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.
Method for preparing silodosin midbody
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, (2016/10/10)
The invention discloses a method for preparing a silodosin midbody. The silodosin midbody is the compound shown in the formula (1) and prepared with indoline derivative and R-alanine derivative which are easy to obtain as starting materials through Friedel-Crafts acylation reaction, reduction reaction, formylation reaction, oximation reaction, dehydration reaction, hydrolysis reaction and salt forming reaction. The compound is used for preparing silodosin. Silodosin is used for treating urination disorder related to benign prostatic hyperplasia. The method has the advantages that raw materials are cheap and easy to obtain, operation is easy, yield is high, production cost is reduced, and the method is suitable for large-scale industrial production.