Route scouting and optimization of a potent sulfoximine-based inverse agonist of ROR gamma t

摘要

During our research looking for novel inverse agonists of ROR gamma t, we identified a potent sulfoximine-based modulator as one of our pre-clinical candidates for the topical treatment for psoriasis. Herein, we describe the various routes we evaluated during the lead generation and optimization phases and the final route chosen for scale-up to deliver the first 100 g of API. (C) 2018 Elsevier Ltd. All rights reserved.