Tetroxoprim

四氧普林Chemical Name: 5-[3,5-Dimethoxy-4-(2-methoxyethoxy)benzyl]pyrimidine-2,4-diamine
CAS No. 53808-87-0
项目整合开发状态: Not Determined
项目研究机构:
合成路线:Tetroxoprim can be synthesised by three different routes:1) 2-Amino-4-hydroxy-5-[3,5-dimethoxy-4-(2-methoxyethoxy)benzyl]pyrimidine can be obtained by conversion of 3,5-dimethoxy-4-(2-methoxyethoxy)hydroxycinnamic acid ethyl ester (I) with the addition of sodium methylate and guanidine hydrochloride (II).With the acid of phosphorousoxychloride (III) can be converted to (IV) and then finally aminolysed to tetroxoprim at 160 C.

合成路线:2) Using 3,5-dimethoxy-4-(2-methoxyethoxy)benzaldehyde (V) as a starting material,Tetroprim can be obtained by reaction with 3-methoxypropionitrile (VI) in the presence of a basic catalyst and ring closure finally brought about with guanidine hydrochloride (II).

合成路线:3) 2,4-Diamino-5-(3,5-dimethoxy-4-hydroxybenzyl)pyrimidine (VII) can be etherised after heating under reflux for three hours with p-toluenesulfonic acid-(2-methoxyethyl)ester (IX) in the presence of a basic catalyst.