Synthesis of ¹⁴C‐labelled 4‐(2‐hydroxy‐3‐isopropylaminopropoxy)‐2‐methyl‐indole (mapindolol)

Abstract

flepindolol, a potent 0-adrenoceptor blocking agent, was labelled with I 4 C by two different routes yielding the 2-PClmethyl and L-l4d products. While the first alternative was abandoned because o f low overall yield, the latter route provided mepindolol with a specific activity o f 2.06 GBq/rnmole (55.8 mCi/mmole) and in a radiochemical yield of 40% starting from Ba14C05.

Preparation of Carbon‐14‐Labeled Compounds via Multi‐Carbon Building Blocks of the [ 14 C]Carbon Dioxide Tree

“…In the latter case, 3-substituted N-½1-14 Cacetylated toluidine 30 served as a key intermediate for the synthesis of ½2-14 Cmepindolol (34). In the latter case, 3-substituted N-½1-14 Cacetylated toluidine 30 served as a key intermediate for the synthesis of ½2-14 Cmepindolol (34).…”