Results 21 to 30 of about 175,047 (318)

Picomolar inhibitor of reverse transcriptase featuring significantly improved metabolic stability

Acta Pharmaceutica Sinica B, 2023
Considering the undesirable metabolic stability of our recently identified NNRTI 5 (t1/2 = 96 min) in human liver microsomes, we directed our efforts to improve its metabolic stability by introducing a new favorable hydroxymethyl side chain to the C-5 ...
Ya-Li Sang, Christophe Pannecouque, Erik De Clercq, Shuai Wang, Fen-Er Chen   +4 more
doaj   +1 more source

Collective Asymmetric Total Synthesis of Cylindricines

, 2023
Collective asymmetric total synthesis of marine tricyclic alkaloids, cylindricines A–H, and the proposed structures of cylindricine I and J, was achieved in a concise manner from a single common spirocyclic pyrrolidine intermediate.
Haruhiko, Fuwa, Ryohei, Hanzawa
core   +1 more source

Structure-based design of novel heterocycle-substituted ATDP analogs as non-nucleoside reverse transcriptase inhibitors with improved selectivity and solubility

Acta Pharmaceutica Sinica B, 2023
Following on our recently developed biphenyl-ATDP non-nucleoside reverse transcriptase inhibitor ZLM-66 (SI = 2019.80, S = 1.9 μg/mL), a series of novel heterocycle-substituted ATDP derivatives with significantly improved selectivity and solubility were ...
Li-Min Zhao, Christophe Pannecouque, Erik De Clercq, Shuai Wang, Fen-Er Chen   +4 more
doaj   +1 more source

Asymmetric Total Synthesis of Pseurotin A [PDF]

Organic Letters, 2003
The asymmetric total syntheses of pseurotin A and 8-O-demethylpseurotin A have been accomplished. Key reactions are a NaH-promoted intramolecular cyclization of an alkynylamide to form a gamma-lactam, an aldol reaction of a benzylidene-substituted ketone, and the late-stage introduction of the benzoyl group by a selective oxidation of a benzylidene ...
Yujiro, Hayashi, Mitsuru, Shoji, Shinpei, Yamaguchi, Takasuke, Mukaiyama, Junichiro, Yamaguchi, Hideaki, Kakeya, Hiroyuki, Osada   +6 more
openaire   +2 more sources

Synthesis of Solution-Phase Phosphoramidite and Phosphite Ligand Libraries and Their In Situ Screening in the Rhodium-Catalyzed Asymmetric Addition of Arylboronic Acids [PDF]

, 2007
Herein, we report the automated parallel synthesis of solution-phase libraries of phosphoramidite ligands for the development of enantioselective catalysts.
Toullec, Patrick Y.,, Jagt, Richard B. C., Minnaard, Adriaan J.,, Minnaard, Adriaan J., Vries, Johannes G. de,, Feringa, Ben L., Jagt, Richard B.C.,, Toullec, Patrick Y., de Vries, Johannes G., Feringa, Ben L.,, Schudde, Ebe P., Minnaard, Adriaan J.; id_orcid, Schudde, Ebe P.,   +12 more
core   +1 more source

Untethering sparteine: 1,3-diamine ligand for asymmetric synthesis in water

, 2021
Chiral ligands are the toolbox for asymmetric synthesis to access 3D molecular world. Enabling efficient asymmetric reaction in water is a big challenge. As moisture/air stable and strong binding moieties, amines, compared to imine and phosphine ligands,
Chen, Chen, Shihao, Huang, Yuting, Yan, Liu, Liu, Guotao, Lin, Yanfeng, Dang, Jianhui, Huang, Fanyun , Zeng, Yuan, Zhang, Mingyu, Zhang, Yifan, Li, Bo, Li   +11 more
core   +1 more source

Chemical asymmetric synthesis

Nature, 1989
Thalidomide comes in two forms: a left-handed compound which is a powerful tranquilizer, and a right-handed version which can disrupt fetal development causing severe handicap. As a necessary consequence of synthetic methods available in the early 1960s the two forms were present in equal proportions in the manufactured drug, with catastrophic ...
Brown, J, Davies, S
openaire   +2 more sources

Optimized Asymmetric Synthesis of Umuravumbolide

ACS Omega, 2022
Herein, the asymmetric synthesis of umuravumbolide (1) is described. The new approach features highly stereoselective transformations (dr ≥ 95:5) to install both stereocenters and the Z olefin, which involve a new radical alkylation, an Ando olefination, and a Krische allylation on a Z allylic alcohol, not reported before.
Marina Pérez-Palau, Eduard Balaguer-Garcia, Pedro Romea, Fèlix Urpí   +3 more
openaire   +3 more sources

Improving the positional adaptability: structure-based design of biphenyl-substituted diaryltriazines as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

Acta Pharmaceutica Sinica B, 2020
In order to improve the positional adaptability of our previously reported naphthyl diaryltriazines (NP-DATAs), synthesis of a series of novel biphenyl-substituted diaryltriazines (BP-DATAs) with a flexible side chain attached at the C-6 position is ...
Kaijun Jin, Minjie Liu, Chunlin Zhuang, Erik De Clercq, Christophe Pannecouque, Ge Meng, Fener Chen   +6 more
doaj   +1 more source

Chiral Syn-1,3-diol Derivatives via a One-Pot Diastereoselective Carboxylation/ Bromocyclization of Homoallylic Alcohols

iScience, 2018
Summary: Chiral syn-1,3-diols are fundamental structural motifs in many natural products and drugs. The traditional Narasaka-Prasad diastereoselective reduction from chiral β-hydroxyketones is an important process for the synthesis of these ...
Guanxin Huang, Minjie Liu, Fangjun Xiong, Ge Meng, Yuan Tao, Yan Wu, Haihui Peng, Fener Chen   +7 more
doaj   +1 more source