37732-87-9Relevant academic research and scientific papers
Thermodynamic Understanding of an Aza-Michael Reaction Enables Five-Step Synthesis of the Potent Integrin Inhibitor MK-0429
Gupta, Anya,Condakes, Matthew L.
supporting information, p. 17523 - 17527 (2021/11/18)
We describe a general strategy for the aza-Michael addition of nucleophilic heterocycles into β-substituted acrylates using potassium tert-butoxide as catalyst. Demonstrating that the reaction is under thermodynamic control underpins optimization efforts and enables rapid exploration of the substrate scope, with yields ranging from 55% to 94%. We further leverage these lessons in a significantly shortened synthesis of MK-0429, a potent pan-integrin inhibitor previously taken into human clinical trials for the treatment of prostate cancer and osteoporosis.
3-(Triflyloxy)benzynes Enable the Regiocontrolled Cycloaddition of Cyclic Ureas to Synthesize 1,4-Benzodiazepine Derivatives
Kaneko, Hideki,Ikawa, Takashi,Yamamoto, Yuta,Arulmozhiraja, Sundaram,Tokiwa, Hiroaki,Akai, Shuji
supporting information, p. 943 - 948 (2018/02/26)
A versatile synthesis of 1,4-benzodiazepine derivatives through the reaction of various 3-(trifluoromethanesulfonyloxy)benzynes with N -(p -toluenesulfonyl)imidazolidin-2-ones is reported. This reaction system provides a 1,4-benzodiazepine bearing a trifluoromethanesulfonyloxy group as a single regioisomer among the four possible regioisomers.
Aryl substituted nitrogen heterocyclic antidepressants
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, (2008/06/13)
Antidepressant agents having the formula STR1 wherein R1 is a polycycloalkyl group; R2 is methyl or ethyl, X is O; and Y comprises a 5-membered heterocyclic ring having one or two nitrogens.
