公开(公告)号：US10556871B1

公开(公告)日：2020-02-11

申请号：US16243091

申请日：2019-01-09

申请人： ZHEJIANG XIANFENG TECHNOLOGIES CO.,LTD

发明人： Feifei Gao ,  Junlong Gao ,  Minliang Zhu ,  Wei Lu ,  Yi Liu

IPC分类号： C07D239/30 ,  B01J21/06 ,  B01J27/053 ,  B01J21/08 ,  B01J23/745

摘要： A method for preparing 5-(4-bromophenyl)-4,6-dichloropyrimidine is provided. The method comprises the steps of: preparing methyl p-bromophenylacetate (Intermediate I) by catalytic esterification of p-bromophenylacetic acid, and then reacting with dimethyl carbonate to synthesize 2-(4-bromophenyl)-malonic acid-1,3-dimethyl ester (Intermediate 2), cyclizing with formamidine hydrochloride to obtain 5-(4-bromophenyl)-4,6-dihydroxypyrimidine (Intermediate 3), and then chlorinating to give the product 5-(4-bromophenyl)-4,6-dichloropyrimidine. In the process of preparing Intermediate 1 in the present invention, a solid acid is used as a catalyst. Moreover, in the process of preparing Intermediate 2, sodium methoxide is used as a base in place of sodium hydride or sodium amide used in the prior art. Furthermore, Intermediate 3 is prepared by a one-pot process.

公开(公告)号：US20200048206A1

公开(公告)日：2020-02-13

申请号：US16243091

申请日：2019-01-09

申请人： ZHEJIANG XIANFENG TECHNOLOGIES CO.,LTD

发明人： Feifei GAO ,  Junlong GAO ,  Minliang ZHU ,  Wei LU ,  Yi LIU

IPC分类号： C07D239/30 ,  B01J21/06 ,  B01J23/745 ,  B01J21/08 ,  B01J27/053

摘要： A method for preparing 5-(4-bromophenyl)-4,6-dichloropyrimidine is provided. The method comprises the steps of: preparing methyl p-bromophenylacetate (Intermediate I) by catalytic esterification of p-bromophenylacetic acid, and then reacting with dimethyl carbonate to synthesize 2-(4-bromophenyl)-malonic acid-1,3-dimethyl ester (Intermediate 2), cyclizing with formamidine hydrochloride to obtain 5-(4-bromophenyl)-4,6-dihydroxypyrimidine (Intermediate 3), and then chlorinating to give the product 5-(4-bromophenyl)-4,6-dichloropyrimidine. In the process of preparing Intermediate 1 in the present invention, a solid acid is used as a catalyst. Moreover, in the process of preparing Intermediate 2, sodium methoxide is used as a base in place of sodium hydride or sodium amide used in the prior art. Furthermore, Intermediate 3 is prepared by a one-pot process.