008-06-10
申请号：US10567492
申请日：2004-07-30
申请人： Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Alberto Bologna , Marcello Rasparini , Vittorio Lucchini
发明人： Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Alberto Bologna , Marcello Rasparini , Vittorio Lucchini
IPC分类号： C07D257/04
CPC分类号： C07D257/04 , C07F3/02
摘要： A process for the preparation of phenyltetrazole derivatives of formula (II) wherein R and Y are as defined in the disclosure, by direct ortho-metallation of (tetrazol-5-γl)benzene. The compounds of formula (II) are useful intermediates for the preparation of angiotensin II antagonists.
摘要翻译：制备式（II）的苯基四唑衍生物的方法，其中R和Y如本公开所定义，通过（四唑-5-基）苯的直接邻金属化。式（II）化合物是制备血管紧张素II拮抗剂的有用的中间体。

8. 发明申请

US20080039640A1 PROCESS FOR THE PREPARATION OF NITRILE COMPOUNDS 审中-公开
标题翻译：制备NITRILE化合物的方法
公开(公告)号：US20080039640A1
公开(公告)日：2008-02-14
申请号：US11835784
申请日：2007-08-08
申请人： Lino COLOMBO , Pietro ALLEGRINI , Alessandra AMOROSI , Gabriele RAZZETTI , Roberto ROSSI
发明人： Lino COLOMBO , Pietro ALLEGRINI , Alessandra AMOROSI , Gabriele RAZZETTI , Roberto ROSSI
IPC分类号： C07D311/02 , C07D405/04
CPC分类号： C07D311/24 , C07D311/22 , C07D405/04
摘要： A process for the preparation of a compound of formula (I) or a salt thereof wherein R is an amino, nitro or —NHCOR1 group, wherein R1 is C1-C6 alkyl or phenyl optionally substituted by a —O—(CH2)n-phenyl group, wherein n is an integer of 1 to 6; comprising reacting a compound of formula (II) or a salt thereof, both as the individual isomer and as an isomeric mixture, wherein R is as defined above; with a dehydrating agent, if necessary in the presence of an organic solvent, and optionally in the presence of a basic agent; and, if desired, converting a compound of formula (I) to another compound of formula (I) or a salt thereof.
摘要翻译：一种制备式（I）化合物或其盐的方法，其中R是氨基，硝基或-NHCOR 1个基团，其中R 1是C < 任选被-O-（CH 2）n - 亚苯基取代的C 1 -C 6烷基或苯基，其中n为1至6的整数; 包括使式（II）化合物或其盐作为单独的异构体和异构体混合物反应，其中R如上定义; 如果需要，在有机溶剂的存在下，任选地在碱性试剂的存在下，使用脱水剂; 如果需要，将式（I）化合物转化为另一种式（I）化合物或其盐。

9. 发明申请

US20070249662A1 PROCESS FOR THE PREPARATION OF PYRIDINE COMPOUNDS 失效
标题翻译：制备吡啶化合物的方法
公开(公告)号：US20070249662A1
公开(公告)日：2007-10-25
申请号：US11737852
申请日：2007-04-20
申请人： Pietro ALLEGRINI , Marcello Rasparini , Gabriele Razzetti , Roberto Rossi , Gianpiero Ventimiglia
发明人： Pietro ALLEGRINI , Marcello Rasparini , Gabriele Razzetti , Roberto Rossi , Gianpiero Ventimiglia
IPC分类号： A61K31/4439 , A61K31/4745 , C07D471/02 , C07D403/02
CPC分类号： C07D471/04 , C07D401/12
摘要： A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ═CR8— or ═N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; andeach R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.
摘要翻译：制备式（I）化合物的方法，均为异构体混合物和各异构体，其中Q为-CR 8 - 或-N-; 每个R 1，R 2，R 3，R 4，R 4独立地选自氢，卤素，羟基; 硝基任选被羟基取代的C 1 -C 6烷基; 烷硫基C 1 -C 6烷基; 任选被卤素或C 1 -C 6烷氧基取代的C 1 -C 6烷氧基; 苯基-C 1 -C 6烷基; 苯基-C 1 -C 6烷氧基; 和-N（RaRb），其中每个R a和R b独立地是氢或C 1 -C 6烷基或R a和R b与它们所连接的氮原子一起形成饱和杂环; 并且每个R 5，R 6，R 7，R 8和R 8独立地选自氢，卤素，羟基 ; 任选被羟基取代的C 1 -C 6烷基; 烷硫基C 1 -C 6烷基; 任选被卤素取代的C 1 -C 6烷氧基; C 1 -C 6烷基 - 羰基，C 1 -C 6烷氧基 - 羰基和恶唑-2（C 1 -C 6） - 基; 包括在催化剂存在下，如果需要在有机溶剂中将式（Ⅳ）化合物转化为所述式（Ⅳ）化合物。

10. 发明申请

US20070191439A1 Intermediates for the preparation of pramipexole 失效
标题翻译：用于制备普拉克索的中间体
公开(公告)号：US20070191439A1
公开(公告)日：2007-08-16
申请号：US10593269
申请日：2005-03-11
申请人： Graziano Castaldi , Alberto Bologna , Pietro Allegrini , Gabriele Razzetti , Vittorio Lucchini
发明人： Graziano Castaldi , Alberto Bologna , Pietro Allegrini , Gabriele Razzetti , Vittorio Lucchini
IPC分类号： A61K31/428 , C07D277/82
CPC分类号： C07D277/82
摘要： Intermediates useful for the preparation of pramipexole and the use thereof in such synthesis.
摘要翻译：可用于制备普拉克索的中间体及其在此类合成中的应用。

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