申请人:Parcor
公开号:US04174448A1
公开(公告)日:1979-11-13
This invention relates to a process for the preparation of compounds having the general formula: ##STR1## in which: R.sub.1 represents a hydrogen atom, an optionaly substituted alkyl, aryl or aralkyl radical; R.sub.2 and R.sub.3 are the same or different and represent independently a hydrogen atom, a lower alkyl, aryl or heterocyclic radical; and R.sub.4 represents a hydrogen atom or an alkyl, cycloalkyl, alkoxy carbonyl, carboxy, aryl or heterocyclic radical, comprising reacting a compound having the formula: ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 are as defined above, with a compound having the formula: ##STR3## in which R.sub.4 is as defined above; X is a halogen atom, or an optionally substituted alkoxy, thioalkyl or amino group; and Y represents an optionally substituted alkoxy, thioalkyl or amino group, or a group of the formula: ##STR4## in which R is a lower alkyl or aryl radical; or both the groups X and Y, together with the carbon atom to which they are attached, form a 6-membered hexahydro-S-triazinic, trioxannic or trithianic heterocyclic nucleus, in an inert solvent, at a temperature between 0.degree. and 150.degree. C. and in an anhydrous medium, and, if desired, liberating the free base.
本发明涉及一种制备具有一般式的化合物的过程:##STR1##
其中:R.sub.1表示氢原子,可选取代的烷基,芳基或芳基烷基基团;R.sub.2和R.sub.3相同或不同,分别独立地表示氢原子,低烷基,芳基或杂环基团;R.sub.4表示氢原子或烷基,环烷基,烷氧羰基,羧基,芳基或杂环基团,包括将具有以下公式的化合物反应:##STR2##
其中R.sub.1,R.sub.2和R.sub.3如上所定义,与具有以下公式的化合物反应:##STR3##
其中R.sub.4如上定义;X表示卤素原子或可选取代的烷氧基,硫代烷基或氨基团;Y表示可选取代的烷氧基,硫代烷基或氨基团,或者表示以下式子的基团:##STR4##
其中R为低烷基或芳基基团;或者,X和Y基团与它们附着的碳原子一起形成6元环的六氢-S-三氮杂环,三氧杂环或三硫杂环核,在惰性溶剂中,在0℃至150℃的温度下,在无水介质中反应,如果需要,释放出自由碱。