104458-24-4Relevant articles and documents
Preparation method of lapatinib intermediate 2-(methanesulfonyl)ethylamine hydrochloride
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Paragraph 0011; 0029; 0032; 0033; 0035-0037, (2017/10/13)
The invention discloses a preparation method of lapatinib intermediate 2-(methanesulfonyl)ethylamine hydrochloride. The preparation method comprises the steps of adopting 2-chloroethylamine hydrochloride (Compound 2) as a starting material, and under an alkaline condition, carrying out dimolecular substitution reaction on the starting material and sodium methyl mercaptide to prepare 2-methylmercapto ethylamine (Compound 3); then adopting water as a solvent, adding hydrochloric acid for salifying, and directly using hydrogen peroxide for oxidizing to obtain the 2-(methanesulfonyl)ethylamine hydrochloride (Compound 1). According to the preparation method provided by the invention, a synthetic route is short, the raw materials are simple and easy to get, the water is adopted as the solvent, the reaction condition is moderate, the after-treatment is simple, and the obtained product is good in quality and high in yield. The method can cause less three wastes, and is environmentally friendly and suitable for industrial production. The formula is shown in the specification.
Lapatinib process for the preparation of intermediates
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Paragraph 0033; 0034, (2017/01/17)
The invention discloses a preparation method of a Tykerb intermediate. The preparation method of the Tykerb intermediate 1 comprises the following steps: (1) performing a nucleophilic substitute reaction on a compound as shown in a formula 3 and a compound as shown in a formula 4 under the effect of a catalyst in an organic solvent, wherein X is chlorine or bromine, M is sodium, potassium or zinc, and n is equal to 1 or 2; and (2) enabling a compound 2 obtained in the step (1) to react in a hydrogen chloride solution. According to the preparation method of the Tykerb intermediate 2, the nucleophilic substitute reaction is carried out on the compound as shown in the formula 3 and the compound as shown in the formula 4 under the effect of the catalyst in the organic solvent. The preparation method disclosed by the invention is simple to operate, the raw materials are cheap and easy to obtain, no environment pollution factor is caused, and the method is suitable for large-scale production in industry.
THE NEW PREPARATION OF ALIPHATIC AMINES WITH SULPHONYL GROUP AND THEIR SALTS
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Page/Page column 6, (2011/04/25)
The present invention relates to a novel preparation method of sulfonyl alkylamine and salts thereof. The method of present invention comprises steps of: adopting sulfonates containing a sulfone moiety as starring material and ammonia oz amine as substituting agent which reacts with the starting material to prepare for the products. Furthermore, the present invention provides a new intermediate 2-(N,N- dibenzylamino) ethyl methyl sulfone and salts thereof obtained from the above novel preparation method and their use. In addition, the present invention also provides a novel salt of 2-(anuno) ethyl methyl sulfone prepared using 2-(amine) ethyl methyl sulfone hydrochloride and the use of novel salt. The present invention is not only advantageous for reducing environmental pollution, but also could be used for mass fabrication of 2-(amino) ethyl methyl sulfone and the salts thereof, in addition, the present invention is advantageous for preparing for the highly purified 2-(amine) ethyl methyl sulfone hydrochloride.