PHA-690509, a cyclin-dependent kinase A inhibitor, has been labelled with carbon-14. [ 14 C]PHA-690509 was obtained via a three-step procedure in 10% overall radiochemical yield starting from [ 14 C]thiourea 3.

The system proved be to highly versatile and inexpensive and allowed a quick translation of the radiochemistry project into a working system even by less experienced personnel, because of predefined interfaces between electronic parts and operating software (preloaded on a laptop and included in the kit). The automatic module proved to be a simple and reliable system for the production of 1-[C]acetate that was prepared in 24 min (total synthesis time) with stable radiochemical yields (20% nondecay corrected) and high radiochemical purity (>97%). The module is used routinely to produce 1-[C]acetate for preclinical studies and is being implemented for the production of the labelled fatty acids.

Use of Microwaves in Organic Synthesis: Application in the Synthesis of Isotopically Labelled Compounds Preparation of Tritium‐Labelled BIIL 260 with High Specific Radioactivity Synthesis of [3H]‐, [14C]‐ and [13C,2H]‐labelled Org 12962 Derivatives Labeling of BAY 58‐2667, an Activator of sGC Preparation and Use of [14C]N,N′‐Carbonylditriazole in the Labelling of Urea Derivatives Efficient Carbon‐14 Labeling of 2‐(3‐Hydroxypropyl)‐1H‐benzimidazole Synthesis of Some 14C‐Labelled Fungicides C‐14 Labelling of NVP‐ABE651 and NVP‐ABE697 Synthesis of Carbon‐13,14 Isotopomers of a Novel 4‐Substituted‐2‐Carboxy Tetrahydroquinoline [14C]CH2N2: A Suitable Precursor for the Preparation of 14C‐Labelled Anthracyclines Preparative HPLC: a Useful Approach to Speed‐up the Purification of Labelled Compounds. Use of Stable Isotopes for the Biosynthesis and Biodegradation of Fosfomycin Metalloradiopharmaceuticals for Nuclear Medicine Strategic outlook: Future Methods in DMPK and subsequent requirements for isotopically labelled compounds Isotopic Imaging of Glass‐based cDNA Microarray Hybridization New Developments in Radiation Measuring Technique

SummaryJTT-501 specifically labelled with 13 C was obtained via a four-step synthesis at an isotopic enrichment level of 99% and in 14% overall chemical yield starting from 4-hydroxy-[ring-U-13 C 6 ]benzaldehyde (3). The hydrogenation of

The cytotoxic antitumor compound PNU‐159548 (1) has been labelled with 14C and 2H. A three‐step sequence starting from [14‐14C]idarubicin (2a) led to radiochemically pure (>98%) [14‐14C]PNU‐159548 with a specific activity of 1.13 GBq/mmol. The synthesis of [2H4]PNU‐159548 was carried out in a similar manner starting from [1,1,2,2‐2H4]2‐bromoethanol (3b). Copyright © 2002 John Wiley & Sons, Ltd.