A large-scale preparation route of MX-68, a novel MTX
derivative bearing a dihydro-2H-1,4-benzothiazine moiety and
l-homogulutamic acid, is described. The original route that is
a laboratory-scale synthesis for preclinical study has been
improved. The improved process involves the following features: each step does not use haloalkane solvents, corrosive
reagents, and chromatographic purification, and the formation
of the major impurity at the final step is minimized. This
improvement has enabled us to supply sufficient quantities of
MX-68, which is required for both the toxicity test and the
clinical study.
The effect of phosphorous on intergranular corrosion of type 310 stainless steel at transpassive potential was investigated using phosphorous added ultra high purity type 310 stainless steel. Intergranular corrosion depth was measured by scanning electron microscopic observation. Grain boundaries were observed using three dimensional atom probe. Intergranular corrosion was observed on phosphorous added stainless steel. The sample heat treated at 600 showed severe integranular corrosion morphology. Observation by three dimensional atom probe revealed that grain boundary with high dissolution rate had segregated zone of chromium and phosphorous about 5nm in width, on the other hand, grain boundary with low dissolution rate had no segregated zone. From these results, it is suggested that intergranular corrosion of phosphorous added type 310 stainless steel at transpassive potential is affected by segregation of phosphorous and chromium along grain boundaries.
The deamination of cyclaradine corresponding to a carbocyclic analogue of ara-A having anti-HSV activity by adenosine deaminase was examined under various pressure. The deamination of (+)-and (*)-cyclaradine was remarkably facilitated by high pressure, and the rate was increased with increasing of pressure. However, (-)-cyclaradine was not deaminated even under high pressure.
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