1402161-28-7

Upstream product

• 87-69-4 L-Tartaric acid 
• 1338365-54-0 5-(2-aminopropyl)-1-[3-(benzoyloxy)propyl]-2,3-dihydro-7-cyano-1H-indole 

Downstream Products

• 239463-85-5 5-[(2R)-2-aminopropyl]-1-[3-(benzoyloxy)propyl]-2,3-dihydro-1H-indol-7-carbonitrile (2R,3R)-2,3-dihydroxybutanedioate salt 
• 160970-54-7 silodosin 
• 885340-13-6 1-(3-hydroxypropyl)-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]-2,3-dihydro-1H-indole-7-carbonitrile 
• 239463-72-0 5-[(2R)-2-aminopropyl]-2,3-dihydro-1-[3-(benzoyloxy)propyl]-1H-indole-7-carbonitrile 

Relevant academic research and scientific papers

Preparation method of silodosin intermediate

The invention discloses a preparation method of a silodosin intermediate and relates to the technical field of medical synthesis, aiming at solving the problem in an existing preparation method that the yield of the silodosin intermediate is low. The preparation method of the silodosin intermediate comprises the following steps: carrying out chirally-induced reductive amination on an alpha-substituted acetone compound to obtain an initial intermediate; carrying out amino protection on the initial intermediate to obtain an amino protected intermediate; carrying out hydroformylation on the aminoprotected intermediate to obtain a hydroformylated intermediate; carrying out oximation on the hydroformylated intermediate to obtain an oximated intermediate; carrying out cyaniding on the oximatedintermediate to obtain a cyanated intermediate; carrying out amino deprotection on the cyanated intermediate to obtain free alkali of the silodosin intermediate; carrying out salt forming treatment onthe free alkali of the silodosin intermediate to obtain the silodosin intermediate. The preparation method of the silodosin intermediate, provided by the invention, is used for preparing silodosin.

Method for preparing silodosin intermediate

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.