Patent Review of Synthetic Routes and Crystalline Forms of the CFTR-Modulator Drugs Ivacaftor, Lumacaftor, Tezacaftor, and Elexacaftor

被引：21
作者：
Hughes, David L. [1 ]
机构：
[1] Cidara Therapeut, 6310 Nancy Ridge Dr,Suite 101, San Diego, CA 92121 USA
来源：
ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2019年 / 23卷 / 11期
关键词：
ivacaftor; lumacaftor; tezacaftor; elexacaftor; patent; synthesis; polymorph; CONTINUOUS-FLOW NITRATION; EFFICIENT SYNTHESIS; CYSTIC-FIBROSIS; SCALE-UP; N-OXIDE; C-C; IONIZATION;
D O I：
10.1021/acs.oprd.9b00326
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
This review surveys synthetic routes and polymorphic forms of the three approved CFTR-modulators ivacaftor, lumacaftor, and tezacaftor and one Phase 3 development candidate, elexacaftor. The patent literature was the source of information for synthetic routes and final forms.
引用
收藏
页码：2302 / 2322
页数：21
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