申请人:Zambon S.p.A.
公开号:US04772719A1
公开(公告)日:1988-09-20
A novel process for the preparation of 3-bromo- and 3-chloro-5-substituted isoxazoles is provided. Dibromo- or dichloro-formaldoxime is reacted with an excess of an 1-alkyne derivative of the formula R--C.tbd.CH where R is hydrogen, phenyl or 1-6 C alkyl optionally substituted by halogen, OH, OR', CHO, COR', COOR', CONH.sub.2, CONR'R" or NHCOR' where, in turn, R' and R", which may be the same or different, are a 1-6 C alkyl or haloalkyl, in the presence of (i) at least an equimolecular amount, with respect to the dibromo- or dichloro-formaldoxime, of an alkaline base selected from the class consisting of sodium and potassium carbonate and bicarbonate and (ii) an inert solvent in which the 1-alkyne is soluble at room temperature.
提供了一种制备3-溴和3-氯-5-取代异噁唑的新工艺。在碱性催化剂的存在下,将二溴或二氯甲醛肟与公式为R-C.tbd.CH的1-炔基衍生物的过量反应,其中R是氢、苯基或1-6个碳原子的烷基,可选地被卤素、OH、OR'、CHO、COR'、COOR'、CONH.sub.2、CONR'R"或NHCOR'取代,其中R'和R"可以相同或不同,是1-6个碳原子的烷基或卤代烷基,且存在惰性溶剂,其中1-炔基在室温下溶解。碱性催化剂可以选择从钠和钾碳酸盐和碳酸氢盐中选择至少一个等摩尔量。