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1. 发明授权

US5721360A Process for the preparation of a thiazoline-azetidinone 失效
标题翻译：制备噻唑啉 - 氮杂环丁酮的方法
公开(公告)号：US5721360A
公开(公告)日：1998-02-24
申请号：US656979
申请日：1996-06-06
申请人： Gianfranco Cainelli , Achille Umani Ronchi , Michele Contento , Mauro Panunzio , Sergio Sandri , Marco Da Col , Leone Dall'Asta
发明人： Gianfranco Cainelli , Achille Umani Ronchi , Michele Contento , Mauro Panunzio , Sergio Sandri , Marco Da Col , Leone Dall'Asta
IPC分类号： C07D205/085 , C07D513/04 , C07D205/12
CPC分类号： C07D513/04
摘要： The present invention refers to process for the preparation of a tiazoline-azetidinone of formula I ##STR1## which comprises N-protecting in position 1 of (3S,4S)-3-phenylace tamido-4-acetoxy-azetidin-2-one, converting the product thus obtained into the corresponding thioamide and subsequently ciclyzing and deprotecting.
摘要翻译：本发明涉及制备（3S，4S）-3-苯基三氨基-4-乙酰氧基 - 氮杂环丁烷-2-酮的式Ⅰ的噻唑烷 - 氮杂环丁酮的方法，将所得产物转化为相应的硫代酰胺随后凝结和脱保护。

2. 发明授权

US5532353A Process for the preparation of halogenated .beta.-lactam compounds 失效
标题翻译：卤代β-内酰胺化合物的制备方法
公开(公告)号：US5532353A
公开(公告)日：1996-07-02
申请号：US58714
申请日：1993-05-10
申请人： Marco Da Col , Leone Dall'Asta , Irene Resta , Gianfranco Cainelli , Michele Contento , Mauro Panunzio , Achille Umani Ronchi
发明人： Marco Da Col , Leone Dall'Asta , Irene Resta , Gianfranco Cainelli , Michele Contento , Mauro Panunzio , Achille Umani Ronchi
IPC分类号： C07D501/00 , C07D501/59 , C07D501/02
CPC分类号： C07D501/00
摘要： There is described the preparation of halogenated .beta.-lactam derivatives by introduction of a chlorine atom in the 3-position of the cephem nucleus starting from a 3-sulfonyloxycephem. Such starting materials are reacted with a chlorine ions donor in a basic medium.
摘要翻译：描述了由3-磺酰氧基头孢烯引入头孢烯核的3-位上的氯原子制备卤代β-内酰胺衍生物。这样的原料与碱性介质中的氯离子供体反应。

3. 发明授权

US5693790A Crystalline form of a cephalosporin antibiotic 失效
标题翻译：结晶形式的头孢菌素抗生素
公开(公告)号：US5693790A
公开(公告)日：1997-12-02
申请号：US455136
申请日：1995-05-31
申请人： Marco Da Col , Leone Dall'Asta , Irene Resta
发明人： Marco Da Col , Leone Dall'Asta , Irene Resta
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/59 , C07D501/32
CPC分类号： C07D501/00 , A61K31/545
摘要： The preparation of a novel crystalline cefaclor and the conversion of such a product to cefaclor monohydrate are described. The new intermediate cefaclor is a particular crystalline form and possesses the same antibiotic properties as cefaclor monohydrate.
摘要翻译：描述了新型结晶头孢克洛的制备和这种产物转化为头孢克洛一水合物。新的中间体头孢克洛是一种特殊的结晶形式，具有与头孢克洛一水合物相同的抗生素特性。

4. 发明授权

US5589593A Crystalline form of a cephalosporin antibiotic 失效
标题翻译：结晶形式的头孢菌素抗生素
公开(公告)号：US5589593A
公开(公告)日：1996-12-31
申请号：US483888
申请日：1995-06-07
申请人： Marco Da Col , Leone Dall'Asta , Irene Resta
发明人： Marco Da Col , Leone Dall'Asta , Irene Resta
IPC分类号： A61K31/545 , C07D501/00 , C07D501/59 , C07D501/32
CPC分类号： C07D501/00 , A61K31/545
摘要： The preparation of a novel crystalline cefaclor and the conversion of such a product to cefaclor monohydrate are described. The new intermediate cefaclor is a particular crystalline form and possesses the same antibiotic properties as cefaclor monohydrate.
摘要翻译：描述了新型结晶头孢克洛的制备和这种产物转化为头孢克洛一水合物。新的中间体头孢克洛是一种特殊的结晶形式，具有与头孢克洛一水合物相同的抗生素特性。

5. 发明授权

US07411077B2 Process for the preparation of a cyano-isobenzofuran 失效
标题翻译：制备氰基异苯并呋喃的方法
公开(公告)号：US07411077B2
公开(公告)日：2008-08-12
申请号：US10549062
申请日：2004-03-09
申请人： Giovanni Cotticelli , Leone Dall'Asta , Gianluca Di Lernia
发明人： Giovanni Cotticelli , Leone Dall'Asta , Gianluca Di Lernia
IPC分类号： C07D307/87 , C07D307/00
CPC分类号： C07D307/87
摘要： A process for the preparation of citalopram and the pharmaceutically acceptable salts therof is disclosed by reacting 5-cyanophthalide with a 4-fluorophenyl magnesium halide, reducing the 3-hydroxymethyl-4-(4-fluorobenzoyl)benzonitrile with an agent reducing ketones to alcohols, submitting the thus-obtained 3-hydroxymethyl-4-[(4-fluorophenyl)hydroxymethyl)benzonitrile to a cyclization reaction to give 1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile without 1,1-bis(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile and treating 1,1-bis(4 fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile with a 3-(dimetylamino)propyl halide in the presence of a base.
摘要翻译：通过5-氰基苯酞与4-氟苯基卤化镁反应来制备西酞普兰和药学上可接受的盐的制备方法，将3-羟甲基-4-（4-氟苯甲酰基）苄腈用还原酮还原成醇，将由此得到的3-羟甲基-4 - [（4-氟苯基）羟甲基）苄腈进行环化反应，得到1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈， 4-氟苯基）-1,3-二氢-5-异苯并呋喃并在碱存在下用1-（二甲基氨基）丙基卤处理1,1-二（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈。

6. 发明申请

US20080249319A1 Process for the preparation of 5-Carboxyphthalide 审中-公开
标题翻译：制备5-羧基苯酞的方法
公开(公告)号：US20080249319A1
公开(公告)日：2008-10-09
申请号：US11975842
申请日：2007-10-22
申请人： Leone Dall'Asta , Umberto Casazza , Giovanni Cotticelli
发明人： Leone Dall'Asta , Umberto Casazza , Giovanni Cotticelli
IPC分类号： C07D307/77
CPC分类号： C07D307/83 , C07D307/88
摘要： There is described a process for the preparation of 5-carboxy phthalide, which comprises adding terephthalic acid to fuming sulfuric acid containing at least 20% of SO3, then adding formaldehyde to the mixture, heating the mixture at a temperature of 120-145° C. and isolating 5-carboxyphthalide from the reaction mixture.
摘要翻译：描述了制备5-羧基苯酞的方法，其包括将对苯二甲酸加入到含有至少20％SO 3 N的发烟硫酸中，然后向混合物中加入甲醛，将混合物加热至温度为120-145℃，并从反应混合物中分离出5-羧基邻苯二甲酸盐。

7. 发明申请

US20060183925A1 Process for the preparation of a cyano-isobenzofuran 失效
标题翻译：制备氰基异苯并呋喃的方法
公开(公告)号：US20060183925A1
公开(公告)日：2006-08-17
申请号：US10549062
申请日：2004-03-09
申请人： Giovanni Cottocelli , Leone Dall'Asta , Gianluca Lemia
发明人： Giovanni Cottocelli , Leone Dall'Asta , Gianluca Lemia
IPC分类号： C07D307/87
CPC分类号： C07D307/87
摘要： A process for the preparation of citalopram and the pharmaceutically acceptable salts therof is disclosed by reacting 5-cyanophthalide with a 4-fluorophenyl magnesium halide, reducing the 3-hydroxymethyl-4-(4-fluorobenzoyl)benzonitrile with an agent reducing ketones to alcohols, submitting the thus-obtained 3-hydroxymethyl-4-[(4-fluorophenyl)hydroxymethyl) benzonitrile to a cyclization reaction to give 1-(4-fluorophenyl)-1,3-dihydro-5isobenzofurancarbonitrile without 1,1-bis(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile and treating 1,1-bis(4 fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile with a 3-(dimetylamino)propyl halide in the presence of a base.
摘要翻译：通过5-氰基苯酞与4-氟苯基卤化镁反应来制备西酞普兰和药学上可接受的盐的制备方法，将3-羟甲基-4-（4-氟苯甲酰基）苄腈用还原酮还原成醇，将由此得到的3-羟甲基-4 - [（4-氟苯基）羟甲基）苄腈进行环化反应，得到1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈，无1-双（4- （4-氟苯基）-1,3-二氢-5-异苯并呋喃腈，并在碱的存在下用3-（二甲基氨基）丙基卤处理1,1-二（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈。

8. 发明授权

US06365747B1 Method for the preparation of citalopram 有权
标题翻译：西酞普兰制备方法
公开(公告)号：US06365747B1
公开(公告)日：2002-04-02
申请号：US09830109
申请日：2001-06-01
申请人： Leone Dall'Asta , Umberto Casazza , Hans Petersen
发明人： Leone Dall'Asta , Umberto Casazza , Hans Petersen
IPC分类号： C07D30787
CPC分类号： C07D307/87 , C07D263/14 , C07D413/04
摘要： The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising treatment of a compound of formula (IV), wherein X is O or S; R1-R2 are each independently selected from hydrogen and C1-6 alkyl, or R1 and R2 together form a C2-5 alkylene chain thereby forming a spiro-ring; R3 is selected from hydrogen and C1-6 alkyl, R4 is selected from hydrogen, C1-6 alkyl, a carboxy group or a precursor group therefore, or R3 and R4 together form a C2-5 alkylene chain thereby forming a spiro-ring, with a dehydration agent or alternatively where X is S, thermally cleavage of the thiazoline ring, or treatment in presence of a radical initiator, to form citalopram. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.
摘要翻译：本发明涉及一种制备西酞普兰或其任何对映异构体及其酸加成盐的方法，包括处理式（IV）化合物，其中X为O或S; R 1 -R 2各自独立地选自氢和C 1-6烷基，或者R 1和R 2一起形成C 2-5亚烷基链，从而形成螺环; R3选自氢和C 1-6烷基，因此R4选自氢，C 1-6烷基，羧基或前体基，或者R 3和R 4一起形成C 2-5亚烷基链，从而形成螺环，用脱水剂或者其中X是S，噻唑啉环的热裂解，或在自由基引发剂的存在下进行处理以形成西酞普兰。本发明还涉及用于制备西酞普兰的新方法的中间体以及根据新方法制备的西酞普兰。

9. 发明授权

US5621085A Process for the preparation of amikacin precursors 失效
标题翻译：制备阿米卡星前体的方法
公开(公告)号：US5621085A
公开(公告)日：1997-04-15
申请号：US459649
申请日：1995-06-02
申请人： Leone Dall'Asta , Eugenio Garegnani
发明人： Leone Dall'Asta , Eugenio Garegnani
IPC分类号： C07H15/234 , C07H15/236 , C07H15/26 , C07H1/00
CPC分类号： C07H15/26 , C07H15/234 , Y02P20/55
摘要： Process for the preparation of a 3,6'-di-N-Acyl-1-[L-(-)-4-Acylamino-2-hydroxybutyryl] kanamycin A, wherein Acyl is a N-protecting acylating group, which comprises reacting kanamycin A with an aluminum salt in an inert organic solvent, treating the aluminum complex thus obtained with a N-acylating agent and acidifiying the reaction mixture, as such or after having removed the complexing aluminum in basic medium and isolated the 3,6'-di-N-Acyl-kanamycin A, to pH 6, treating the protonated 3,6'-di-N-Acyl-kanamycin A, in form of a salt thereof, with an active derivative of L-(-)-4-Acyl-amino-2-hydroxybutyric acid, wherein Acyl is a N-protecting group preferably identical with that which protects the amino groups in the positions 3 and 6' of kanamycin A, and isolating the product thus obtained by simple correction of the pH.
摘要翻译：制备3,6'-二-N-酰基-1- [L - （ - ） - 4-酰基氨基-2-羟基丁酰基]卡那霉素A的方法，其中酰基是N-保护性酰化基团，其包括使卡那霉素A与铝盐在惰性有机溶剂中反应，用N-酰化剂处理由此获得的铝络合物，并酸化反应混合物，或者在除去碱性介质中的络合铝并分离出3,6'- 将二-N-酰基卡那霉素A转化至pH6，用其盐形式的质子化的3,6'-二-N-酰基卡那霉素A与活性衍生物L - （ - ） - 酰基 - 氨基-2-羟基丁酸，其中酰基是N-保护基，优选与保护卡那霉素A的3'和6'位氨基的那些相同，并通过简单校正pH分离由此获得的产物。

10. 发明授权

US3959266A Process for the conversion of penicillin S-oxide into a corresponding desatoxycephalosporin 失效
标题翻译：将青霉素S-氧化物转化成相应的脱氢头孢菌素的方法
公开(公告)号：US3959266A
公开(公告)日：1976-05-25
申请号：US372638
申请日：1973-06-22
申请人： Leone Dall'Asta
发明人： Leone Dall'Asta
IPC分类号： C07D20060101 , C07D205/08 , C07D209/48 , C07D233/28 , C07D261/18 , C07D279/06 , C07D307/54 , C07D333/24 , C07D501/10 , C07D501/20 , C07G20060101
CPC分类号： C07D501/10
摘要： A penicillin S-oxide is rearranged into the corresponding desacetoxycephalosporin compound by heating said penicillin S-oxide at a temperature of from 70 to 140.degree.C in the presence of a sulfoxide of formula R.sup.1 -SO-R.sup.2, preferably dimethyl sulfoxide, or a sulfonium or sulfoxonium salt of said sulfoxyde or a mixture of said sulfoxide and said sulfonium or sulfoxonium salt. The sulfoxide may act as reaction medium as well as reactant or an inert organic solvent may be used as a reaction medium.
摘要翻译：在式R1-SO-R2亚砜，优选二甲基亚砜存在下，在70〜140℃的温度下加热所述青霉素S-氧化物，将青霉素S-氧化物重排成相应的去乙酸基头孢菌素化合物，或锍或所述亚砜基的氧化锍盐或所述亚砜和所述锍或氧化锍盐的混合物。亚砜可以作为反应介质以及反应物，也可以使用惰性有机溶剂作为反应介质。

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