An Efficient Substrate-Induced Method for the Synthesis of CF3 -Substituted Cyclopropanes by Metal-Free Reaction of Trifluoromethyl Styrylisoxazoles with Nitromethane.

Autor: Zhao, Qing-he, Yu, Guang-hao, Meng, Ye-chen, Sui, Feng, Yang, Mi-yi, Liu, Li, Li, Hui-jie, Li, Feng, Ma, Hai
Předmět:
Zdroj: Synthesis; 2021, Vol. 53 Issue 9, p1597-1604, 8p
Abstrakt: A series of (trifluoromethyl)cyclopropanes (TFCPs) tolerating a broad range of functional groups, known as tert -butyl bioisosteres, have been obtained from the cyclization reaction between nitromethane- and 5-[β-(trifluoromethyl)styryl]isoxazoles in 70–94% yields and 75:25 to 90:10 dr. This method offers practical access to this cyclopropyl moiety of pharmacological interest, employing an inorganic base under phase-transfer conditions. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index