Abstract

D-threo-chloramphenicol is a structurally unique natural product and has been labelled in the past with 14C. These earlier synthetic efforts were characterized by either low yield or low specific activity and likely scalability issues. We needed to prepare large amounts of [14C] D-threo-chloramphenicol over an extended period of time and required a robust synthetic process to accomplish this. Like several other past approaches, we also employed [14C] dichloroacetic acid as an intermediate but utilized a unique preparation of it based on non radioactive synthetic literature. We also devised an HPLC purification of [14C] D-threo-chloramphenicol for increased purity as well as optimized its storage conditions to minimize decomposition.

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