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1. 发明授权

US5097059A Resolution process of intermediates useful for the preparation of diltiazem 失效
标题翻译：用于制备DILTIAZEM的中间体的解决方法
公开(公告)号：US5097059A
公开(公告)日：1992-03-17
申请号：US557808
申请日：1990-07-26
申请人： Claudio Giordano , Dario Tentorio , Roberto Casagrande , Placido Bertin , Valeriano Merli , Giorgio Sagramora
发明人： Claudio Giordano , Dario Tentorio , Roberto Casagrande , Placido Bertin , Valeriano Merli , Giorgio Sagramora
IPC分类号： C07B57/00 , A61K31/55 , C07C319/20 , C07C319/28 , C07C323/56 , C07D281/10
CPC分类号： C07C319/28
摘要： A process of spontaneous resolution of compounds of formula ##STR1## wherein R has the meanings reported in the description, is described. The compounds of formula III are intermediates useful for the preparation of Diltiazem.
摘要翻译：描述了其中R具有说明书中报道的含义的式（III）化合物III（苏式）的自发拆分方法。式III化合物是可用于制备地尔硫卓的中间体。

2. 发明授权

US5162309A Mono (2-ammonium-2-hydroxymethyl-1,3-propanediol)(2R,cis)-1,2-ep-oxipropyl-ph osphonate with improved characteristics of stability and processing 失效
标题翻译：具有改进的稳定性和加工特性的单（2-氨基-2-羟基甲基-1,3-丙二醇）（2R，CIS）-1,2-EP-氧代吡咯烷酮
公开(公告)号：US5162309A
公开(公告)日：1992-11-10
申请号：US557030
申请日：1990-07-25
申请人： Dario Tentorio , Graziano Castaldi , Claudio Giordano , Franco Pozzi
发明人： Dario Tentorio , Graziano Castaldi , Claudio Giordano , Franco Pozzi
IPC分类号： A61K31/665 , A61P31/04 , C07F9/38 , C07F9/655
CPC分类号： C07F9/65505
摘要： A process is described for the preparation of mono (2-ammonium-2-hydroxymethyl-1,3-propanediol) (2R,cis)-1,2-epoxypropyl-phosphonate with improved characteristics of stability, of processing for the preparation of pharmaceutical forms and of stability of the pharmaceutical forms that contain it.
摘要翻译：描述了制备具有改进的稳定性特征的制备单（2-氨基-2-羟甲基-1,3-丙二醇）（2R，顺式）-1,2-环氧丙基膦酸酯的方法，用于制备药物形式和含有它的药物形式的稳定性。

3. 发明授权

US5315005A Process for the single crystallization of enatiomeric ratio's (2S,3S):(2R,3R) of substituted 1,5-benzothiazepinone 失效
标题翻译：对映异构体比例（2S，3S）：（2R，3R）的取代的1,5-苯并硫氮酮的单结晶方法
公开(公告)号：US5315005A
公开(公告)日：1994-05-24
申请号：US8892
申请日：1993-01-25
申请人： Claudio Giordano , Dario Tentorio , Laura Russo
发明人： Claudio Giordano , Dario Tentorio , Laura Russo
IPC分类号： C07B57/00 , C07D281/10 , C07D281/02
CPC分类号： C07D281/10
摘要： A purification method of intermediates for the preparation of Diltiazem which consists of the crystallization of a mixture enantiomerically enriched in (2S,3S)-2,3-dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one is described.
摘要翻译：用于制备地尔硫卓的中间体的纯化方法，其由对映体富集（2S，3S）-2,3-二氢-3-羟基-2-（4-甲氧基苯基）-1,5-苯并硫氮杂 -4（5H） - 酮。

4. 发明授权

US5198557A Process for the resolution of 3-(4-substituted-phenyl)-glycidic acid derivatives 失效
标题翻译： 3-（4-取代苯基） - 甘氨酸衍生物的分解方法
公开(公告)号：US5198557A
公开(公告)日：1993-03-30
申请号：US698073
申请日：1991-05-10
申请人： Claudio Giordano , Roberto Casagrande
发明人： Claudio Giordano , Roberto Casagrande
IPC分类号： C07D301/32 , C07B57/00 , C07C319/28 , C07C323/56 , C07D281/10 , C07D303/48
CPC分类号： C07D281/10 , C07C319/28 , C07D303/48
摘要： A process for the kinetic resolution of cis or trans enantiomeric mixtures of the compounds of formula ##STR1## wherein R.sub.3 and X have the meanings reported in the specification and the asterisks mark the asymmetric carbon atoms, is described.The compounds of formula III-A are intermediates useful in the preparation of compounds active on the cardiovascular system.
摘要翻译：描述了式（III-A）化合物的顺式或反式对映异构体混合物的动力学拆分方法，其中R3和X具有本说明书中报道的含义和标记不对称碳原子的星号。式III-A的化合物是可用于制备在心血管系统上活性的化合物的中间体。

5. 发明授权

US5023381A Process for preparing an organic synthesis intermediate 失效
标题翻译：制备有机合成中间体的方法
公开(公告)号：US5023381A
公开(公告)日：1991-06-11
申请号：US454001
申请日：1989-12-20
申请人： Giulio Perdoncin , Claudio Giordano , Maurizio Paiocchi , Roberto Casagrande
发明人： Giulio Perdoncin , Claudio Giordano , Maurizio Paiocchi , Roberto Casagrande
IPC分类号： C07C45/46
CPC分类号： C07C45/46
摘要： A process is described for the preparation of 2-methoxy-6-propionyl-naphthalene, an intermediate in the synthesis of naproxen.The process consists of Friedel-Crafts acylation of 2-methoxy-naphthalene, and obviates the drawbacks related to the use of nitrobenzene as solvent.
摘要翻译：描述了一种制备2-甲氧基-6-丙酰基萘（萘普生合成中的中间体）的方法。该方法由2-甲氧基萘的Friedel-Crafts酰化反应，并且消除了与使用硝基苯作为溶剂相关的缺点。

6. 发明授权

US5102999A Process for the preparation of an intermediate of diltiazem 失效
标题翻译：制备DILTIAZEM中间体的方法
公开(公告)号：US5102999A
公开(公告)日：1992-04-07
申请号：US612954
申请日：1990-11-15
申请人： Claudio Giordano , Roberto Casagrande
发明人： Claudio Giordano , Roberto Casagrande
IPC分类号： C07B57/00 , C07D281/10
CPC分类号： C07D281/10
摘要： A process for the preparation of intermediates useful for the synthesis of Diltiazem consisting in the racemization of (--)-cis-2,3-dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one is described.
摘要翻译：（ - ） - 顺-2,3-二氢-3-羟基-2-（4-甲氧基苯基）-1,5-苯并硫氮杂-4（外消旋化合物）的外消旋化可用于合成地尔硫卓的中间体的制备方法 5H） - 酮。

7. 发明申请

US20130039983A1 PROCESS FOR THE PRODUCTION OF RALFINAMIDE SALTS SUBSTANTIALLY FREE FROM IMPURITIES HAVING GENOTOXIC EFFECTS 有权
标题翻译：生产具有生殖毒性作用的重金属盐生产过程大量免费
公开(公告)号：US20130039983A1
公开(公告)日：2013-02-14
申请号：US13643716
申请日：2011-04-06
申请人： Claudio Giordano , Erwin Waldvogel
发明人： Claudio Giordano , Erwin Waldvogel
IPC分类号： C07C303/32 , A61K9/28 , C07C309/04 , A61P25/28 , A61P25/08 , A61P25/04 , A61P25/06 , A61P25/24 , A61P25/00 , A61P29/00 , A61P15/00 , A61P13/00 , A61P3/00 , A61P1/00 , A61K31/205
CPC分类号： C07C237/08 , A61K31/165 , C07C231/24
摘要： The invention relates to a new process for the production and/or purification of the salt of the compound (S)-2-[4-(2-fluorobenzyloxy)benzylamino]propanamide, i.e. ralfinamide, or the respective R-enantiomer, with methanesulfonic acid in high yields and very high enantiomeric and chemical purity in the form of the crystalline anhydrous polymorph identified as form A, wherein said salt is substantially free from impurities having genotoxic effect, such as (C1-C5)alkanylmethanesulfonates, and residual solvents known as potential precursors thereof, such as (C1-C5)alkanols or esters thereof with lower alkanoic acids.The process foresees (i) production and/or crystallization of the salt, from water, acetone, an aliphatic ketone of 4-5 carbon, atoms or mixtures thereof with water, or (ii) slurring the solid salt with (a) water, (b) a mixture of water with acetone or an aliphatic ketone of 4-5 carbon atoms, (c) acetone, an aliphatic ketone of 4-5 carbon atoms or a mixture thereof, or (iii) exposure of the solid salt to air stream having high degree of relative humidity, and, when the obtained product consists as a whole or in part of crystalline hemihydrate pseudopolymorph form H crystals, converting said product into anhydrous form A crystals by submitting it to water removal.The crystalline hemihydrate pseudopolymorph form H of ralfinamide methanesulfonate, or its R-enantiomer, is a useful intermediate for obtaining the crystalline anhydrous polymorph A free from the above impurities having genotoxic effect and/or residual solvents known as precursors thereof, and exhibits a physicochemical profile conferring significant advantages in the design and development of solid dosage forms, in particular, of modified release formulations.
摘要翻译：本发明涉及一种用于生产和/或纯化化合物（S）-2- [4-（2-氟苄氧基）苄氨基]丙酰胺（即Ralfinamide）或相应的R-对映异构体与甲磺酸盐的新方法酸的高产率和非常高的对映异构体和化学纯度，以结晶无水多晶型物的形式鉴定为形式A，其中所述盐基本上不含具有基因毒性作用的杂质，例如（C 1 -C 5）烷基甲磺酸盐，以及称为其潜在的前体，例如（C1-C5）链烷醇或其与低级链烷酸的酯。该方法预期（i）从水，丙酮，4-5碳原子或其混合物的水的脂族酮生成和/或结晶盐，或（ii）将固体盐与（a）水，（b）水与丙酮或4-5个碳原子的脂族酮的混合物，（c）丙酮，4-5个碳原子的脂肪族酮或其混合物，或（iii）将固体盐暴露于空气中具有高相对湿度的流，并且当所得产物全部或部分由晶体半水合物假多晶型物形成H晶体时，通过将所述产物转移到除去水中而将所述产物转化为无水形式的A晶体。 Ralfinamide甲磺酸盐或其R-对映异构体的结晶半水合物假多晶型物形式H是获得不含上述具有遗传毒性作用的杂质的结晶无水多晶型物A和/或已知为其前体的残留溶剂的有用中间体，并且显示出物理化学特征赋予固体剂型，特别是改性释放制剂的设计和开发中显着的优点。

8. 发明授权

US06765097B1 Process for the preparation of aryl-pyridinyl compounds 有权
标题翻译：芳基 - 吡啶基化合物的制备方法
公开(公告)号：US06765097B1
公开(公告)日：2004-07-20
申请号：US10110685
申请日：2002-04-11
申请人： Claudio Giordano , Claudio Pozzoli , Fabio Benedetti
发明人： Claudio Giordano , Claudio Pozzoli , Fabio Benedetti
IPC分类号： C07D21346
CPC分类号： C07D213/53 , C07D213/48 , C07D405/10
摘要： A process is described for the preparation of arylpyridine compounds by aryl-aryl cross-coupling reactions between a halopyridine and an arylmagnesium halide carried out in the presence of a catalytic amount of a zinc salt and a catalytic amount of palladium. The zinc salt is preferably selected from ZnCl2, ZnBr2 and/or Zn(OAc)2, while the palladium is preferably used in the form of Pd(PPh3)4 or Pd(OAc)2 +4 PPh3. The reaction can also be carried out in the presence of bidentate phosphines, such as, for example, 1,3-bis(diphenylphosphine)propane or 1,4-bis(diphenylphosphine)-butane. It is thus possible to obtain molar yields higher than 97% (calculated relative to the halopyridine) and a catalyticity of more than 2000.
摘要翻译：描述了通过在催化量的锌盐和催化量的钯的存在下在卤代吡啶和卤化吡嗪之间的芳基 - 芳基交叉偶联反应制备芳基吡啶化合物的方法。锌盐优选选自ZnCl 2，ZnBr 2和/或Zn（OAc）2，而钯优选以Pd（PPh 3）4或Pd（OAc）2 + 4 PPh 3的形式使用。反应也可以在二齿膦存在下进行，例如1,3-双（二苯基膦）丙烷或1,4-双（二苯基膦） - 丁烷。因此可以获得高于97％的摩尔收率（相对于卤代吡啶计算）和超过2000的催化剂。

9. 发明授权

US5362871A Process for the direct and regioselective functionalization in position 2 of phenothiazine 失效
标题翻译：吩噻嗪2位直接和区域选择性官能化方法
公开(公告)号：US5362871A
公开(公告)日：1994-11-08
申请号：US833800
申请日：1992-02-12
申请人： Claudio Giordano , Maurizio Paiocchi , Paolo Cavalleri
发明人： Claudio Giordano , Maurizio Paiocchi , Paolo Cavalleri
IPC分类号： C07D279/22 , C07D279/20 , C07D279/30 , C07D279/32 , C07B45/06
CPC分类号： C07D279/30 , C07D279/20
摘要： A process for the direct and regioselective functionalization of phenothiazine which allows one to introduce an SH group in position 2, said process comprising the sulfination or sulfonation of the phenothiazine N-protected with an alkoxycarbonyl, an alkylsulfonyl or an arylsulfonyl group, the reduction of the produce obtained to give the N-protected 2-mercapto-phenothiazine, and the deprotection of the nitrogen atom. The thus-obtained 2-mercapto-phenothiazine is an important intermediate for the preparation of pharmacological active compounds.
摘要翻译：用于直接和区域选择性官能化吩噻嗪的方法，其允许在位置2引入SH基团，所述方法包括被烷氧基羰基，烷基磺酰基或芳基磺酰基N-保护的吩噻嗪的硫酸化或磺化，得到N-保护的2-巯基吩噻嗪得到的产物和氮原子的去保护。由此获得的2-巯基吩噻嗪是制备药理活性化合物的重要中间体。

10. 发明授权

US5274186A Intermediates and their use in the synthesis of organic compounds 失效
标题翻译：中间体及其在合成有机化合物中的应用
公开(公告)号：US5274186A
公开(公告)日：1993-12-28
申请号：US299075
申请日：1989-01-19
申请人： Claudio Giordano , Graziano Castaldi
发明人： Claudio Giordano , Graziano Castaldi
IPC分类号： C07C51/00 , C07D317/34 , C07C63/36 , C07C63/04
CPC分类号： C07D317/34 , C07C51/00
摘要： Compounds of formula ##STR1## (wherein Ar, R, R.sub.1 and X have the meaning reported in the description) are useful intermediates for the preparation of a variety of organic compounds, also optically active, like alpha-haloketones, alpha-hydroxyketones or ketals, alpha-arylalkanoic acids.
摘要翻译：式（I）化合物（其中Ar，R，R 1和X具有说明书中报道的含义）是制备各种有机化合物的有用的中间体，也是光学活性的，如α-卤代酮，羟基酮或缩酮，α-芳基链烷酸。

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