An efficient conversion of 1-abietic acid to (+)−3-deoxyaphidicolin

The first total synthesis of (+)?3-deoxyaphidicolin, a selective inhibitor of eukaryotic DNA polymerase α, has been completed efficiently and stereoselectively starting from 1-abietic acid.     

A conducting crystal based on a single-component paramagnetic molecule, [Cu(dmdt)(2)] (dmdt = dimethyltetrathiafulvalenedithiolate)

A single-component conducting molecular crystal composed of paramagnetic copper complexes, [Cu(dmdt)2]0+, was prepared. The crystal has an unprecedented three-dimensionally packed molecular arrangement and exhibits a fairly high conductivity (1 S cm-1 at room temperature). The magnetic susceptibility measurements revealed that [Cu(dmdt)2]0+ molecule keeps most of S = 1/2 spin moments. The difference of the bond lengths between [Cu(dmdt)2]0+ and [Cu(dmdt)2]2- is consistent with the result of the molecular orbital calculation.     

Drug-carrying latices for prolonged release of drugs

Dichlorophene was used as a model drug. Drug-carrying latex particles were prepared by soap-free emulsion copolymerization of dichlorophene acrylate with some hydrophilic methacrylate comonomers. The comonomers used affected not only the structure and colloidal stability of particles, but also the drug-activity of particles. Preliminary study of the drug activity revealed that highly hydrophilic latex particles were very stable and too inactive to be engulfed by amoebae and kill them. On the contrary, less hydrophilic particles carrying a large amount of drug can be an effective device to release drugs at a moderate rate to fight against extracelluar targets such as parasites.     

Non-destructive determination of spontaneously fissioning nuclides by neutron coincidence counting using multichannel time spectroscopy

A non-destructive method for determining the amount of actinoids has been developed. The method is based on thermal neutron coincidence counting and employs a selective detection of neutrons resulting from the spontaneous fission of actinoids. The detection system is described in detail and the measurement results of²⁴⁴Cm as an example are presented. The results show that the measured fission rate of²⁴⁴Cm is consistent with the fission rate calculated from ENDF/B-V data and that the amount of²⁴⁴Cm can be determined within about 5% accuracy even in the presence of a large amount of actinoids, for example, up to 2.6·10⁶, 3.6·10⁴, or 1.6·10³ times in the mass ratio of²³⁹Pu,²⁴¹Am, or²⁴⁰Pu to²⁴⁴Cm, respectively.     

A study on LH- and FSH-RIA kits by immunoradiometric assay

An evaluation of LH- and FSH-RIA BEAD kits based on IRMA was carried out. The results obtained with the methods characterized by the use of monoclonal antibodies, i.e., one is linked to solid phase, and another is isotopically labeled, were compared with those determined by the Daiichi LH- and FSH-kits. Intra- and inter-assay precision, recovery, linearity, and specificity of both methods were favorable without exceptions. The cross reactivity of the LH kit to 5,000 mIU/ml hCG revealed within the range of less than 3 mIU/ml. Significant correlations were observed between the results derived from conventional Daiichi LH- and FSH-kits. The results from the conventional kits exhibited 30 to 40% of those from the Daiichi kits, considered to be mainly due to the difference in standard calibrations used. Among the individuals within the normal menstrual cycle, the serum LH- and FSH-levels determined by the present kits gave a typical pattern with a peak in the preovulatory phase. On the other hand, the LH- and FSH-values of individuals in normal pregnancy revealed strikingly decreased in comparison with those of non-pregnant women.     

Condensed thienopyrimidines. II. Synthesis and gastric antisecretory activity of thiazole and polymethylene condensed thienopyrimidine derivatives

Thiazolo[3,2-a]thieno[3,2-d]-, [3,4-d]- and [2,3-d]pyrimidin-5-one derivatives (6, 11 and 16), and polymethylene condensed thieno[3,2-d]-, [3,4-d]- and [2,3-d]pyrimidin-5-one derivatives (19-21), in which the oxygen atom of the oxazolidine moiety in 3 was replaced by a sulfur atom or methylene groups, were synthesized and evaluated for gastric antisecretory activity in pylorus-ligated rats. The structure-activity relationships of these compounds are discussed.