- (S)- (-) - 3 - methylamino - 1 - (2 - thienyl) - 1 - propanol synthetic method
-
The present invention relates to a method for preparing (S)-(-)-3-methylamino-1-(2-thienyl)-1-propanol with high purity. The method comprises: taking the (S)-(-)-3-dimethylamino-1-(2-thienyl)-1-propanol as an starting material; in the presence of an organic solvent, protecting hydroxyl by a hydroxy protecting agent, then carrying out a demethylation reaction; and finally, carrying out a hydroxyl de-protection reaction in a strong alkaline environment in the presence of a hydroxyl de-protection agent, thereby obtaining a target product. According to the synthetic method, the (S)-(-)-3-methylamino-1-(2-thienyl)-1-propanol is over 99% in purity and ee value, and is over 80% in the yield, and the method is suitable for industrial production.
- -
-
Paragraph 0061; 0062; 0063; 0064; 0065; 0066-0068
(2017/08/25)
-
- PROPANOLAMINE DERIVATIVES, PROCESS FOR PREPARATION OF 3-N-METHYLAMINO-1-(2-THIENYL)-1-PROPANOLS AND PROCESS FOR PREPARATION OF PROPANOLAMINE DERIVATIVES
-
The present invention provides means for preparing a racemate or an optically active substance (S- or R-isomer) of 3-N-methylamino-1-(2-thienyl)-1-propanol represented by the following general formula (I): wherein R1 represents any of a hydrogen atom, a C1-8 acyl group, a substituted or substituted C1-8 alkyloxycarbonyl group and a substituted or substituted phenyloxycarbonyl group and R2 represents any of a hydrogen atom, a C1-8 alkyl group, a substituted or substituted benzyl group, a C1-8 acyl group, a substituted or substituted C1-8 alkyloxycarbonyl group and a substituted or substituted phenyloxycarbonyl group, with the exception that R1 is a hydrogen atom and R2 is a methyl group or a hydrogen atom, in a simple manner at low cost and in high yield.
- -
-
Page/Page column 32
(2010/02/10)
-