Synthetic Route of C11H24N2OIn 2022 ,《Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106》 appeared in Journal of Medicinal Chemistry. The author of the article were Heinrich, Timo; Peterson, Carl; Schneider, Richard; Garg, Sakshi; Schwarz, Daniel; Gunera, Jakub; Seshire, Anita; Koetzner, Lisa; Schlesiger, Sarah; Musil, Djordje; Schilke, Heike; Doerfel, Benjamin; Diehl, Patrizia; Boepple, Pia; Lemos, Ana R.; Sousa, Pedro M. F.; Freire, Filipe; Bandeiras, Tiago M.; Carswell, Emma; Pearson, Nicholas; Sirohi, Sameer; Hooker, Mollie; Trivier, Elisabeth; Broome, Rebecca; Balsiger, Alexander; Crowden, Abigail; Dillon, Christian; Wienke, Dirk. The article conveys some information:
The dysregulated Hippo pathway and, consequently, hyperactivity of the transcriptional YAP/TAZ-TEAD complexes is associated with diseases such as cancer. Prevention of YAP/TAZ-TEAD triggered gene transcription is an attractive strategy for therapeutic intervention. The deeply buried and conserved lipidation pocket (P-site) of the TEAD transcription factors is druggable. The discovery and optimization of a P-site binding fragment are described. Utilizing structure-based design, enhancement in target potency was engineered into the hit, capitalizing on the established X-ray structure of TEAD1. The efforts culminated in the optimized in vivo tool MSC-4106 (I), which exhibited desirable potency, mouse pharmacokinetic properties, and in vivo efficacy. In close correlation to compound exposure, the time- and dose-dependent downregulation of a proximal biomarker could be shown. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Synthetic Route of C11H24N2O)
tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Synthetic Route of C11H24N2O
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics