-
公开(公告)号：US06982335B2
公开(公告)日：2006-01-03
申请号：US10439263
申请日：2003-05-15
IPC分类号： C07D277/56
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： A useful and efficient method of preparing an alkylated thiazoline carboxylic acid, or a derivative thereof, comprises coupling a substituted aryl nitrile such as, for example, 2,4-dimethoxybenzonitrile or 4-methoxybenzonitrile, with a cysteine ester to form a substituted thiazoline carboxylic acid ester; optionally hydrolyzing the substituted thiazoline carboxylic acid ester to form a substituted thiazoline carboxylic acid; optionally, protecting the carboxyl group; alkylating the thiazoline ring at the 4-carbon position, as indicated in Structural Formula (I), with a compound of the formula R1-L, wherein R1 is as defined above and L is a leaving group, in the presence of a phase transfer catalyst; and, optionally, deprotecting the carboxyl group.In one embodiment of the present invention, a cinchona-alkaloid derived phase transfer catalyst is used to alkylate a protected substituted thiazoline carboxylic acid.
摘要翻译： 制备烷基化噻唑啉羧酸或其衍生物的有效和有效的方法包括将取代的芳基腈例如2,4-二甲氧基苄腈或4-甲氧基苄腈与半胱氨酸酯偶合以形成取代的噻唑啉羧酸 酸酯; 任选地水解取代的噻唑啉羧酸酯以形成取代的噻唑啉羧酸; 任选地，保护羧基; 如结构式（I）所示，在4-碳位置上使噻唑啉环与式R 1 -L的化合物烷基化，其中R 1为 在相转移催化剂存在下，L是离去基团; 并任选地使羧基脱保护。 在本发明的一个实施方案中，使用致cin生物碱衍生的相转移催化剂烷基化受保护的取代噻唑啉羧酸。
-
公开(公告)号：US07285670B2
公开(公告)日：2007-10-23
申请号：US11242640
申请日：2005-10-03
IPC分类号： C07D277/14
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： A useful and efficient method of preparing an alkylated thiazoline carboxylic acid, or a derivative thereof, comprises coupling a substituted aryl nitrile such as, for example, 2,4-dimethoxybenzonitrile or 4-methoxybenzonitrile, with a cysteine ester to form a substituted thiazoline carboxylic acid ester; optionally hydrolyzing the substituted thiazoline carboxylic acid ester to form a substituted thiazoline carboxylic acid; optionally, protecting the carboxyl group; alkylating the thiazoline ring at the 4-carbon position, as indicated in Structural Formula (I), with a compound of the formula R1-L, wherein R1 is as defined above and L is a leaving group, in the presence of a phase transfer catalyst; and, optionally, deprotecting the carboxyl group.In one embodiment of the present invention, a cinchona-alkaloid derived phase transfer catalyst is used to alkylate a protected substituted thiazoline carboxylic acid.
摘要翻译： 制备烷基化噻唑啉羧酸或其衍生物的有效和有效的方法包括将取代的芳基腈例如2,4-二甲氧基苄腈或4-甲氧基苄腈与半胱氨酸酯偶合以形成取代的噻唑啉羧酸 酸酯; 任选地水解取代的噻唑啉羧酸酯以形成取代的噻唑啉羧酸; 任选地，保护羧基; 如结构式（I）所示，在4-碳位置上使噻唑啉环与式R 1 -L的化合物烷基化，其中R 1为 在相转移催化剂存在下，L是离去基团; 并任选地使羧基脱保护。 在本发明的一个实施方案中，使用致cin生物碱衍生的相转移催化剂烷基化受保护的取代噻唑啉羧酸。
-
公开(公告)号：US20060217561A1
公开(公告)日：2006-09-28
申请号：US11242640
申请日：2005-10-03
IPC分类号： C07D277/14
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： A useful and efficient method of preparing an alkylated thiazoline carboxylic acid, or a derivative thereof, comprises coupling a substituted aryl nitrile such as, for example, 2,4-dimethoxybenzonitrile or 4-methoxybenzonitrile, with a cysteine ester to form a substituted thiazoline carboxylic acid ester; optionally hydrolyzing the substituted thiazoline carboxylic acid ester to form a substituted thiazoline carboxylic acid; optionally, protecting the carboxyl group; alkylating the thiazoline ring at the 4-carbon position, as indicated in Structural Formula (I), with a compound of the formula R1-L, wherein R1 is as defined above and L is a leaving group, in the presence of a phase transfer catalyst; and, optionally, deprotecting the carboxyl group. In one embodiment of the present invention, a cinchona-alkaloid derived phase transfer catalyst is used to alkylate a protected substituted thiazoline carboxylic acid.
-
-
搜索结果
3 条记录 (耗时 0.02 秒)
