1592614-01-1Relevant articles and documents
Directed lithiation of N′-[2-(4-methoxyphenyl)ethyl]-N, N-dimethylurea and tert-butyl [2-(4-methoxyphenyl)ethyl]carbamate
Smith, Keith,El-Hiti, Gamal A.,Alshammari, Mohammed B.
, p. 394 - 402 (2014)
N′-[2-(4-Methoxyphenyl)ethyl]-N,N-dimethylurea and tert-butyl [2-(4-methoxyphenyl)ethyl]carbamate are doubly lithiated on the nitrogen and ortho to the directing metalating group at -20 to 0 °C with three mole equivalents of n-BuLi in anhydrous THF. Reactions of the dilithium reagents produced in situ with various electrophiles give high yields of the corresponding substituted products. In the case of the urea, side-products due to lithiation and substitution on one of the methyl groups of the urea unit are obtained in low yields (0-17%). Georg Thieme Verlag KG Stuttgart · New York.
Antioxidant Activity, Acetylcholinesterase, and Carbonic Anhydrase Inhibitory Properties of Novel Ureas Derived from Phenethylamines
Aksu, Kadir,?zgeri?, Bünyamin,Taslimi, Parham,Naderi, Ali,Gül?in, ?lhami,G?ksu, Süleyman
, p. 944 - 954 (2016)
A series of ureas derived from phenethylamines were synthesized and evaluated for human carbonic anhydrase (hCA) I and II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activities and antioxidant properties. The ureas were synthesized from the reactions of substituted phenethylamines with N,N-dimethylcarbamoyl chloride; then, the synthesized compounds were converted to their corresponding phenolic derivatives via O-demethylation. hCA I and II were effectively inhibited by the newly synthesized compounds, with Ki values in the range of 0.307–0.432 nM for hCA I and 0.149–0.278 nM for hCA II. On the other hand, the Ki parameters of these compounds for AChE and BChE were determined in the range of 0.129–0.434 and 0.095–0.207 nM, respectively. Phenolic ureas also showed good antioxidant activities.
