17013-30-8Relevant articles and documents
Pd-Catalyzed Carbonylation of Acyl Azides
Chang, Wenxu,Fu, Bin,Huang, Baoliang,Jiao, Lei,Li, Zongyang,Wang, Peng,Xu, Shiyang,Yuan, Chenhui,Zhang, Zhenhua
, p. 9497 - 9508 (2019/08/26)
Pd-catalyzed reactions of azides with CO to access an isocynate intermediate have been developed extensively in recent years. However, the catalytic carbonylation of sensitive acyl azides has not been reported. Herein, we report a simple Pd-catalyzed carbonylation reaction of acyl azides with broad substrate scope, high efficiency, and simple operation under mild conditions, which provides facile access to acyl ureas. In addition, a mechanistic study was carried out by both experiment and DFT calculation. Control experiments and kinetic study revealed that the real active palladium species were Pd(0). The result of kinetic study suggested that palladium catalyst, azide, and CO were all involved in the turnover-limiting step except for amine. Further DFT study suggested that an unprecedented five-membered palladacycle intermediate was the key intermediate in the carbonylation reaction. ?
NOVEL THIOUREA OR UREA DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING AIDS, CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 0048; 0050; 0054, (2013/05/09)
Disclosed are novel thiourea or urea derivatives inhibitory of HIV activity. Also provided are a method for preparing the thiourea or urea derivatives, and a pharmaceutical composition for the prophylaxis or therapy of AIDS comprising the derivatives. Hav
Solid-phase synthesis of disubstituted N -acylureas from resin-bound ureas and acyl chlorides
Haecker, Hans-Georg,Meusel, Manuela,Aschfalk, Melanie,Guetschow, Michael
experimental part, p. 59 - 64 (2011/04/15)
Acylureas (ureides) are valued for their important biological activities. Whereas cyclic acylureas have frequently been the object of solid-phase chemistry, only few reports have focused on the solid-supported preparation of acyclic representatives. We have prepared different types of acylureas on Rink amide resin in three or four steps. The products are either N-acylated (9, 18), N-acylated-N′-alkylated (10, 19), or N-acylated-N-alkylated (22). Characteristic NMR parameters of isomeric acylureas 10, 19, and 22 are discussed.