专利号:US-11078163-B2 优先权日:2014-01-24 标 题 :Processes for the synthesis of substituted urea compounds 发明人:RUSSO DOMENICO; WAHNON JORGE BRUNO REIS; MATON WILLIAM; ESZENYI TIBOR 权利人:BIAL PORTELA & CA SA; BIAL PORTELA & Cª S A 摘要:The present invention concerns a process for preparing a compound having the Formula A; or a pharmaceutically acceptable salt or derivative thereof, or for preparing a substituted urea compound of Formula IIa, or a pharmaceutically acceptable salt or ester thereof, the process comprising the reaction of an imidazolyl intermediate of Formula IIa′ with a carbamoyl halide of the formula: R1R2NC(â•?O)Hal, wherein Hal represents Cl, F, I or Br, wherein the intermediate of Formula IIa′ is prepared by oxidation of the derivative of R5 and R6, R6-C(â•?O)CH2R5 to form a glyoxal intermediate R6-C(â•?O)(Câ•?O)R5, which is subjected to treatment with ammonium hydroxide and an aldehyde R8CHO to provide the intermediate of Formula IIa′ and wherein the compound substituents are as defined herein.
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