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1.
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。
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公开(公告)号:US20080146829A1
公开(公告)日:2008-06-19
申请号:US11958778
申请日:2007-12-18
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.
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公开(公告)号:US20070270483A1
公开(公告)日:2007-11-22
申请号:US11749977
申请日:2007-05-17
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。
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4.
公开(公告)号:US20100297711A1
公开(公告)日:2010-11-25
申请号:US12785746
申请日:2010-05-24
CPC分类号: C07F9/3264 , C07F9/306 , C07F9/572
摘要: Process for the preparation of intermediates useful in the synthesis of [1[S(R)],2α,4β]-4-cyclohexyl-1-[[[(2-methyl-1-oxypropoxy)propoxy](4-phenylbutyl)phosphinyl]acetyl]-L-proline, and the synthesis thereof, in particular as sodium salt.
摘要翻译: 制备可用于合成[1 [S(R)],2α,4α-环己基-1 - [[[(2-甲基-1-氧丙氧基)丙氧基](4-苯基丁基) )氧膦基]乙酰基] -L-脯氨酸及其合成,特别是钠盐。
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公开(公告)号:US20120277443A1
公开(公告)日:2012-11-01
申请号:US13451651
申请日:2012-04-20
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。
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公开(公告)号:US20080039640A1
公开(公告)日:2008-02-14
申请号:US11835784
申请日:2007-08-08
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。
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公开(公告)号:US20120149772A1
公开(公告)日:2012-06-14
申请号:US13295224
申请日:2011-11-14
IPC分类号: A61K31/216 , A61K31/225 , C07C69/34
CPC分类号: A61K31/222 , C07C213/06 , C07C217/62 , C07C219/28
摘要: A process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine) or a pharmaceutically acceptable salt thereof having low content in impurities.
摘要翻译: 一种制备杂质含量低的(R)-2-(3-二异丙基氨基-1-苯基丙基)-4-(羟甲基)苯酚异丁酸酯(非索罗定)或其药学上可接受的盐的方法。
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公开(公告)号:US20080076932A1
公开(公告)日:2008-03-27
申请号:US11861569
申请日:2007-09-26
申请人: Gabriele RAZZETTI , Lino COLOMBO , Paola ROTA , Pietro ALLEGRINI
发明人: Gabriele RAZZETTI , Lino COLOMBO , Paola ROTA , Pietro ALLEGRINI
IPC分类号: C07D405/14 , C07D233/90 , C07D403/10 , C07D405/12
CPC分类号: C07D405/14 , C07D233/90 , C07D405/10 , C07D405/12
摘要: A process for the preparation of olmesartan medoxomil, and derivatives thereof, by use of novel phenyltetrazole intermediates.
摘要翻译: 通过使用新的苯基四唑中间体制备奥美沙坦酯和其衍生物的方法。
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公开(公告)号:US20110034523A1
公开(公告)日:2011-02-10
申请号:US12849069
申请日:2010-08-03
IPC分类号: A61K31/4192 , C07D249/04 , A61P25/08
CPC分类号: C07D249/04
摘要: Disclosed is a crystalline form of rufinamide selected from: a substantially anhydrous and approximately monosolvated with trifluoroacetic acid crystalline form, hereinafter designated as Form α, and a crystalline form, hereinafter designated as Form β, characterised by an XRPD spectrum as shown in FIG. 3, wherein the most intense peaks fall at 4.5, 9.0, 13.5, 18.0, 18.8, 19.5, 20.6, 24.6, 25.7, 26.5, 27.4, 27.9, 28.7, 30.0 and 31.8±0.2° in 2θ.
摘要翻译: 公开了一种结晶形式的rufinamide,其选自:基本上无水并且用三氟乙酸结晶形式近似单溶剂化,以下称为形式α,和结晶形式,以下称为Form&bgr;其特征在于XRPD光谱如图1所示。 3,其中最强烈的峰在2℃下分别为4.5,9.0,13.5,18.0,18.8,19.5,20.6,24.6,27.7,26.5,27.4,27.9,28.7,30.0和31.8±0.2°。
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公开(公告)号:US20100292506A1
公开(公告)日:2010-11-18
申请号:US12770044
申请日:2010-04-29
IPC分类号: C07C227/32
CPC分类号: C07C229/08 , C07C227/04
摘要: A process for the preparation of a compound of formula (I) is disclosed, which comprises: a) the reaction of a compound of formula (II) with zinc azide of formula (III) Zn(N3)2 (III) in the presence of a solvent of formula R1—OH, wherein R1 is herein defined, to obtain a compound of formula (IV), b) its conversion into a compound of formula (V); c) its enantiomeric enrichment to obtain the (S) enantiomer of formula (VI); and d) the hydrolysis thereof.
摘要翻译: 公开了制备式(I)化合物的方法,其包括:a)在存在下使式(II)化合物与式(III)的叠氮化锌(N 3)2(III) 的式R 1 -OH的溶剂,其中R 1在本文中定义,以获得式(IV)的化合物,b)其转化为式(V)的化合物; c)其对映体富集以获得式(VI)的(S)对映异构体; 和d)其水解。
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