877265-10-6Relevant academic research and scientific papers
A Series of Analogues to the AT2R Prototype Antagonist C38 Allow Fine Tuning of the Previously Reported Antagonist Binding Mode
Isaksson, Rebecka,Lindman, Jens,Wannberg, Johan,Sallander, Jessica,Backlund, Maria,Baraldi, Dhaniel,Widdop, Robert,Hallberg, Mathias,?qvist, Johan,Gutierrez de Teran, Hugo,Gising, Johan,Larhed, Mats
, p. 114 - 125 (2019/02/07)
We here report on our continued studies of ligands binding to the promising drug target angiotensin II type 2 receptor (AT2R). Two series of compounds were synthesized and investigated. The first series explored the effects of adding small subs
Initial process development and scale-up of the synthesis of a triple reuptake inhibitor ALB 109780
Yang, Qiang,Ulysse, Luckner G.,McLaws, Mark D.,Keefe, Daniel K.,Haney, Brian P.,Zha, Congxiang,Guzzo, Peter R.,Liu, Shuang
, p. 499 - 506 (2012/08/08)
Early process development toward a triple reuptake inhibitor is described. Three different routes were evaluated; one of them was optimized and scaled up to generate 470 g of API as this route minimized the formation of undesired side products. The select
Process development and pilot-scale synthesis of new cyclization conditions of substituted phenylacetamides to tetrahydroisoquinoline-2-ones using Eaton's reagent
Ulysse, Luckner G.,Yang, Qiang,McLaws, Mark D.,Keefe, Daniel K.,Guzzo, Peter R.,Haney, Brian P.
experimental part, p. 225 - 228 (2010/04/29)
Tetrahydroisoquinoline is a ubiquitous structural framework presented in numerous pharmacologically relevant molecules. Although accessible by the Pictet-Spengler cyclization, conditions commonly used for such cyclizations are often difficult to implement on scale. Herein, we report the development of a scaleable approach utilizing Eaton's reagent for the cyclization of substituted phenylacetamide analogues to tetrahydroisoquinoline-2-one. The development, optimization, and safety hazard evaluations, which outline the benefits and ease of workup of this new process, are discussed.
