17462-82-7Relevant articles and documents
Synthesis of Biuret Derivatives as Potential HIV-1 Protease Inhibitors Using (LDHs-g-HMDI-Citric Acid), as a Green Recyclable Catalyst
Ghiasifar, Zahra,Salehabadi, Hafezeh,Adibpour, Neda,Alipour, Eskandar,Kobarfard, Farzad,Shoushizadeh, Mohammad Reza
, p. 48 - 59 (2020/12/07)
In this study, a novel catalyst based on layered double hydroxides (LDHs) attached by hexamethylene-1,6-diisocyanate (HMDI) and citric acid (LDHs-g-HMDI-Citric acid) is reported and used to increase the yield of biurets synthesis. Biuret derivatives 5a–n were prepared by reaction of several phenyl allophanates (3a–d), which prepared from the reaction of phenyl chloroformate and urea derivatives (2a–d), with variously substituted amines (4a–g) in the presence of LDHs-g-HMDI-Citric acid as a reusable heterogeneous catalyst at reflux condition for 60–180 min. These biurets (5a–n) were evaluated for human immunodeficiency virus type-1 (HIV-1) protease inhibitory activity by HIV-1 p24 antigen ELISA kit and six of them (5n, 5i, 5j, 5 m, 5f, and 5a) showed moderate activity on HIV-1 virus with IC50 values ranging from 55 to 100 μM compared with the azidothymidine as the reference drug (IC50 = 0.11 μM). Results of the in vitro test and docking study were in good correlation.
Carbonyl Isocyanate Isothiocyanate
Bunnenberg, Rolf,Jochims, Johannes C.
, p. 2064 - 2074 (2007/10/02)
A synthesis of carbonyl isocyanate isothiocyanate (1) is described. 1 reacts with H2O, H2S, or HCl to give the thiadiazines 3, 6, and 14, resp.With one mol equivalent of alcohol the isothiocyanates 7 are obtained which form with further alcohol or amines compounds 8 - 10.With one mol equivalent of amine 1 gives the carbamoyl isothiocyanates 11 which form compounds 12 and 13 with further amine.Compound 1 can be chlorinated to carbonyl isocyanate isocyanide dichloride (18).Partial hydrolysis of 18 leads to carbamoyl isocyanide dichloride (19) yielding with aliphaticamines the stable carbamoyl carbodiimides 16.With alcohols 18 reacts to give the (dichloromethylene)allophanic esters 20.