Entry to Chiral 1,1,2,3-Tetrasubstituted Arylcyclopropanes by Pd(II)-Catalyzed Arylation via Directing Group-Mediated C(sp3)‑H Activation

• Published in: Journal of organic chemistry Vol. 82; no. 5; pp. 2535 - 2544
• Main Authors: Hoshiya, Naoyuki, Kondo, Moemi, Fukuda, Hayato, Arisawa, Mitsuhiro, Uenishi, Jun’ichi, Shuto, Satoshi
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 03.03.2017; Amer Chemical Soc
• Subjects: Chemistry; Chemistry, Organic; Physical Sciences; Science & Technology; STEREOSELECTIVE CYCLOPROPANATION; CONFORMATIONAL RESTRICTION; POTENT; CARBON; PRIVILEGED STRUCTURES; ALKYLATION; RING; PALLADIUM-CATALYZED ARYLATION; AUXILIARY; C-H BONDS

Here we report the construction of highly functionalized chiral 1,1,2,3-tetrasubstituted arylcyclopropanes of medicinal chemical importance using Pd­(II)-catalyzed arylation via directing group-mediated C­(sp3)-H activation. The key aspect for the effective arylation was control of the substrate con...