- Process Design and Optimization in the Pharmaceutical Industry: A Suzuki-Miyaura Procedure for the Synthesis of Savolitinib
-
A multidisciplinary approach covering synthetic, physical, and analytical chemistry, high-throughput experimentation and experimental design, process engineering, and solid-state chemistry is used to develop a large-scale (kilomole) Suzuki-Miyaura process. Working against clear criteria and targets, a full process investigation and optimization package is described highlighting how and why key decisions are made in the development of large-scale pharmaceutical processes.
- Adlington, Neil K.,Agnew, Lauren R.,Campbell, Andrew D.,Cox, Robert J.,Dobson, Andrew,Barrat, Cristina Fernandez,Gall, Malcolm A. Y.,Hicks, William,Howell, Gareth P.,Jawor-Baczynska, Anna,Miller-Potucka, Lucie,Pilling, Michael,Shepherd, Katy,Tassone, Ross,Taylor, Brian A.,Williams, Aled
-
-
Read Online
- PROCESS FOR PREPARATION OF SAVOLITINIB AND ITS INTERMEDIATES
-
The present application relates to a process for preparation of chiral amine fragment (IV) of savolitinib. The present application also relates to a process for preparation of savolitinib using the chiral amine (IV), as prepared by the process of the present application. The present application also discloses new intermediates useful for the synthesis of savolitinib. The present application further relates to crystalline forms of savolitinib, namely AA1, formic acid solvate and AA2. The present application also relates to amorphous solid dispersion of savolitinib.
- -
-
Page/Page column 38
(2021/11/20)
-
- IMPROVED METHOD FOR THE MANUFACTURE OF 3-[(1S)-1-IMIDAZO[1,2-A]PYRIDIN-6-YLETHYL]-5-(1-METHYLPYRAZOL-4-YL)TRIAZOLO[4,5-B]PYRAZINE AND POLYMORPHIC FORMS THEREOF
-
This specification generally relates to an improved method for the manufacture of 3-[(lS)-l -imidazo[ 1,2-a]pyridin-6-ylethyl]-5-(l-methylpyrazol-4-yl)triazolo[4,5- bjpyrazine (I), or pharmaceutically acceptable salts thereof; polymorphic forms thereof; and intermediates useful in the manufacture of such compounds and salts thereof. Formula (I).
- -
-
-
- Discovery of (S)-1-(1-(Imidazo[1,2- a ]pyridin-6-yl)ethyl)-6-(1-methyl-1 H -pyrazol-4-yl)-1 H -[1,2,3]triazolo[4,5- b ]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal-Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer
-
HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure-activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.
- Jia, Hong,Dai, Guangxiu,Weng, Jianyang,Zhang, Zhulin,Wang, Qing,Zhou, Feng,Jiao, Longxian,Cui, Yumin,Ren, Yongxin,Fan, Shiming,Zhou, Jinghong,Qing, Weiguo,Gu, Yi,Wang, Jian,Sai, Yang,Su, Weiguo
-
p. 7577 - 7589
(2014/12/11)
-
- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
-
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
- -
-
Page/Page column 100-101
(2012/10/08)
-
