548772-42-5Relevant articles and documents
Regiospecific synthesis of 5-halo-substituted thiophene pyridyl thiourea compounds as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Venkatachalam,Uckun
, p. 2451 - 2461 (2007/10/03)
The regiospecific synthesis of 5-halothiophenethylamines and halo-substituted phenylethyl thioureas was accomplished with an overall yield of 45-60%. Condensation of t-boc protected 2-thiophenethylamine with N-halo succinamide in dimethylformamide furnished the desired halo-substituted thiophenethylamines. These thiophenethyl amines were further converted into biologically active thiourea compounds using thiocarbonyldiimidazole chemistry. Several of the halo-substituted thiophene pyridyl thiourea compounds inhibited HIV-1 reverse transcriptase (RT) at nanomolar concentrations.
Mono-chlorination of electron-rich arylalkyl- and heteroarylalkyl-amines and amino acids using sulfuryl chloride
Yu, Guixue,Mason, Helen J.,Galdi, Kim,Wu, Ximao,Cornelius, Lyndon,Zhao, Ning,Witkus, Michael,Ewing, William R.,Macor, John E.
, p. 403 - 407 (2007/10/03)
Sulfuryl chloride has been used to mono-chlorinate electron-rich arylalkyl- and heteroarylalkyl-amines and amino acids in a mild and efficient one-pot transformation with straightforward purification. Protection of the amines was not needed, and racemization of the chiral amino acids was minimal.