Abstract
A family of effective bifunctional chelators for technetium- and rhenium-based radiopharmaceuticals was conveniently synthesized in high yields through direct reductive N-alkylations of amino acids and their analogues with aldehydes, using NaBH(OAc)3 as an efficient reagent. The mono-, di-, tetra- and even mixed alkylated amino acid derivatives were all prepared in one-pot synthesis.
Key words
reductive alkylation - amino acids - bifunctional chelators - radiopharmaceuticals - sodium triacetoxyborohydride
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[1 6 (C22 H25 N3 O3 , formula weight 379.45): Orthorhombic, space group P 21 21 21 with a = 7.3392(4) Å, b = 15.0539(7) Å, c = 17.9286(9) Å, V = 1980.82(17) Å3 , Z = 4, R 1 = 0.0556, wR 2 = 0.1079 (F2 , all data). Full details on the crystal structure of 6 are available from the authors.
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