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1. 发明授权

US07662610B2 Synthesis of intermediates for the preparation of pramipexol 失效
标题翻译：用于制备普拉克索的中间体的合成
公开(公告)号：US07662610B2
公开(公告)日：2010-02-16
申请号：US11622259
申请日：2007-01-11
申请人： Sergio Riva , Paola Fassi , Michele Scarpellini , Pietro Allegrini , Gabriele Razzetti
发明人： Sergio Riva , Paola Fassi , Michele Scarpellini , Pietro Allegrini , Gabriele Razzetti
IPC分类号： C12P41/00
CPC分类号： C12P17/14 , C07D277/82 , C12P41/005
摘要： A process for the preparation of an acid of formula (I), as the individual (R) enantiomer or (S), or a salt thereof wherein R is a protected amino group; and the asterisk * denotes the stereogenic carbon atom, comprising contacting an ester of formula (II), as mixture of (R,S) enantiomers, or a salt thereof, wherein R1 is straight or branched C1-C6 alkyl, optionally substituted with phenyl; (the asterisk * and R defined above), with a lipase from Candida antarctica, under conditions effective to obtain a mixture comprising an acid of formula (I), as the individual (R) enantiomer, and an ester of formula (II), as the individual (S) enantiomer; the subsequent hydrolysis of the latter to obtain an acid of formula (I), as the individual (S) enantiomer; and, if desired, the conversion of an acid of formula (I), either as the (R) or (S) enantiomer, to a salt thereof.
摘要翻译：制备式（I）的酸作为单个（R）对映异构体或（S）的方法或其盐，其中R是被保护的氨基; 并且星号*表示立体碳原子，包括使式（II）的酯作为（R，S）对映体或其盐的混合物接触，其中R 1是直链或支链的C 1 -C 6烷基，任选被苯基 ; （上文定义的星号*和R）与来自南极念珠菌的脂肪酶在有效获得包含式（I）的酸的混合物作为个体（R）对映异构体的条件下，和式（II）的酯，作为个体（S）对映体; 随后水解后者以获得式（I）的酸作为单独的（S）对映异构体; 如果需要，将式（I）的酸作为（R）或（S）对映异构体转化为其盐。

2. 发明申请

US20070166814A1 SYNTHESIS OF INTERMEDIATES FOR THE PREPARATION OF PRAMIPEXOL 失效
标题翻译：合成制备PRAMIPEXOL的中间体
公开(公告)号：US20070166814A1
公开(公告)日：2007-07-19
申请号：US11622259
申请日：2007-01-11
申请人： Sergio RIVA , Paola Fassi , Michele Scarpellini , Pietro Allegrini , Gabriele Razzetti
发明人： Sergio RIVA , Paola Fassi , Michele Scarpellini , Pietro Allegrini , Gabriele Razzetti
IPC分类号： C12P41/00
CPC分类号： C12P17/14 , C07D277/82 , C12P41/005
摘要： A process for the preparation of an acid of formula (I), as the individual (R) enantiomer or (S), or a salt thereof wherein R is a protected amino group; and the asterisk * denotes the stereogenic carbon atom, comprising contacting an ester of formula (II), as mixture of (R, S) enantiomers, or a salt thereof, wherein R1 is straight or branched C1-C6 alkyl, optionally substituted with phenyl; the asterisk * and R defined above), with a lipase from Candida antarctica, under conditions effective to obtain a mixture comprising an acid of formula (I), as the individual (R) enantiomer, and an ester of formula (II), as the individual (S) enantiomer; the subsequent hydrolysis of the latter to obtain an acid of formula (I), as the individual (S) enantiomer; and, if desired, the conversion of an acid of formula (I), either as the (R) or (S) enantiomer, to a salt thereof.
摘要翻译：制备式（I）的酸作为单个（R）对映异构体或（S）的方法或其盐，其中R是被保护的氨基; 并且星号*表示立体碳原子，包括使式（II）的酯作为（R，S）对映体或其盐的混合物，其中R 1是直链或支链C 任选被苯基取代的C 1 -C 6烷基; 在有效获得包含式（I）的酸的混合物作为单独的（R）对映异构体和式（II）的酯的混合物的条件下，将来自南极念珠菌的脂肪酶与式（II）的酯作为个体（S）对映体; 随后水解后者以获得式（I）的酸作为单独的（S）对映异构体; 如果需要，将式（I）的酸作为（R）或（S）对映异构体转化为其盐。

3. 发明申请

US20070087422A1 Process for the preparation of (-) modafinil 失效
标题翻译：（ - ）莫达非尼的制备方法
公开(公告)号：US20070087422A1
公开(公告)日：2007-04-19
申请号：US11581580
申请日：2006-10-17
申请人： Sergio Riva , Paola Fassi , Pietro Allegrini , Gabriele Razzetti
发明人： Sergio Riva , Paola Fassi , Pietro Allegrini , Gabriele Razzetti
IPC分类号： C12P7/40
CPC分类号： C12P11/00 , C12P13/02
摘要： An enzymatic process for the preparation of intermediates useful in the synthesis of (−) modafinil.
摘要翻译：用于制备可用于合成（ - ）莫达非尼的中间体的酶促方法。

4. 发明授权

US07316918B2 Process for the preparation of (−) modafinil 失效
标题翻译：（ - ）莫达非尼的制备方法
公开(公告)号：US07316918B2
公开(公告)日：2008-01-08
申请号：US11581580
申请日：2006-10-17
申请人： Sergio Riva , Paola Fassi , Pietro Allegrini , Gabriele Razzetti
发明人： Sergio Riva , Paola Fassi , Pietro Allegrini , Gabriele Razzetti
IPC分类号： C12P13/02 , C12P11/00
CPC分类号： C12P11/00 , C12P13/02
摘要： An enzymatic process for the preparation of intermediates useful in the synthesis of (−) modafinil.
摘要翻译：用于制备可用于合成（ - ）莫达非尼的中间体的酶促方法。

5. 发明申请

US20080311635A1 PROCESS FOR THE PREPARATION OF (S)(+)-3-(AMINOMETHYL)-5-METHYLHEXANOIC ACID 审中-公开
标题翻译：（S）（+） - 3-（氨基甲酰基）-5-甲基六氢叶酸的制备方法
公开(公告)号：US20080311635A1
公开(公告)日：2008-12-18
申请号：US12119967
申请日：2008-05-13
申请人： Sergio Riva , Pietro Allegrini , Elena Serafini , Gabriele Razzetti , Simone Mantegazza , Dario Pastorello
发明人： Sergio Riva , Pietro Allegrini , Elena Serafini , Gabriele Razzetti , Simone Mantegazza , Dario Pastorello
IPC分类号： C12P13/00 , C07C271/10 , C07C229/02
CPC分类号： C07C271/22 , C07C229/08 , C12P13/007 , C12P41/005
摘要： A process for the preparation of (S)(+)-3-(aminomethyl)-5-methylhexanoic acid (pregabalin) of formula (I) or a salt thereof, comprising the reaction of a compound of formula (II) with an alcohol ROH, in the presence or absence of enzyme, to give a compound of formula (III) as herein defined the transformation of a compound of formula (III) into a compound of formula (VI) or (VIII) as herein defined, and the subsequent hydrolysis of a compound of formula (VI) or (VIII), to give pregabalin.
摘要翻译：制备式（I）的（S）（+） - 3-（氨基甲基）-5-甲基己酸（普瑞巴林）或其盐的方法，其包括式（II）化合物与醇的反应 ROH，在存在或不存在酶的情况下，得到本文定义的式（III）化合物，将式（III）化合物转化为本文定义的式（VI）或（VIII）化合物，并且随后水解式（VI）或（VIII）化合物，得到普瑞巴林。

6. 发明授权

US08203002B2 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：US08203002B2
公开(公告)日：2012-06-19
申请号：US12776588
申请日：2010-05-10
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： 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。

7. 发明申请

US20100267954A1 PROCESS FOR THE PURIFICATION OF PALIPERIDONE 审中-公开
标题翻译： PALIPERIDONE的纯化方法
公开(公告)号：US20100267954A1
公开(公告)日：2010-10-21
申请号：US12762522
申请日：2010-04-19
申请人： Simone Mantegazza , Emanuele Attolino , Gabriele Razzetti , Pietro Allegrini
发明人： Simone Mantegazza , Emanuele Attolino , Gabriele Razzetti , Pietro Allegrini
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Process for the purification of paliperidone by formation of a salt thereof, such as the hydrochloride.
摘要翻译：通过其盐形成盐酸盐来纯化帕培酮的方法。

8. 发明授权

US07741490B2 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：US07741490B2
公开(公告)日：2010-06-22
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： 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。

9. 发明授权

US07605268B2 Process for the preparation of pyridine compounds 失效
标题翻译：吡啶化合物的制备方法
公开(公告)号：US07605268B2
公开(公告)日：2009-10-20
申请号：US11737852
申请日：2007-04-20
申请人： Pietro Allegrini , Marcello Rasparini , Gabriele Razzetti , Roberto Rossi , Gianpiero Ventimigla
发明人： Pietro Allegrini , Marcello Rasparini , Gabriele Razzetti , Roberto Rossi , Gianpiero Ventimigla
IPC分类号： C07D401/12
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; and each 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-CR8-或-N-; 每个R 1，R 2，R 3，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C1-C6; 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C1-C6; 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烷氧羰基和恶唑-2-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. 发明授权

US07345189B2 Process for the preparation of adapalene 失效
标题翻译：阿达帕林制备方法
公开(公告)号：US07345189B2
公开(公告)日：2008-03-18
申请号：US11392909
申请日：2006-03-30
申请人： Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Mauro Ercoli
发明人： Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Mauro Ercoli
IPC分类号： C07C69/76
CPC分类号： C07C51/412 , C07C51/02 , C07C67/343 , C07C2603/74 , C07C65/26 , C07C69/94
摘要： A process for the preparation of a compound of formula (I), or a salt thereof wherein R is H, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; comprising the reaction between a compound of formula (II) wherein R1 and R2 are independently hydrogen, C1-C8 alkyl, aryl, aryl-C1-C8 alkyl, or R1 and R2, taken together, form a —(CH2)m—V—(CH2)n— group, in which V is NR3 or C(R3)2 wherein R3 is hydrogen, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III) in which R4 and R5 are independently C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; in the presence of a Ni (II) salt, an organic ligand and a basic agent, to obtain a compound of formula (I) wherein R is C1-C8 alkyl, aryl or aryl-C1-C8 alkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.
摘要翻译：制备式（I）化合物或其盐的方法，其中R为H，C 1 -C 8烷基，芳基或芳基-C C 1 -C 8烷基; 包括其中R 1和R 2独立地是氢，C 1 -C 8的式（II）化合物之间的反应烷基，芳基，芳基-C 1 -C 8烷基或R 1和R 2

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