The hydrogenation of three different pharmaceutical nitro-containing compounds has been studied using high-throughput experimentation (HTE) methods. Significant improvements to the existing reactions were obtained for two of the examples. Each reaction exhibits distinct features regarding activity and chemoselectivity. The best catalyst and reaction conditions found were remarkably different for each of the reactions. For one of the reactions, larger-scale studies are presented, which show that the screening reactions provided a fast and reliable indicator of the most promising reaction conditions.

A New 3-Amino-2H-azirine as an Aib-Pro Synthon: Synthesis of the C-Terminal Nonapeptide of Trichovirin I 1B.-The chiral azirinylprolinate (S)-(V) is prepared and used as synthon for the dipeptide moiety aminoisobutyric acid-isovaline, used in the synthesis of a nonapeptide, which is the C-terminal 6-14 segment of the tetradecapeptide trichovirin I 1B, isolated from Trichoderma viride. -(LUYKX, R.; BUCHER, C. B.; LINDEN, A.; HEIMGARTNER, H.; Helv.

Total Synthesis of (-)-(2R)-Dihydromyricoidine.-The key steps in the synthesis of the title compound (IX) are diastereoselective Michael addition of the azine (II) to the ester (I), ring enlargement of the lactam (III) and the amine (V), and (Z)-selective Wittig reaction of the aldehyde (VII) generated in situ. Based on this synthesis and comparison of specific rotation it is proposed that the natural product has (S)-configuration, but not (R)-configuration as reported previously. -(HAEUSERMANN, U. A.; LINDEN, A.; SONG, J.; HESSE, M.; Helv.

organic chemistry, review organic chemistry, review Z 0200 23 -279 Synthesis, e.e. Determination and Absolute Configuration of Chiral Organophosphorus Inhibitors of Serine Hydrolases -[5 refs.]. -(FUREGATI, S.; LINDEN, A.; PRZIBILLE, G.; RENTSCH, D.; RUEDI, P.; Proc. ECSOC-1: First Int. Electron. Conf. Synth. Org. Chem.; Proc.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.