Abstract
AbstractAuranofin (1), a phosphine gold(I) thiolate antiarthritic agent effective on oral administration, was labelled separately with 195Au, 32P and 35S. 195Au‐labelled auranofin 19 was made from H195AuCl4.3H20 via the intermediate chloro(triethylphosphine)gold‐195Au (18). Auranofin ‐35S (23) was prepared using thiourea‐35S. The synthetic routes for 19 and 23 were similar to those used for unlabelled 1. However, auranofin‐32p (28) was made by the novel, direct coupling of the 1: complex (2,3,4,6‐tetraO‐acetyl‐l‐thio‐β‐D‐glucopyranosato‐S)gold (27) with 32p(C2H5)3 (26) synthesized from 32PCl3 (24). The labelled compounds were used in pharmacokinetic, tissue distribution and metabolism studies.
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