82098-65-5Relevant articles and documents
Synthesis of 4-(4-Amidinophenyl)-2-arylsulphonylaminobutyric Acid Amides
Wagner, G.,Vieweg, H.
, p. 13 - 16 (2007/10/02)
4-(4-Amidinophenyl)-2-arylsulphonylaminobutyric acid amides with differing amide and arylsulphonyl components were synthetized to test their inhibitory activity against serine proteinases.For the purpose of preparing these compounds, β-(4-cyanophenyl)ethylbromide (5) was reacted with acetaminomalonic acid diethyl ester to give 6, the acid hydrolysis of which yielded predominantly 4-(4-carbamoylphenyl)-2-aminobutyric acid (7).The simultaneously formed dicarboxylic acid 9 was separated after N-arylsulphonylation.The reaction of the N-arylsulphonylated acids 10-15 with thionyl chloride afforded acid chlorides (16-18) with a cyano function from which carboxylic acid amides (19-39) were obtained by reaction with diffrent amines.These compounds were converted into the hydroiodides of the compounds named in the title via the thioamides and the thioimidic acid ester hydroiodides.