公开(公告)号：US06388070B1

公开(公告)日：2002-05-14

申请号：US09754302

申请日：2001-01-05

申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

IPC分类号： C07D41712

CPC分类号： C07D417/12 ,  C07D501/00 ,  Y02P20/55

摘要： The present invention provides novel thioester derivatives of thiazolyl acetic acid of the general formula (I), wherein, R1 represents H, trityl, CH3, or CRaRbCOOR3, in which Ra and Rb, independently of one another, represents hydrogen or methyl and R3 represents H or C1-C7 alkyl; and R2 represents C1-C4 alkyl or phenyl. The invention also provides a method for preparation of the thioester derivatives and reaction of the thioester derivatives with cephem carboxylic acids to produce cephalosporin antibiotic compounds having general formula (II), wherein, R1 represents H, trityl, CH3, or CRaRbCOOR3, in which Ra and Rb, independently of one another, represents hydrogen or methyl and R3 represents H or C1-C7 alkyl; R4 is CH3, —CH═CH2, CH2OCH3, CH2OCOCH3, and R5 is H or a salt or a carboxylic protecting group, comprising, acylating a compound of formula (III), wherein, R4 and R5 are defined as above, and R6 is H or trimethylsilyl; with a compound of formula (I).

摘要翻译： 本发明提供通式（I）的噻唑基乙酸的新型硫酯衍生物，其中R1表示H，三苯甲基，CH3或CRaRbCOOR3，其中Ra和Rb彼此独立地表示氢或甲基，R3表示 H或C 1 -C 7烷基; 并且R 2表示C 1 -C 4烷基或苯基。 本发明还提供了硫酯衍生物的制备方法和硫酯衍生物与头孢烯羧酸反应产生具有通式（II）的头孢菌素抗生素化合物，其中R1表示H，三苯甲基，CH3或CRaRbCOOR3，其中Ra 和R b彼此独立地表示氢或甲基，R 3表示H或C 1 -C 7烷基; R4是CH3，-CH = CH2，CH2OCH3，CH2OCOCH3，R5是H或盐或羧基保护基，其包括酰化式（III）化合物，其中R4和R5定义如上，R6是 H或三甲基甲硅烷基;与式（I）的化合物反应。

公开(公告)号：US20120165548A1

公开(公告)日：2012-06-28

申请号：US13392564

申请日：2010-09-13

申请人： Shreerang Joshi ,  Sachin Bhuta ,  Sanjay Talukdar ,  Sudhir Sawant ,  Deepak Venkataraman ,  Abhinay Pise ,  Shashikant Metkar ,  Dattatraya Chavan ,  Parven Kumar Luthra

发明人： Shreerang Joshi ,  Sachin Bhuta ,  Sanjay Talukdar ,  Sudhir Sawant ,  Deepak Venkataraman ,  Abhinay Pise ,  Shashikant Metkar ,  Dattatraya Chavan ,  Parven Kumar Luthra

IPC分类号： C07D209/08 ,  C07D317/22 ,  C07C45/81 ,  C07C47/277 ,  C07C45/80

CPC分类号： C07D209/08 ,  C07D317/22

摘要： Processes for the preparation of Silodosin and its intermediates comprising reductive amination of compound of Formula (VIII) with a compound of Formula (VII) or a compound of Formula (XV) in a suitable solvent using a reducing agent.

摘要翻译： 制备Silodosin及其中间体的方法包括使用还原剂在合适的溶剂中将式（Ⅷ）化合物与式（Ⅶ）化合物或式（ⅩⅤ）化合物还原胺化。

公开(公告)号：US08471039B2

公开(公告)日：2013-06-25

申请号：US13392564

申请日：2010-09-13

申请人： Shreerang Joshi ,  Sachin Bhuta ,  Sanjay Talukdar ,  Sudhir Sawant ,  Deepak Venkataraman ,  Abhinay Pise ,  Shashikant Metkar ,  Dattatraya Chavan ,  Parven Kumar Luthra

发明人： Shreerang Joshi ,  Sachin Bhuta ,  Sanjay Talukdar ,  Sudhir Sawant ,  Deepak Venkataraman ,  Abhinay Pise ,  Shashikant Metkar ,  Dattatraya Chavan ,  Parven Kumar Luthra

IPC分类号： C07D209/08

CPC分类号： C07D209/08 ,  C07D317/22

摘要： Processes for the preparation of Silodosin and its intermediates comprising reductive amination of compound of Formula (VIII) with a compound of Formula (VII) or a compound of Formula (XV) in a suitable solvent using a reducing agent.

摘要翻译： 制备Silodosin及其中间体的方法包括使用还原剂在合适的溶剂中将式（Ⅷ）化合物与式（Ⅶ）化合物或式（ⅩⅤ）化合物还原胺化。