416852-53-4Relevant articles and documents
Biocatalytic Strategy for the Highly Stereoselective Synthesis of CHF2-Containing Trisubstituted Cyclopropanes
Carminati, Daniela M.,Decaens, Jonathan,Couve-Bonnaire, Samuel,Jubault, Philippe,Fasan, Rudi
, p. 7072 - 7076 (2021/02/27)
The difluoromethyl (CHF2) group has attracted significant attention in drug discovery and development efforts, owing to its ability to serve as fluorinated bioisostere of methyl, hydroxyl, and thiol groups. Herein, we report an efficient biocat
Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt
Kummer, David A.,Cummings, Maxwell D.,Abad, Marta,Barbay, Joseph,Castro, Glenda,Wolin, Ronald,Kreutter, Kevin D.,Maharoof, Umar,Milligan, Cynthia,Nishimura, Rachel,Pierce, Joan,Schalk-Hihi, Celine,Spurlino, John,Urbanski, Maud,Venkatesan, Hariharan,Wang, Aihua,Woods, Craig,Xue, Xiaohua,Edwards, James P.,Fourie, Anne M.,Leonard, Kristi
, p. 2047 - 2057 (2017/04/10)
A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity relationships and structure-based drug design methods led to the discovery of a series of modulators with improved RORγt inhibitory potency and inverse agonism properties.
One-Pot Direct Synthesis of Weinreb Amides from Aryl and Hetero Aryl Halides Using Co 2(CO) 8 as an Effective CO Source under Conventional Thermal Heating
Baburajan, Poongavanam,Elango, Kuppanagounder P.
, p. 541 - 548 (2015/10/29)
A successful protocol for the synthesis of Weinreb amides directly from aryl halides via aminocarbonylation with N,O-dimethyl hydroxylamine using Co2(CO)8 as an in situ CO source has been demonstrated. The effects of various reaction parameters such as temperature, base, and CO source have also been investigated and optimized. GRAPHICAL ABSTRACT.
