A process is described for the preparation of (RR,SS)-2-dimethylaminomethyl-1-(3-methoxyphenyl) cyclohexanol hydrochloride (hereinafter 'tramadol hydrochloride'), which process comprises reacting an intermediate comprising one or more of:
(a) a mixture of (RR,SS)- and (RS,SR)-2-dimethylaminomethyl-1-(3-methoxyphenyl) cyclohexanol; and/or
(b) a hydrate of (RR,SS)-2-dimethylaminomethyl-1-(3-methoxyphenyl) cyclohexanol;
with HCl in the presence of a catalytic amount of water.
The process can be carried out in the absence of 1,4-dioxane or other category 1 carcinogenic solvent, and in one step, providing commercial advantages of simplicity, safety and purity. Tramadol hydrochloride is a known non-narcotic analgesic.
本发明描述了一种制备(RR,SS)-2-二
甲基氨基甲基-
1-(3-甲氧基苯基)环己醇盐酸盐(以下简称 "
盐酸曲马多")的工艺,该工艺包括使包含以下物质中的一种或多种的中间体发生反应:
(a) (RR,SS)-和(RS,SR)-2-二
甲基氨基甲基-
1-(3-甲氧基苯基)环己醇的混合物;和/或
(b) (RR,SS)-2-二
甲基氨基甲基-
1-(3-甲氧基苯基)环己醇的
水合物;
在一定量的
水催化下与
盐酸反应。
该工艺可在不使用 1,4-
二恶烷或其他 1 类致癌溶剂的情况下一步完成,具有简单、安全和纯度高等商业优势。
盐酸曲马多是一种已知的非麻醉性
镇痛药。