SummaryBleomycin sulfate in D 2 O was deuterated using microwave irradiation under catalyst free conditions. Following the removal of labile deuterium and purification, bleomycin A 2 with mass M þ 1 to M þ 7 was obtained. Successful selective uncatalyzed microwave deuterium exchange reactions on examples from the following classes of heterocycles are also described: imidazole, thiazole, indole, purine, and quinazoline. The described method was used as a test for non-labile active protons.
SummaryThe octahydroindenone intermediate was tritium labeled using T 2 O isotope exchange labeling, and then elaborated to the vitamin D derivative RO275646. Though this method of labeling was expected to give the minor isomer, it was the shortest and most convenient route to the high specific activity metabolically stable labeled sites. A total of 34 mCi (from two separate runs) at 64 Ci/mmol of [ 3 H]-RO275646 were prepared by this method.
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