65434-72-2Relevant academic research and scientific papers
Design and synthesis of potent macrocyclic HIV-1 protease inhibitors involving P1-P2 ligands
Ghosh, Arun K.,Schiltz, Gary E.,Rusere, Linah N.,Osswald, Heather L.,Walters, D. Eric,Amano, Masayuki,Mitsuya, Hiroaki
, p. 6842 - 6854 (2014)
A series of potent macrocyclic HIV-1 protease inhibitors have been designed and synthesized. The compounds incorporated 16- to 19-membered macrocyclic rings between a nelfinavir-like P2 ligand and a tyrosine side chain containing a hydroxyethylamine sulfonamide isostere. All cyclic inhibitors are more potent than their corresponding acyclic counterparts. Saturated derivatives showed slight reduction of potency compared to the respective unsaturated derivatives. Compound 8a containing a 16-membered ring as the P1-P2 ligand showed the most potent enzyme inhibitory and antiviral activity. This journal is the Partner Organisations 2014.
New facile synthesis of furan-2(3H)-ones and 2,3,5-trisubstituted furans via intramolecular Wittig reaction of acid anhydride
Sun, Mei,Wan, Qin,Ding, Ming-Wu
supporting information, p. 3441 - 3447 (2019/05/15)
A new facile preparation of furan-2(3H)-ones and 2,3,5-trisubstituted furans by a sequential O-acylation/Wittig(/O-acylation)reaction has been developed. The easily accessible 2-(triphenylphosphoranylidene)-succinic acid 1-ester 3 reacted with acid chloride produced furan-2(3H)-ones 4 in good yields in the presence of DMAP via sequential O-acylation and intramolecular Wittig reaction of acid anhydride. Subsequently, the 2,3,5-trisubstituted furans 5 were prepared from furan-2(3H)-ones 4 and diverse aryl chlorides in presence of triethylamine through further O-acylation.
Structural and conformational analysis of 2-triphenylphosphoranylidene succinic acid derivatives by 1H, 13C and 31P one and two dimensional NMR spectroscopy and molecular modelling
Bacaloglu, Radu,Blasko, Andrei,Bunton, Clifford A.,Cerichelli, Giorgio,Castaneda, Fernando,Rivera, Enrique
, p. 965 - 972 (2007/10/02)
The structure and conformation of 2-triphenylphosphoranylidenesuccinic acid derivatives have been studied by 1H, 13C and 31P NMR spectroscopy, in various solvents and at variable temperatures.In 2-triphenylphosphoranylidenesuccinic anhydride (1) the confo
