Xu Jian-fe
2013
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Journal
Fine chemicals
Abstract
Friedel-Crafts acylation of salicylaldehyde with bromoacetyl chloride afforded 5(bromoacetyl)-2-hydroxybenzaldehyde(Ⅱ),which then went through amination with tert-butylamine and acid hydrolysis.After going through the purification column the intermediate 5-{[(1,1dimethylethyl) amino]acetyl }-2-hydroxybenzaldehyde hydrochloride(Ⅲ) was obtained.The target compound albuterol-D 2(Ⅳb) was obtained by reduction with boron sodium deuteride.The advantage of this synthetic route lies in the last step of the reaction,where deuterium isotope was introduced to ensure that deuterium labeled isotope abundance was not diluted.The synthetic route boasts the advantages of simple operation,short process flow,and less side product.The yield was more than 70%.The product was characterized by means of MS and1HNMR,and the deuterium enrichment was more than 97.1%.