Multiple labeling of a potent CX3CR1 antagonist for the treatment of multiple sclerosis

J Malmquist, P Ström

Index: Malmquist, Jonas; Stroem, Peter Journal of Labelled Compounds and Radiopharmaceuticals, 2012 , vol. 55, # 10 p. 387 - 392,6

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Abstract

Several methods for the preparation of five isotopologues of the CX3CR1 antagonist 1 were developed. Volatile and radioactive 1-chloro-and 1-bromo-ethyl-benzene was handled in [2 0-14C] and [3 0, 5 0-3H] labeling of 1. D-Leucinol ((R)-2-amino-4-methylpentan-1-ol) was labeled as [1-14C] and [4-14C] via a Wittig reaction using Garner's aldehyde and a Strecker amino acid synthesis with D-acylase resolvation, respectively. A [2H10] D-leucinol was ...