公开(公告)号：US20090076277A1

公开(公告)日：2009-03-19

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： C07D401/02

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是-CR 8 - 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。

公开(公告)号：US20070270483A1

公开(公告)日：2007-11-22

申请号：US11749977

申请日：2007-05-17

申请人： Simone MANTEGAZZA ,  Gabriele RAZZETTI ,  Marcello RASPARINI ,  Roberto ROSSI ,  Pietro ALLEGRINI

发明人： Simone MANTEGAZZA ,  Gabriele RAZZETTI ,  Marcello RASPARINI ,  Roberto ROSSI ,  Pietro ALLEGRINI

IPC分类号： A61K31/381 ,  C07D333/22

CPC分类号： C07C213/08 ,  Y02P20/55

摘要： A process for preparation of a compound of formula (I), or a salt thereof, both as individual isomer and as mixtures thereof, wherein each of A and B is independently aryl or heteroaryl optionally substituted with 1 to 4 substituents; and R and R1, which can be the same or different, are hydrogen, C1-C6 alkyl or an amino-protecting group; comprising the reaction of a compound (II) wherein A and B are as defined above, with a compound (III) wherein each of R and R1 is independently C1-C6 alkyl or an amino-protecting group; and X is a leaving group; in the presence of a basic agent; and, if desired the conversion of a compound (I) to another compound (I); and/or, if desired, the separation of an isomeric mixture of a compound (I) into the individual isomers; and/or, if desired, the conversion of a compound (I) to a salt thereof.

摘要翻译： 制备式（I）化合物或其盐作为单独异构体及其混合物的方法，其中A和B各自独立地为任选被1至4个取代基取代的芳基或杂芳基; R 1和R 2可以相同或不同，为氢，C 1 -C 6烷基或氨基保护基 ; 包括其中A和B如上定义的化合物（II）与化合物（III）的反应，其中R和R 1各自独立地为C 1〜 C 6烷基或氨基保护基; X为离去群; 在一个基本代理人的面前; 并且如果需要，化合物（I）转化为另一化合物（I）; 和/或如果需要，将化合物（I）的异构体混合物分离成单独的异构体; 和/或如果需要，化合物（I）转化为其盐。

公开(公告)号：US20080146829A1

公开(公告)日：2008-06-19

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), as herein defined, by condensation of N,N-diethyl-cyano-acetamide with a compound of formula (IV), as herein defined, in the presence of a strong basic agent; the dealkylation of said compound of formula (V) to obtain entacapone and the crystallization thereof to the polymorphic form A.

摘要翻译： 恩替卡朋的制备方法，特别是多晶型A，其包括通过N，N-二乙基 - 氰基 - 乙酰胺与式（III）化合物的缩合制备如本文定义的式（Ⅴ）化合物 IV），如本文所定义的，在强碱性剂的存在下; 所述式（V）化合物的脱烷基化以获得恩他卡朋，并将其结晶化为多晶型A.

公开(公告)号：US20110269962A1

公开(公告)日：2011-11-03

申请号：US13092171

申请日：2011-04-22

申请人： Maurizio TADDEI ,  Evita BALDUCCI ,  Emanuele ATTOLINO ,  Simone MANTEGAZZA ,  Gianmaria DELL'ANNA

发明人： Maurizio TADDEI ,  Evita BALDUCCI ,  Emanuele ATTOLINO ,  Simone MANTEGAZZA ,  Gianmaria DELL'ANNA

IPC分类号： C07D215/14 ,  C07F7/18

CPC分类号： C07D215/14

摘要： Process for the preparation of β-ketoester synthetic intermediates useful in the preparation of statins, in particular Pitavastatin.

摘要翻译： 用于制备可用于制备他汀类药物的合成中间体的方法，特别是匹他伐他汀。