41198-42-9Relevant academic research and scientific papers
Biosynthesis method of dapoxetine intermediate and intermediate thereof (by machine translation)
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Paragraph 0010; 0032-0036; 0046; 0048; 0049; 0051; 0052, (2019/09/17)
The method comprises a compound (2) and a compound (3) as starting materials, wherein the compound (4), the compound (4) and the biological enzyme conversion reaction are subjected to biological enzyme conversion reaction to finally obtain the dapoxetine intermediate compound (1), and the reaction formula is as follows: The method has the advantages, such as novel, simple and easy synthesis route, low cost, high synthesis yield, high yield, good product purity, good product quality, cheap and accessible raw materials and suitability for industrial production, and provides a new intermediate raw material for the preparation of dapoxetine intermediate . the synthetic method has the advantages of simple and easy synthesis route, high yield, good product quality, cheap and easily available raw materials and the like. (by machine translation)
Preparation method of dapoxetine hydrochloride
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Paragraph 0041; 0048; 0054; 0055, (2018/04/01)
The invention belongs to the technical field of drug preparation and particularly relates to a preparation method of dapoxetine hydrochloride. The method comprises steps as follows: a compound 3 and alkali are dissolved in an organic solvent for a reaction, then, a compound 2 is added, an esterification reaction is performed, and a compound 4 is obtained; the compound 4 is subjected to asymmetric reduction by a chiral reducing agent in an organic solvent, and a compound 5 is obtained; the compound 5 reacts with MsCl, trimethylamine and 4-dimethylamino-pyridine in an organic solvent, dimethylamine hydrochloride is added for a further reaction, a product is added to water, extracted with ethyl acetate and steamed to form an oily substance, cooling, crystallization and suction filtration are performed, dapoxetine free alkali solids are obtained and dissolved in isopropanol, an isopropanol solution of hydrogen chloride is added and crystalized, and dapoxetine hydrochloride is obtained. The chemical purity and the optical purity are high, the quality is stable, operation is simple and convenient, the yield is high, the quality is stable, large-scale production is facilitated, the production cycle is shorter, and the synthesis route is shown in the specification.
Dapoxetine intermediate and preparation method thereof
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, (2017/03/28)
The invention discloses a dapoxetine intermediate and a preparation method thereof and provides a preparation method for the compound represented in the formula (2). The preparation method includes a step of performing a nucleophilic substitution reaction to the compound represented in the formula (3) with 1-naphthol in a solvent in the presence of alkali to prepare the compound represented in the formula (2). The R1 and the R2 are independently C1-C4 alkyl groups, or that the R1, the R2, oxygen atoms connected thereto respectively and carbon atoms connected to the oxygen atoms form a five-membered saturated ring structure or six-membered saturated ring structure, wherein X is Cl, Br or I. The raw materials are low in cost and easy to obtain. The preparation method is mild in reaction conditions, is high in conversion rate, is high in yield, is simple in after treatment, is low in production cost, is high in chemical purity of product, and is suitable for industrial production.
Corey-itsuno reduction of ketones: A development of safe and inexpensive process for synthesis of some API intermediates
Mahale, Rajendra D.,Chaskar, Sudhir P.,Patil, Kiran E.,Maikap, Golak C.,Gurjar, Mukund K.
supporting information; experimental part, p. 710 - 713 (2012/07/27)
A safe and inexpensive procedure for asymmetric reduction of ketones using in situ prepared N,N-diethylaniline borane (DEANB) and oxazaborolidine catalyst from sodium borohydride, N,N-diethylaniline hydrochloride and (S)-α,α-diphenylprolinol is described. This protocol is demonstrated successfully to manufacture enantiopure dapoxetine at the plant scale.
