首页> 外国专利> Process for producing N- 4-(substituted phenyl) alkylthienyl-and N-4-(substituted phenyl) alkylfuryl -but-3-yn-2-yl -N-hydroxyurea compounds

Process for producing N- 4-(substituted phenyl) alkylthienyl-and N-4-(substituted phenyl) alkylfuryl -but-3-yn-2-yl -N-hydroxyurea compounds

机译:N- [4-[(取代的苯基)烷基噻吩基]-和N-4-[(取代的苯基)烷基呋喃基] -but-3-yn-2-yl] -N-羟基脲化合物的制备方法

摘要

A process for preparing a compound of the structure I IMAGE I where A is oxygen and sulfur and R1 is selected from the group consisting of hydrogen, halogen, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, and trifluoromethyl, and R2 is alkyl of one to four carbon atoms, comprising coupling a compound of formula II: IMAGE II where X is bromine or iodine, with an N-hydroxyurea compound of formula III: IMAGE III in the presence of a palladium catalyst followed by reaction of the product thus formed with an alkali metal isocyante. The compounds of formula I are inhibitors of the enzyme 5-lipoxygenase and are thus useful as therapeutic agents for the treatment of allergic and inflammatory disease conditions.
机译:制备结构I I的化合物的方法,其中A是氧和硫,R 1选自氢,卤素,1-6个碳原子的烷基,1-6个碳原子的烷氧基和三氟甲基,并且R 2是具有1-4个碳原子的烷基,包括在存在下,将式II的化合物: II,其中X是溴或碘,与式III的N-羟基脲化合物: III钯催化剂,然后使如此形成的产物与碱金属异氰酸酯反应。式I化合物是5-脂氧合酶的抑制剂,因此可用作治疗变应性和炎性疾病的治疗剂。

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