239463-85-5Relevant articles and documents
THE MANUFACTURING METHOD OF INTERMEDIATE FOR SYNTHESIS OF SILODOSIN AND THE MANUFACTURING METHOD OF SILODOSIN
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, (2020/03/31)
The present invention relates to a method for producing an intermediate for the synthesis, of a cilodosin, and a method for producing, a cilodosin using the, same, which can be used in a method for producing a cilodosin, which can increase the price competitiveness and can reduce. risk factors in the production process, facilitate mass production, and obtain a high purity of xylodosin. (by machine translation)
Method for preparing silodosin intermediate
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Paragraph 0039; 0049; 0058; 0067; 0076; 0084; 0085, (2019/01/06)
The invention discloses a method for preparing silodosin intermediate 5-[(2R)-2-aminopropyl]-2,3-dihydro-1-[3-(benzoyloxy)propyl]-1H-indolyl-7-nitrily-L-(+)-tartrate. The method specifically comprisesthe steps of recovering waste filter liquor in a resolution reaction, subjecting the filter liquor to catalyzed racemation by a palladium catalyst so as to prepare a raw material, i.e., 5-[2-aminopropyl]-2,3-dihydro-1-[3-(benzoyloxy)propyl]-1H-indolyl-7-nitrile, and then, at least repeating resolution once, thereby increasing the yield of the resolution product, i.e., a key intermediate of silodosin, i.e., 5-[(2R)-2-aminopropyl]-2,3-dihydro-1-[3-(benzoyloxy)propyl]-1H-indolyl-7-nitrily-L-(+)-tartrate. The target product prepared by the method disclosed by the invention is high in yield and low in cost, preconceptions in the prior art are overcome, and thus, the method is more applicable to industrial production.
Process for Production of Optically Active Indoline Derivatives or Salts Thereof
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Paragraph 0123; 0159; 0160; 0162; 0164; 0166, (2018/03/01)
The present invention relates to a synthesis method of optically active indoline derivatives or salts thereof, which are represented by general formula I and useful as a starting material for the production of drugs. By introducing terephthaloyl chloride as a starting material and using the same as a link in the synthesis of indoline derivatives or salts thereof, the present invention increases efficiency, greatly facilitates confirmation of intermediates, purification, and processes, and also increases the efficiency of reaction due to excellent stability. By using inexpensive and easy-to-handle zinc instead of expensive platinum catalyst, the present invention improves the yield thereof. By introducing a benzyl group into an amine group (general formula III, preferably chemical formula 23) to ensure optical purity in the final process, the present invention can produce, merely by means of recrystallization, optically pure indoline derivatives or salts thereof, represented by the general formula I.COPYRIGHT KIPO 2016