Guaiacol esters of alpha- and beta-mercaptopropionylalanine and alpha- and beta-mercaptopropionylglycine, process for their preparation and pharmaceutical compositions containing same
申请人:Sigma-Tau Industrie
Farmaceutiche Riunite S.p.A.
公开号:EP0013261A1
公开(公告)日:1980-07-09
Gualacol esters of alpha- and beta-mercaptopropionyl alanine and of alpha- and beta-mercaptopropionyl glycine having formulae:
wherein R is hydrogen or methyl and Y is hydrogen or an acyl radical (acetyl, benzoyl or methoxycarbonyl).
Pharmaceutical compositions containing these guaiacol esters have mucolytic activity.
The process for manufacturing these guaiacol esters comprises preparing in a known per se manner a sulhydryl group-containing intermediate wherein the sulfhydryl is protected by a trityl or p-methoxybenzyl group, and removing the protective group under acid conditions.
α-和β-巯基丙酰基丙氨酸以及α-和β-巯基丙酰基甘氨酸的愈创木酚酯,其化学式为
其中 R 是氢或甲基,Y 是氢或酰基(乙酰基、苯甲酰基或甲氧基羰基)。
含有这些愈创木酚酯的药物组合物具有粘液溶解活性。
制造这些愈创木酚酯的工艺包括以已知的本身方式制备含巯基的中间体,其中的巯基被三苯甲基或对甲氧基苄基保护,然后在酸性条件下去除保护基。