Treatment of 4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-carboxylic acid (I) with di-tert-butyl dicarbonate and triethylamine provided the N-Boc derivative (II), which was subsequently coupled with di-n-butyl [[4-(aminoacetyl)-o-phenylene]dioxy]diacetate (III) using BOP and N-methylmorpholine to afford amide (IV). The Boc protecting group of (IV) was finally cleaved by treatment with trifluoroacetic acid in the presence of anisole.