Synthesis, Optimization, and Large-Scale Preparation of the Low-Dose Central Nervous System-Penetrant BACE1 Inhibitor LY3202626 via a [3 + 2] Nitrone Cycloaddition

Autor:	Hao Sun, Michael O. Frederick, Roger Ryan Rothhaar, Amy C. DeBaillie, Brian Morgan Watson, Carlos Mateos, Leonard L. Winneroski, Carlos Jaramillo, Talbi Kaoudi, Matthew Johnson, Pablo Garcia-Losada, Srinivas Gangula, Peter J. Lindsay-Scott, Steven James Green, Dustin J. Mergott, Dajiang Jing, Marvin M. Hansen, José Eugenio de Diego, Juan A. Rincón, Kevin D. Seibert, Lei Zhang, Jiuyuan Li
Rok vydání:	2020
Předmět:	chemistry.chemical_classification 010405 organic chemistry Organic Chemistry Low dose 010402 general chemistry 01 natural sciences Combinatorial chemistry Cycloaddition 0104 chemical sciences Nitrone chemistry.chemical_compound chemistry Physical and Theoretical Chemistry Penetrant (biochemical)
Zdroj:	Organic Process Research & Development. 24:306-314
ISSN:	1520-586X 1083-6160
Popis:	Herein we report a summary of the synthetic development of LY3202626 from the initial discovery route to a final route that was scaled to make 150 kg. Key developments include the use of a [3 + 2] ...
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::bd409beaf54c99668ae6510bc63b7fdb https://doi.org/10.1021/acs.oprd.9b00471 Zobrazit plný text záznamu