申请人:Gruppo Lepetit S.p.A.
公开号:US03953513A1
公开(公告)日:1976-04-27
Process for preparing an .alpha.-aminoalcohol of formula ##EQU1## wherein R represents hydrogen or alkyl of from 1 to 5 carbon atoms, which comprises contacting a compound of formula ##EQU2## wherein R has the same meaning as above, with an alcohol of formula R'-OH wherein R' represents benzyl or the group ##EQU3## in which R" and R"' are independently selected from hydrogen and alkyl of from 1 to 4 carbon atoms in an organic solvent, in the presence of a basic catalyst, at from about 140.degree. to about 170.degree.C., treating the obtained product of formula ##EQU4## wherein R and R' have the above meanings, with at least an equimolecular amount of a p-toluene-sulfonyl halide, at from about -5.degree. to about 20.degree.C. in the presence of a tertiary organic nitrogen-containing base and reacting in a closed system the resulting compound of formula ##EQU5## wherein R and R' are as above defined, with an excess of gaseous ammonia, in the presence of an inert organic solvent, at from about 95.degree. to about 120.degree.C. and recovering the resulting product as its acid addition salt.
制备一种具有以下结构式的α-氨基醇的过程##EQU1##其中R代表氢或1至5个碳原子的烷基,包括将具有以下结构式的化合物与具有以下结构式的醇在有机溶剂中与碱性催化剂一起在大约140℃至170℃下接触,其中R具有与上述相同的含义,其中R'代表苄基或基团##EQU3##其中R"和R"'分别选自氢和1至4个碳原子的烷基,处理得到的具有以下结构式的产物##EQU4##其中R和R'具有上述含义,至少与对甲苯磺酰卤反应,反应温度在-5℃至20℃之间,在三级有机氮含基存在的情况下,在封闭系统中反应得到的具有以下结构式的化合物##EQU5##其中R和R'如上定义,与过量氨气反应,在惰性有机溶剂存在下,在大约95℃至120℃之间,并将得到的产物作为其酸盐进行回收。