公开(公告)号：US20160272642A1

公开(公告)日：2016-09-22

申请号：US15076846

申请日：2016-03-22

申请人： Glenmark Pharmacueticals Limited

发明人： Sunil Kumar Singh ,  Sachin Srivastava ,  Shekhar Bhaskar Bhirud

IPC分类号： C07D473/18 ,  C07C69/78

CPC分类号： C07D473/18 ,  C07C69/78 ,  C07D401/04 ,  C07D473/04 ,  C07D473/06

摘要： The present invention provides a process for the preparation of linagliptin, a compound of Formula I, the process comprising deprotecting a compound of Formula II wherein R1 and R2 together with the nitrogen to which they are attached form a phthalimido group, wherein the aromatic ring of the phthalimido group is substituted with one or more R3 substituents selected from the group consisting of halogen, alkyl, nitro and amino; or R1 is H and R2 is selected from the group consisting of trialkylsilyl, 2-trialkylsilylethoxycarbamates, acetyl, trihaloacetyl, 9-fluorenylmethoxycarbonyl, trityl, alkylsulfonyl, arylsulfonyl, diphenylphosphine and sulfonylethoxycarbonyl.

公开(公告)号：US09593119B2

公开(公告)日：2017-03-14

申请号：US15076846

申请日：2016-03-22

申请人： Glenmark Pharmacueticals Limited

发明人： Sunil Kumar Singh ,  Sachin Srivastava ,  Shekhar Bhaskar Bhirud

IPC分类号： C07D473/04 ,  C07D473/18 ,  C07D401/04 ,  C07D473/06 ,  C07C69/78

CPC分类号： C07D473/18 ,  C07C69/78 ,  C07D401/04 ,  C07D473/04 ,  C07D473/06

摘要： The present invention provides a process for the preparation of linagliptin, a compound of Formula I, the process comprising deprotecting a compound of Formula II wherein R1 and R2 together with the nitrogen to which they are attached form a phthalimido group, wherein the aromatic ring of the phthalimido group is substituted with one or more R3 substituents selected from the group consisting of halogen, alkyl, nitro and amino; or R1 is H and R2 is selected from the group consisting of trialkylsilyl, 2-trialkylsilylethoxycarbamates, acetyl, trihaloacetyl, 9-fluorenylmethoxycarbonyl, trityl, alkylsulfonyl, arylsulfonyl, diphenylphosphine and sulfonylethoxycarbonyl.

摘要翻译： 本发明提供制备式I的利格列汀的方法，其包括使式II化合物脱保护，其中R 1和R 2与它们所连接的氮一起形成苯二甲酰亚氨基，其中苯二酰亚氨基的芳环被一个 或更多选自卤素，烷基，硝基和氨基的R3取代基; 或R 1为H且R 2选自三烷基甲硅烷基，2-三烷基硅烷基乙氧基氨基甲酸酯，乙酰基，三卤代乙酰基，9-芴基甲氧基羰基，三苯甲基，烷基磺酰基，芳基磺酰基，二苯基膦和磺酰基乙氧基羰基。