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公开(公告)号：US20170305860A1
公开(公告)日：2017-10-26
申请号：US15515863
申请日：2016-02-23
IPC分类号： C07D223/26
CPC分类号： C07D223/26 , B01J2231/643 , B01J2540/32 , C07D223/28
摘要： An improved process for the preparation of Elsicarbazepine and Eslicarbazepine acetate by means of chiral Ruthenium catalysts is provided.
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公开(公告)号：US09670169B2
公开(公告)日：2017-06-06
申请号：US15116332
申请日：2015-05-07
IPC分类号： C07D265/18
CPC分类号： C07D265/18
摘要： An improved process for the preparation of Efavirenz which avoids the distillations of the solvents is provided.
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公开(公告)号：US09624221B2
公开(公告)日：2017-04-18
申请号：US15213668
申请日：2016-07-19
发明人： Elena Brasola , Filippo Tomasi
IPC分类号： C07D401/14 , C07D471/04 , G01N30/86 , G01N30/02
CPC分类号： C07D471/04 , G01N30/8631 , G01N2030/027
摘要： Object of the present invention is an improved process for the preparation of Apixaban, through new intermediates which undergo to a faster amidation reaction. Impurities of Apixaban are also identified and quantified.
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54.发明申请公开(公告)号：US20170029863A1
公开(公告)日：2017-02-02
申请号：US15206582
申请日：2016-07-11
发明人： Alfredo Paio , Stefano Fogal , Riccardo Motterle
CPC分类号： C12P33/005 , C07J9/00 , C12N9/20 , C12P33/18 , C12Y301/01003
摘要： The present invention relates to a new process for the preparation of testosterone by means of enzymatic hydrolysis of testosterone esters.
摘要翻译： 本发明涉及通过睾酮酯的酶水解制备睾酮的新方法。
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公开(公告)号：US20160347705A1
公开(公告)日：2016-12-01
申请号：US15115133
申请日：2015-10-26
IPC分类号： C07C217/54 , C07C213/08 , C07C53/10 , C07C59/265
CPC分类号： C07C217/54 , C07B2200/13 , C07C51/412 , C07C53/10 , C07C59/265 , C07C213/08 , C07C217/18
摘要： The present invention refers to new solid forms of Enclomiphene citrate and Enclomiphene base, processes for preparing thereof and uses.
摘要翻译： 本发明涉及新型固体形式的枸橼酸塞米芬和内罗米芬碱，其制备方法及用途。
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56.发明授权公开(公告)号：US09359333B2
公开(公告)日：2016-06-07
申请号：US14804828
申请日：2015-07-21
发明人： Francesco Fontana , Alfredo Paio
IPC分类号： C07D405/14 , C07D405/04 , C07C309/30
CPC分类号： C07D405/04 , C07C309/30 , C07D405/14
摘要： The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof.In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
摘要翻译： 本发明涉及合成活性药物成分拉帕替尼及其盐的新的有效方法。 特别地，本合成使用新的中间体进行，其中胺官能团由可在基本环境中切割的基团保护，其提供更高的合成过程的总产率。
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公开(公告)号：US09315470B2
公开(公告)日：2016-04-19
申请号：US14395703
申请日：2014-02-11
发明人： Ottorino De Lucchi , Stefano Tartaggia , Clark Ferrari , Marco Galvagni , Marta Pontini , Stefano Fogal , Riccardo Motterle , Rosa Maria Moreno , Alex Comely
IPC分类号： C07D239/42 , C07F7/18 , C07D317/30 , C07D215/14 , C07D209/24 , C07D413/12 , C07D419/12
CPC分类号： C07F7/1804 , B01J27/13 , B01J31/122 , B01J2231/543 , C07D209/12 , C07D209/24 , C07D213/30 , C07D215/14 , C07D239/42 , C07D317/30 , C07D413/12 , C07D419/12 , C07F7/188 , C07F7/1892
摘要： Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of statins.
摘要翻译： 本发明的目的是制备用于合成他汀类药物的关键中间体的改进方法。
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58.发明授权公开(公告)号：US09169236B2
公开(公告)日：2015-10-27
申请号：US14624997
申请日：2015-02-18
发明人： Francesco Fontana , Alfredo Paio
IPC分类号： C07D405/04 , C07D405/14
CPC分类号： C07D405/04 , C07C309/30 , C07D405/14
摘要： The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
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59.发明申请公开(公告)号：US20150299164A1
公开(公告)日：2015-10-22
申请号：US14619542
申请日：2015-02-11
发明人： Ennio GRENDELE , Alberto SOLDÀ
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The invention relates to an improved process for the preparation of Imatinib and salts thereof, in particular Imatinib Mesylate, having a content of a particular genotoxic impurity, named impurity F, within the pharmacopeia limits.
摘要翻译： 本发明涉及在药典限度内制备伊马替尼及其盐，特别是伊马替尼甲磺酸盐的改进方法，其具有特定基因毒性杂质（称为杂质F）的含量。
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公开(公告)号：US20130165650A1
公开(公告)日：2013-06-27
申请号：US13777817
申请日：2013-02-26
发明人： Alessandro Leganza , Marco Galvagni
IPC分类号： C07D265/18 , C07C215/70
CPC分类号： C07D265/18
摘要： A process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I): comprising reacting the intermediate of formula (II): as a free base or a salt thereof, with diphosgene (TCMCF, trichloromethylchloroformate) Cl3CO—COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralize the reaction mixture or in an up to 30% molar excess of such amount.
摘要翻译： 制备式（I）的依法韦伦，（4S）-6-氯-4-（环丙基乙炔基）-4-（三氟甲基）-1,4-二氢-2H-3,1-苯并恶嗪-2-酮的方法 ）：包括使式（II）的中间体：游离碱或其盐与有机溶剂中的双光气（TCMCF，氯甲酸三氯甲酯）Cl 3 CO-COCl反应或由有机溶剂和水组成的双相介质中，优选但不限于 在弱碱存在下，强度不足以中和反应混合物或以高达30％摩尔过量的量存在。
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