10199-50-5Relevant articles and documents
Design and Synthesis of Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors
Huang, David S.,Leblanc, Emmanuelle V.,Shekhar-Guturja, Tanvi,Robbins, Nicole,Krysan, Damian J.,Pizarro, Juan,Whitesell, Luke,Cowen, Leah E.,Brown, Lauren E.
, p. 2139 - 2180 (2019/10/11)
The molecular chaperone Hsp90, essential in all eukaryotes, plays a multifaceted role in promoting survival, virulence, and drug resistance across diverse pathogenic fungal species. The chaperone is also critically important, however, to the pathogen's hu
Difluoromethylthiolation of Phenols and Related Compounds with a HF2CSO2Na/Ph2PCl/Me3SiCl System
Huang, Zhongyan,Matsubara, Okiya,Jia, Shichong,Tokunaga, Etsuko,Shibata, Norio
supporting information, p. 934 - 937 (2017/02/26)
A novel HF2CSO2Na/Ph2PCl/Me3SiCl system is disclosed for the late-stage direct difluoromethylthiolation of Csp2 and Csp3 nucleophiles. Difluoromethylthiolation of phenols and naphthols proceeded nicely under this system to regioselectively provide corresponding SCF2H compounds in good yields. Other substrates such as indoles, pyrroles, pyrazoles, enamines, ketones, and β-keto esters were also transformed to corresponding SCF2H products in good yields. The late-stage direct difluoromethylthiolation of a number of natural products and pharmaceutically attractive molecules was also achieved.
Direct synthesis of pyrazoles from esters using tert-butoxide-assisted C-(C=O) coupling
Kim, Bo Ram,Sung, Gi Hyeon,Ryu, Ki Eun,Lee, Sang-Gyeong,Yoon, Hyo Jae,Shin, Dong-Soo,Yoon, Yong-Jin
supporting information, p. 9201 - 9204 (2015/06/08)
This paper describes the direct synthesis of pyrazoles from esters that comprises two sequential reactions: tert-butoxide-assisted C-C(=O) coupling reaction to yield β-ketonitrile or α,β-alkynone intermediates, and condensation by hydrazine addition. The method reported allows for easy control of the regioselectivity and structure of substituents at N-1, C-3, C-4 and/or C-5 positions.
