Tritiodestannylation. Synthesis of a Specifically Labelled [³H]Tamoxifen

Addition of arylstannanes to alkynes givingortho-alkenylarylstannanes catalysed cooperatively by a rhodium complex and zinc chloride

“…The synthetic utility of arylstannanes has been well established. 1 According to the reported procedures, 21 – 23 tributylstannyl group in 3aa was converted into deuterio ( 8 ), iodo ( 9 ) and fluoro ( 10 ) successfully ( Scheme 4 ). The palladium-catalysed cross-coupling with an aryl iodide 2 and the rhodium-catalysed conjugate addition to 2-cyclohexenone 16 gave high yields of the corresponding products, 11 and 12 , respectively, as expected.…”

Single Isomer Technetium-99m Tamoxifen Conjugates

“…Since over 60% of breast cancer tumors contains estrogen receptors, the discovery of an estrogen receptor specific radiopharmaceutical is desirable. Not surprisingly, tamoxifen has been the target of several radiolabeling studies including 3 H ( , ), 18 F (), 111 In (), 123 I (), 125 I (), and 131 I (), but labeling with 99m Tc has not been reported. Given the widespread use of technetium-99m for radiopharmaceuticals, our previous experience with a radiolabeled tamoxifen, and our recent preparation of an N 2 S 2 bifunctional chelator, the attachment of 99m Tc via a linker from tamoxifen to an N 2 S 2 bifunctional chelator was attempted.…”