A Chiron Approach to the Practical and Scalable Synthesis of the β₃‐Adrenergic Receptor Agonist Vibegron
Sign Up to like & getrecommendations! Published in 2025 at "European Journal of Organic Chemistry"
DOI: 10.1002/ejoc.202500469
Abstract: A practical and scalable synthesis of the β3‐adrenergic receptor agonist Vibegron has been developed using a streamlined chiral‐pool approach from readily available 4‐nitro‐D‐phenylalanine and (R)‐mandelic acid. The synthesis features a key acid‐catalyzed N‐acyl iminium ion… read more here.
Keywords: synthesis adrenergic; receptor agonist; synthesis; adrenergic receptor ... See more keywords
Mechanistic Insight Enables Practical, Scalable, Room Temperature Chan–Lam N-Arylation of N-Aryl Sulfonamides
Sign Up to like & getrecommendations! Published in 2018 at "ACS Catalysis"
DOI: 10.1021/acscatal.8b03238
Abstract: Sulfonamides are profoundly important in pharmaceutical design. C–N cross-coupling of sulfonamides is an effective method for fragment coupling and structure–activity relationship (SAR) mining. However, cross-coupling of the important N-arylsulfonamide pharmacophore has been notably unsuccessful. Here,… read more here.
Keywords: mechanistic insight; room temperature; chan; lam arylation ... See more keywords
An Improved, Practical, and Scalable Five-Step Synthesis of Psilocybin
Sign Up to like & getrecommendations! Published in 2020 at "Synthesis"
DOI: 10.1055/s-0039-1691565
Abstract: Described herein is an improved synthesis of 3-[2-(dimethylamino)ethyl]-1H-indol-4-yl dihydrogen phosphate (psilocybin). The protocol outlines: synthesis of multigram quantities of psilocybin, identification of critical in-process parameters, and isolation of psilocybin without the use of chromatography, TLC,… read more here.
Keywords: five step; scalable five; psilocybin; practical scalable ... See more keywords
A practical and scalable synthesis of KRN7000 using glycosyl iodide as the glycosyl donor
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Chemical Research"
DOI: 10.1177/1747519820961018
Abstract: KRN7000 is particularly useful because it is a powerful and specific CD1d agonist and has prompted intense interest in the context of immunology in the past 25 years. Its limited commercial availability and high price has… read more here.
Keywords: synthesis krn7000; glycosyl iodide; practical scalable; scalable synthesis ... See more keywords