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1.发明申请17.Beta-(alpha-hydroxy)-esters of androstanes as intermediates for the preparation of 17.beta-fluorinated-androstane esters 审中-公开17.作为制备17.β-氟化 - 雄甾烷酯的中间体的雄甾烷的β-（α-羟基） - 酯公开(公告)号：US20060116359A1
公开(公告)日：2006-06-01
申请号：US10538083
申请日：2003-12-18
申请人： Gianfranco Cainelli , Achille Umani Ronchi , Sergio Sandri , Michele Contento , Giuseppe Fortunato , Marco Da Col , Maria Boriani , Stefano Da Col
发明人： Gianfranco Cainelli , Achille Umani Ronchi , Sergio Sandri , Michele Contento , Giuseppe Fortunato , Marco Da Col , Maria Boriani , Stefano Da Col
IPC分类号： A61K31/573 , C07J3/00
CPC分类号： C07J31/006 , C07J71/0015 , C07J71/0031
摘要： Process for the preparation of polyhalogenated steroids, in particular of androstanic fluoro derivatives corticosteroids by means of the formation of new androstanic S-hydroxy alkyl or aralkyl-17-carbothioate intermediates.
摘要翻译： 通过形成新的雄激素S-羟基烷基或芳烷基-17-硫代磷酸酯中间体，制备多卤代类固醇，特别是曲霉氟衍生物皮质类固醇的方法。
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2.发明申请Process for the preparation of 6alpha-fluoro steroids by isomerisation of 6beta-fluorosteroids 审中-公开通过6β-荧光素类异构化制备6α-氟类固醇的方法公开(公告)号：US20050192437A1
公开(公告)日：2005-09-01
申请号：US10508668
申请日：2003-03-31
申请人： Gianfranco Cainelli , Achille Umani-Ronchi , Sergio Sandri , Michele Contento , Marco Da Col , Maria Boriani , Stefano Da Col
发明人： Gianfranco Cainelli , Achille Umani-Ronchi , Sergio Sandri , Michele Contento , Marco Da Col , Maria Boriani , Stefano Da Col
CPC分类号： C07J71/0031 , C07J3/005 , C07J31/006
摘要： The process for the preparation of 6α-fluoro steroids, comprising the reaction of the corresponding 6β-fluoro steroids, or of 6α/6β isomeric mixtures with an organic base having a diazo iminic group, in a suitably selected organic solvent, is described.
摘要翻译： 描述了制备6α-氟类固醇的方法，其包括相应的6β-氟类固醇或6α/6β异构体混合物与具有重氮亚胺基团的有机碱在适当选择的有机溶剂中的反应。
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3.发明授权Method for the removal of the formyl group from an ester of an N-formyl peptide or N-formyl aminoacid 失效从N-甲酰基肽或N-甲酰基氨基酸的酯中除去甲酰基的方法
公开(公告)号：US4851563A
公开(公告)日：1989-07-25
申请号：US905476
申请日：1986-09-09
CPC分类号： C07K5/0613 , C07K1/063 , C07K1/122 , Y10S530/801
摘要： A method for the removal of the formyl group from an ester of an N-formyl peptide or N-formyl aminoacid, in which the ester is reacted with urea in the presence of a polar solvent and a strong acid.
摘要翻译： 从N-甲酰基肽或N-甲酰基氨基酸的酯除去甲酰基的方法，其中该酯在极性溶剂和强酸存在下与脲反应。
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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。
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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。
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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。
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7.发明授权Process for the preparation of 17-acyl esters of 17.alpha., 21-dihydroxysteroids of the pregnane series and novel products 失效制备17 {60，孕烷系列和新产物{0-21-二羟基类固醇的17-酰基酯的方法
公开(公告)号：US3998701A
公开(公告)日：1976-12-21
申请号：US529134
申请日：1974-12-03
申请人： Alberto Ercoli , Marco Da Col
发明人： Alberto Ercoli , Marco Da Col
IPC分类号： C07C20060101 , C07J20060101 , C07J5/00 , C12D13/02
摘要： A process is disclosed for making 17-monoesters of 17 .alpha., 21-dihydroxy steroids by acylating a 17 .alpha., 21-dihydroxy steroid phosphate and then subjecting the intermediate 17-acyloxy-21-phosphate to dephosphorylation using an acid phosphatase to achieve enzymatic hydrolysis. Several new 17-monoesters having an anti-inflammatory property are also disclosed.
摘要翻译： 公开了通过酰化17α，21-二羟基类固醇磷酸酯然后使用酸性磷酸酶对中间体17-酰氧基-21-磷酸进行脱磷酸化来制备17α，21-二羟基类固醇的17-单酯以达到酶水解的方法 。 还公开了几种具有抗炎性质的新型17-单酯。
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公开(公告)号：US06794503B2
公开(公告)日：2004-09-21
申请号：US09858692
申请日：2001-05-16
申请人： Filippo La Loggia , Marco Da Col
发明人： Filippo La Loggia , Marco Da Col
IPC分类号： C07J7100
CPC分类号： C07J71/0015
摘要： Described herein is a process for the preparation of 6&agr;-fluorosteroids of formula (I), in which R is chosen from H, OH and an alkyl group with from 1 to 4 carbon atoms and R′ is a carboxyalkyl group with from 1 to 4 carbon atoms in the alkyl chain, comprising the selective fluorination at the 6&agr;-position by treatment of the compound of formula (III), wherein R and R′ are as defined above, with an electrophilic fluorinating agent.
摘要翻译： 本文描述了制备式（I）的6α-荧光素的方法，其中R选自H，OH和具有1至4个碳原子的烷基，R'是具有1-4个碳原子的羧基烷基 包括通过用亲电氟化剂处理其中R和R'如上定义的式（III）化合物在6α-位置的选择性氟化。
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9.发明授权Isomerisation of 6&bgr;-fluorosteroids into the corresponding 6&agr;-fluoro derivatives 失效6β-氟甾类异构化成相应的6α-氟衍生物公开(公告)号：US06369218B1
公开(公告)日：2002-04-09
申请号：US09858407
申请日：2001-05-16
IPC分类号： C07J500
摘要： Described herein is the isomerisation process of 6&bgr;-fluorosteroids into the corresponding pharmacologically active 6&agr;-fluoro derivatives, comprising the reaction of 6&bgr;-fluorosteroids, or 6&agr;/6&bgr; isomeric mixtures, with an organic base containing a diazoimino group in a suitable organic solvent.
摘要翻译： 本文描述了6β-荧光素类化合物进入相应的药理学活性6α-氟衍生物的异构化过程，其包括6β-荧光素类或6α/6β异构体混合物与合适的有机溶剂中含有重氮基亚氨基的有机碱的反应。
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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。
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