- 专利标题: Process for the synthesis of substituted chloromethyl dialkylphosphates
-
申请号: US17699522申请日: 2022-03-21
-
公开(公告)号: US12071421B2公开(公告)日: 2024-08-27
- 发明人: Luca Fadini , Peter Manini , Claudio Pietra , Claudio Giuliano , Emanuela Lovati , Roberta Cannella , Alessio Venturini , Valentino J. Stella
- 申请人: HELSINN HEALTHCARE SA
- 申请人地址: CH Lugano/Pazzallo
- 专利权人: Helsinn Healthcare SA
- 当前专利权人: Helsinn Healthcare SA
- 当前专利权人地址: CH Lugano/Pazzallo
- 代理商 Clark G. Sullivan
- 主分类号: C07D401/04
- IPC分类号: C07D401/04 ; A61K9/00 ; A61K31/4178 ; A61K31/439 ; A61K31/44 ; A61K31/473 ; A61K31/496 ; A61K31/56 ; A61K31/573 ; A61K31/675 ; A61K45/06 ; A61P1/08 ; A61P13/10 ; A61P25/22 ; A61P25/24 ; C07D213/74 ; C07D213/76 ; C07D213/89 ; C07F9/02 ; C07F9/6509
摘要:
Disclosed are compounds including phosphate and N-oxide prodrugs of the NK1 antagonist netupitant, useful in the prevention and/or treatment of diseases including emesis induced by chemotherapy. Also disclosed are methods of making a di-tert-butyl (chloromethyl) phosphate useful in the manufacture of such prodrugs by reacting a dialkylphosphate salt with an acid to obtain the corresponding ester of phosphoric acid, reacting the ester with a quaternary ammonium hydroxide base to form a monobasic salt, and reacting the monobasic salt with chloroiodomethane to form the corresponding chloromethyl dialkyl phosphate.
公开/授权文献
- US20220401463A1 SUBSTITUTED 4-PHENYL-PYRIDINES 公开/授权日:2022-12-22
信息查询