[en] The Hantzsch synthesis has been applied to the general preparation of 4-aryl-dihydropyridines labelled in the metabolically stable 4-position of the dihydropyridine ring. The synthesis is based on the preparation of a key common intermediate, m-nitrobenzaldehyde-[formyl-¹⁴C], in high yield from Ba¹⁴CO₃. (author)

[en] Synthesis of the potent immunosuppressive agent, mycophenolate mofetil labelled with carbon-14 is described. Methoxyethoxymethyl (MEM) protected mycophenolate norbromide was prepared from unlabelled mycophenolic acid using a modified Hunsdiecker reaction. A three step synthesis furnished the title compound, having a specific activity of 53.8 mCi/mmol, in 49.5% overall yield from K¹⁴CN. (author)

[en] The synthesis of high specific activity 3-nitrobenzaldehyde-[4,6-³H], a key intermediate in the general synthesis of tritiated 4-aryldihydropyridines, is described. This substance was then used to prepare the calcium channel entry blocker, nicardipine-[4',6'-³H] at a specific activity of 51 Ci/mmole via the Hantzsch process. (author)

[en] The labelled dehydroamino acid, 2-N-acetylamino-3-(2-naphthyl)-3-[¹⁴C]-acrylic acid was prepared at 52.8 mCi/m mol from Ba¹⁴CO₃. Asymmetric reduction of this precursor with hydrogen in the presence of the chiral homogeneous catalyst (S,S) BPPMRh⁺ afforded N-acetyl-D-3-(2-naphthyl)-3-[¹⁴C]-alanine in greater than 98% optical yield. This unnatural amino acid was used in a solution phase synthesis of 2 ¹⁴C-labelled LHRH analogs, [N-Ac-D-3[¹⁴C]Nal¹ D-p-Cl-Phe², D-Trp³, D-hArg(Et₂)⁶, D-Ala¹⁰] LHRH and [D-3-[¹⁴C] Nal⁶] LHRH having specific activities in excess of 50 mCi/mmol. (author)

[en] A facile synthesis of the anti-inflammatory agent RS-42169-¹⁴C, based on a carbonation/cycloaddition sequence is described. The product was obtained in 36% yield from Ba¹⁴CO₃ at a specific activity of 52 mCi/mmole. The design of the six step sequence was such that pure intermediates were isolated by extractive workup, and only a single chromatographic purification was required. (author)

[en] The synthesis of the high specific activity (39 Ci/mmole) tritium labelled steroid norgestrel is described. A practical synthesis of the required substrate for tritium incorporation, 18-methyl-Δ⁹⁽¹¹⁾-estradiol-3-methyl ether, was developed from norgestrel itself. Following reduction with carrier-free tritium gas, microscale conditions were employed for the conversion of the resulting labelled intermediate back to norgestrel-[9,11-³H], including a selective in situ projection of the A-ring ketone of 19-norandrost-4-ene-3,17-dione. (Author)

[en] For the Chinese industry as the mainstay of the national economy and dominant energy user and carbon emitter, an integrative assessment is performed from major energy policy perspectives of energy security, energy efficiency and carbon emission. Extensive systems indicators, including oil dependence ratio, average oil growth rate; indices of energy diversity, of carbonization and of oil growth risk; ratios of energy use to output, to value added and to compensation for laborers; ratios of carbon emission to output, to value added and to compensation for laborers, are devised to assess the Chinese industry 2002-2007 with most recent statistics availability. Combined indicators are identified by sparse principle component analysis to characterize sector performances. The industrial sectors are classified into five clusters and the main features of each cluster are pinpointed using fuzzy clustering algorithm. Concrete results facilitate comparisons of sectors to enable more accurate policy recommendations. - Highlights: → An assessment is performed from major energy policy perspectives in China. → Extensive systems indicators are devised to assess the Chinese industry. → Combined indicators are identified by SPCA to characterize sector performance. → Industrial sectors are classified for more accurate policy recommendations.