51062-14-7

The invention discloses a preparation method of a dobutamine hydrochloride intermediate compound. According to the method, 3, 4-dimethoxyphenylethylamine and 4-(4-methoxyphenyl)-2-butanone are adoptedas the starting materials, acetic acid is adopted as a catalyst, cyclohexane is adopted as a reflux water diversion agent, reflux water diversion is performed to obtain a condensation product, potassium borohydride is adopted for further hydrogenation reduction, and hydrochloric acid salification is performed to obtain a crude product of a dobutamine hydrochloride intermediate. Isopropanol is adopted for refluxing and dissolving, an inorganic salt generated in the preparation process of the intermediate is removed through filtering while the solution is hot, and refining is conducted to obtain the dopamine hydrochloride intermediate. According to the method, high-pressure catalytic hydrogenation operation in the prior art is avoided, potential safety hazards are greatly reduced, meanwhile, an expensive metal catalyst is prevented from being used, and the production cost is reduced; and the use of some high-toxicity reagents and genotoxic reagents is avoided.

The invention belongs to the field of bulk drug synthesis, and especially relates to a synthetic method of dobutamine hydrochloride. The synthetic method of dobutamine hydrochloride comprises following steps: anisyl acetone, an acid or acid hydrogenation donor, a catalyst, and 3, 4-dimethoxyphenethylamine are added into an organic solvent for mixing, reaction is carried out for 1 to 5h at 30 to 40DEG C; an obtained product is cooled to 10 to 30 DEG C through natural cooling, and filtering is carried out; the pH value of an obtained filtrate is adjusted with a 2% sodium hydroxide aqueous solution to 7 to 8, liquid separating and water washing are carried out; an obtained organic phase is added into concentrated hydrochloric acid for stirring salt forming, the organic phase is collected, and is distilled; an obtained concentrate is subjected to recrystallization in an organic solvent, and vacuum drying is carried out so as to obtain an intermediate; the intermediate is subjected to demethylating at 10 to 20 DEG C under the effect of Lewis acid, and salt forming in concentrated hydrochloric acid is carried out so as to obtain high purity dobutamine hydrochloride. The synthetic methodis capable of avoiding defects in the prior art, a novel dobutamine hydrochloride preparation method is provided, operation is simple, synthesis route is short, the synthetic method is friendly to the environment, yield is high, and cost is low.

This invention relates to an optically active (+)-secondary amine of the formula: STR1 wherein R1 is a lower alkyl, and to a process for preparing a useful intermediate for the production of the optically active dopamine derivatives, namely, optically active (+)-primary amine of the formula: STR2 wherein R1 is a lower alkyl, characterized by the reduction of said optically active (+)-secondary amine.

N-Mono or dihydroxyphenylalkyl dopamine derivatives and salts thereof are inotropic agents useful in a method for treatment of acutely depressed cardiac insufficiency.