Abstract: Methods and processes for preparation and production of deuterated ?-diphenylurea are disclosed. Especially, a kind of deuterated ?-diphenylurea compounds which can inhibit phosphokinase and the preparation method of N-(4-chloro-3-(trifluoromethyl)phenye-N?-(4-(2-(N-d3-methylcarbamoyl)-4-pridinyloxy)phenyl)urea are disclosed. The said deuterated diphenylurea compounds can be used for treating or preventing tumors and relative diseases.

Abstract: Preparation methods of methyl-d3-amine and salts thereof are provided, which contain the following steps: (i) nitromethane is subjected to react with deuterium oxide in the present of bases and phase-transfer catalysts to form nitromethane-d3, which is subsequently subjected to reduction in an inert solvent to form methyl-d3-amine, and optionally, methyl-d3-amine reacts subsequently with acids to form salts of methyl-d3-amine; or (ii) N-(1,1,1-trideuteriomethyl)phthalimide is subjected to react with acids to form salts of methyl-d3-amine. The present methods are easy, high efficient, and low cost.

Abstract: This invention relates to deuterated ?-diphenylurea and derivatives and pharmaceutical acceptable salts thereof. And the pharmaceutical compositions comprising the pharmaceutically acceptable carrier and the deuterium-substituted ?-diphenylurea and derivatives and pharmaceutical acceptable salts thereof are also provided. The deuterium-substituted diphenylurea can be used in treatment or prevention of cancer and other related diseases.