1204589-80-9Relevant academic research and scientific papers
A new type of L-Tertiary leucine-derived ligand: Synthesis and application in Cu(II)-catalyzed asymmetric Henry reactions
Cai, Zedong,Lan, Ting,Ma, Pengfei,Zhang, Jingfang,Yang, Qingqing,He, Wei
, (2019/08/08)
A new series of Schiff bases derived from amino acids were developed as chiral ligands for Cu(II)-catalyzed asymmetric Henry reactions. The optimum ligand 7d exhibited outstanding catalytic efficiency in the Cu(II)-catalyzed asymmetric Henry additions of four nitroalkanes to different kinds of aldehydes to produce 76 desired adducts in high yields (up to 96%) with excellent enantioselectivities, up to 99% enantiomeric excess (ee).
Synthesis and antimalarial activity of new 4-aminoquinolines active against drug resistant strains
Kondaparla, Srinivasarao,Soni, Awakash,Manhas, Ashan,Srivastava, Kumkum,Puri, Sunil K.,Katti
, p. 105676 - 105689 (2016/11/18)
In the present study we have synthesized a new class of 4-aminoquinoline derivatives via replacement of the diethylamine functionality of chloroquine (CQ) with acyclic and/or cyclic amine groups containing basic tertiary terminal nitrogen and bioevaluated them for antimalarial activity against Plasmodium falciparum in vitro (CQ-sensitive strain-3D7 & CQ-resistant strain-K1) and Plasmodium yoelii in vivo (N-67 strain). Among the series, thirteen compounds showed superior antimalarial activity against K1 strain as compared to CQ. In addition, all these analogs showed 100% suppression of parasitaemia on day 4 in the in vivo mouse model against N-67 strain when administered orally. Further, biophysical studies suggest that these compounds act on the heme polymerization target.
Chiral primary amine catalyzed asymmetric direct cross-aldol reaction of acetaldehyde
Hu, Shenshen,Zhang, Long,Li, Jiuyuan,Luo, Sanzhong,Cheng, Jin-Pei
, p. 3347 - 3352 (2011/08/03)
The first primary aminocatalytic direct cross-aldol reaction of acetaldehyde is presented. Among the various vicinal diamines screened, the L-tert-leucine derivative 1c in conjunction with (H4SiW 12O40)0.25 was identified as the optimal catalyst; good catalytic activity (up to 99% yield in 4 h), and high enantioselectivities (up to 92% ee) were achieved for a range of donors, including aromatic aldehydes and isatin derivatives. Aqueous acetaldehyde solution and paraldehyde can be conveniently applied in this system.
Highly enantio- and diastereoselective synthesis of α- trifluoromethyldihydropyrans using a novel bifunctional piperazine-thiourea catalyst
Li, Peng,Chai, Zhuo,Zhao, Sheng-Li,Yang, Ying-Quan,Wang, Hai-Feng,Zheng, Chang-Wu,Cai, Yue-Peng,Zhao, Gang,Zhu, Shi-Zheng
supporting information; experimental part, p. 7369 - 7371 (2010/06/14)
The first enantioselective Michael addition of α-cyanoketones to α,β-unsaturated trifluoromethyl ketones using a novel piperazine-thiourea catalyst was described. The resulting α- trifluoromethyldihydropyrans were obtained in high yields and with up to 95
