您的位置: 首页 > 农业专利 > 详情页

New polymorph and new path to synthesize tafamidis
专利权人:
AZAD Pharmaceutical Ingredients AG
发明人:
申请号:
GB201804005
公开号:
GB201804005D0
申请日:
2018.03.13
申请国别(地区):
GB
年份:
2018
代理人:
摘要:
A process for the production of 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid (2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol F (Tafemidis meglumine) comprising the step of cyclization of 4-(3,5-dichlorobenzamido)-3-hydroxybenzoic acid D in the presence of acetic acid and a sulfonic acd to yield the Tafamidis acetic acid adduct E followed by adduct exchange with N-Methyl-D-Glucamine; precipitation and drying of the precipitate to give Tafamidis meglumine. The process is preferably conducted in glacial acetic acid, and the sulfonic acid is preferably p-toluenesulfonic acid. The temperature of the process is preferably below 125°C. The process preferably comprises the additional step of contacting the obtained Tafamidis meglumine with an aprotic solvent with successive removal of the solvent to yield crystalline Tafamidis meglumine. A crystalline form of Tafamidis meglumine is also disclosed characterized by powder X-ray diffraction peaks at 12.2, 23.0 and 25.5 (2θ ± 0.2; which may further comprise peaks at 5.5, 17.2 and 24.7. Pharmaceutical compositions comprising the crystalline form are disclosed, and their use in the treatment of familial amyloid polyneuropathy (FAP), familial transthyretin (TTR) amyloidosis or transthyretin familial amyloid polyneuropathy.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
相关发明人
相关专利

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充