27063-56-5Relevant articles and documents
Potent inhibitory effects of N-aryl S-alkylthiocarbamate derivatives on the dopa oxidase activity of mushroom tyrosinase
Lee, Kun Ho,Koketsu, Mamoru,Choi, Sang Yoon,Lee, Kang Jin,Lee, Pyeongjae,Ishihara, Hideharu,Kim, Sun Yeou
, p. 747 - 749 (2005)
This study reports the potent inhibitory effect of N-aryl S-alkylthiocarbamate derivatives on mushroom tyrosinase (MT) activity. N-Aryl S-alkylthiocarbamate derivatives were found to exhibit a potent inhibitory effect on the dopa (3,4-dihydroxyphenylalanine) oxidase activity of mushroom tyrosinase. Most of the N-aryl S-alkylthiocarbamate derivatives (compounds from A to J) exhibited higher inhibitory effects than kojic acid (IC50=318 μm), a well known tyrosinase inhibitor. Tyrosinase was the most inhibited by S-phenetyl N-phenylthiocarbamate (compound E, IC50=7.25 μM), and this inhibition was 44 times stronger than that of kojic acid. Compound E exhibited 95.0% of inhibition at 100 μM. A kinetic study of MT inhibition by compound E using the Lineweaver-Burk plots analysis was performed. And the kinetics profiles observed suggest that compound E competitively inhibits MT.
Preparation method of amide derivative
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Paragraph 0040-0044, (2020/05/30)
The invention provides a preparation method of an amide derivative. The method comprises the following steps: taking hydroxamic acid and an amine or thiol compound as raw materials, sequentially adding alkali and a solvent, carrying out a reaction for 2-7 hours at the temperature of 25-50 DEG C in an SO2F2 atmosphere, and after the reaction is finished, carrying out aftertreatment on a reaction solution to obtain the asymmetric urea compound or thiocarbamate compound. According to the invention, cheap, easily available and environment-friendly SO2F2 is used as an accelerant to efficiently promote the generation of isocyanate intermediates and form C-N and C-S bonds. The generation of isocyanate avoids the use of a large amount of halogen or azide dangerous reagents, so that the compound can be used as a green substitute for standard treatment conditions in Curtius rearrangement and Hofmann rearrangement reactions. The substrate is wide in applicability, and the corresponding asymmetricurea and thiocarbamate compounds can be obtained at a relatively good yield. The operation process is simple and suitable for large-scale preparation.
An efficient one-pot synthesis of: N, N ′-disubstituted ureas and carbamates from N -acylbenzotriazoles
Singh, Anoop S.,Kumar, Dhananjay,Mishra, Nidhi,Tiwari, Vinod K.
, p. 84512 - 84522 (2016/10/12)
A facile and high-yielding one-pot synthesis of carbamates and N,N′-disubstituted symmetrical ureas from N-acylbenzotriazoles has been devised. It is believed that, the intermediate acyl-azide undergo Curtius rearrangement and in different solvents gives different products i.e. carbamates in alcohols and N,N′-disubstituted symmetrical urea in THF.
