An improved process to access an aldehyde en route to a LSD1 inhibitor was developed using an aerobic alcohol oxidation with a Cu/TEMPO (2,2,6,6-tetramethylpiperdine 1-oxyl) catalyst system. In this report, kinetic information is utilized to understand the generation a of number of key byproducts that impact catalyst performance and aldehyde yield. This Cu<sup>I</sup>/TEMPO catalyst facilitates rapid conversion of the starting aliphatic alcohol in 1–2 h with apparent zero-order kinetics unprecedented for this substrate class with this catalyst. Process optimization of the reaction components led to the successful 400 g scale-up of this oxidation with bubbling air in a batch reactor.

Development of a large-scale copper(I)/TEMPO-catalyzed aerobic alcohol oxidation for the synthesis of a pharmaceutical intermediate

Fall 2022 abstracts, posters, and presentations will launch in mid-September.

ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.