2079-54-1Relevant articles and documents
Selegiline hydrochloride synthesis process
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Paragraph 0135-0141, (2020/01/25)
The invention relates to the field of chemical pharmacy, particularly to a selegiline hydrochloride preparation method. According to the invention, the method avoids the use of ephedrine, pseudoephedrine, deoxyephedrine and other management and control products, has characteristics of inexpensive and easily-available raw materials, short synthesis route, safe and environmentally-friendly production and synthesis cost reducing, can obtain the high-purity target compound at high yield, and is suitable for industrial large-scale production.
Improved process for the preparation of propargyl ammonium-chloride derivatives
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, (2008/06/13)
The present invention relates to a process for the preparation of L-isomer of propargyl-ammonium-chloride derivatives of the general formula (I) by decomposing D-tartarate of L-isomer of the amine of the general formula (II) and by reacting the obtained L-isomer amine of the general formula (II) in the presence of a base with a halide of the general formula (V), and by reacting the so-obtained L-isomer of the general formula (III) with hydrogen-chloride in an organic solvent, wherein, ???- x stands for a halogen atom,???- y stands for a hydrogen or fluorine atom, ???which comprises releasing the amine base from the D-tartarate of the L-isomer of the amine of the general formula (II), wherein y is as given above, in aqueous suspension with ammonium hydroxide or basic alkaline salt and/or ammonium salt, and reacting same with 1-1.5 mole equivalent of a halide of the general formula (V), wherein, ???- x is as defined above -, ???at 0-50 °C in a buffer system of the pH of 8-12 directly formed in the course of the base release and after separating the aqueous layer extracting the mixture containing L-isomer amines of the general formulae (II) and (III) in the organic layer with water and with a mixture of ammonium hydroxide and water and/or with a solution of aqueous phosphate salt of a pH of 5.5-7.5 and dissolving the L-isomer amine of the general formula (II) or salts thereof into the aqueous layer and selectively separating it from the L-isomer amine of the general formula (III) and converting the L-isomer amine of the general formula (III) after distillation to L-isomer salt of the general formula (I) by a method known per se.
Process for the preparation of propargyl amines
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, (2008/06/13)
The invention relates to a new process for the preparation of propargyl ammonium chlorides of the Formula I STR1 by alkaline decomposition of the d-tartarate of the 1-isomer of an amine of the Formula II STR2 and subsequent reaction of the amine of the Formula II with a halide of the Formula III in the presence of an organic solvent, alkali and water in which in Formulae II and III respectively, n is 1 or 0 and X stands for halogen which comprises reacting the d-tartarate of the 1-isomer of an amine of the Formula II in aqueous suspension with an alkali, dissolving the base of the Formula II, thus set free without isolation in a water non-miscible organic solvent and reacting the same in the said phase with a halide of the Formula III, and thereafter--preferably after separating the aqueous layer--reacting the mixture which contains the amines of the Formulae II and IV STR3 in the organic phase in the presence of water with an organic acid or a solution which has a pH value of 1.5-6 and consists of an inorganic acid and water, thus dissolving in the two-phase mixture formed the salt of the amine of the Formula II in the aqueous layer and selectively separating the amine of the Formula II from the amine of the Formula IV, and thereafter adding after the separation of the phases hydrogen chloride to the amine of the Formula IV being in the organic phase and thus precipitating the salt of the Formula I. The compounds of Formula I are known pharmaceutical active ingredients. The advantage of the process of the present invention that it is highly economical and enables the recovery of the starting materials on large scale production too.
