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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′‐14C] and [3′, 5′‐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,...
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