申请人:Bayer Aktiengesellschaft
公开号:US04524205A1
公开(公告)日:1985-06-18
A process for the preparation of a herbicidally active 1-amino-1,3,5-triazone-2,4 (1H,3H)-dione of the formula ##STR1## comprising in a first stage at a temperature from about 0.degree. to 100.degree. C. reacting an isocyanate of the formula R.sup.1 - NCO (II) with an isothio semicarbazone of the tautomeric formulas ##STR2## in which R.sup.3 and R.sup.4 each independently is hydrogen, alkyl, cycloalkyl, aralkyl o alkyl, cycloalkyl, aralkyl or aryl, thereby to form a urea derivative of the tautomeric formulas ##STR3## in a second stage at a temperature between about -50.degree. and 0.degree. C. reacting the urea derivative with phosgene (COCl.sub.2) in the presence of an auxiliary organic base and in the presence of a diluent, at least about 2 mols of phosgene and at least about 2 mols of the auxiliary base being used per mol of urea derivative, thereby to form a 1-alkylideneamino-1,3,5-triazine-2,4(1H,3H)-dione of the formula V ##STR4## and in a third stage converting the 1-alkylideneamino group to a 1-amino group.
一种制备具有除草活性的1-氨基-1,3,5-三唑-2,4(1H,3H)-二酮的方法,该方法包括在第一阶段在温度约为0℃至100℃的条件下,将式R1-NCO(II)的异氰酸酯与式的互变式之一的异硫脲半胱氨酸反应,其中R3和R4各自独立地是氢、烷基、环烷基、芳基烷基或烷基、环烷基、芳基烷基或芳基,从而形成互变式的脲衍生物的公式。在第二阶段,在温度约为-50℃至0℃的条件下,将脲衍生物与光气(COCl2)在辅助有机碱和稀释剂的存在下反应,每摩尔脲衍生物使用至少2摩尔光气和至少2摩尔辅助碱,从而形成公式V的1-烷基亚甲基氨基-1,3,5-三嗪-2,4(1H,3H)-二酮,第三阶段将1-烷基亚甲基氨基基转化为1-氨基基。