52321-06-9Relevant articles and documents
Streamlined Synthesis of a Bicyclic Amine Moiety Using an Enzymatic Amidation and Identification of a Novel Solid Form
Brown, Maria S.,Caporello, Michaella A.,Goetz, Adam E.,Johnson, Amber M.,Jones, Kris N.,Knopf, Kevin M.,Kulkarni, Samir A.,Lee, Taegyo,Li, Bryan,Lu, Cuong V.,Magano, Javier,Puchlopek-Dermenci, Angela L. A.,Reyes, Giselle P.,Ruggeri, Sally Gut,Wei, Lulin,Weisenburger, Gerald A.,Wisdom, Richard A.,Zhang, Mengtan
, p. 1419 - 1430 (2021/06/28)
We describe a series of improvements to the synthesis of a 3,8-diazabicyclo[3.2.1]octane derivative that result in a reduced step count and higher overall efficiency compared to previously published syntheses. Our method includes optimization and mechanistic understanding of a key diastereoselective cyclization to achieve a >95:5 diastereomeric ratio, as well as demonstration of a unique enzyme-catalyzed amidation reaction using hexamethyldisilazane as both an ammonia source and scavenger. Finally, we identify a novel cocrystal solid form of the target compound that provides improved purity and material properties. Demonstration of the new chemistry to prepare >100 kg of the target compound serves to illustrate the robustness of the new process.
INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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Paragraph 00478, (2019/08/29)
The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
Pyruvate kinase activators for use in therapy
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Page/Page column 177-178, (2016/08/29)
Described herein are methods for using compounds that activate pyruvate kinase.