Wire-grown, massive amorphous boron heated in inert atmospheres at pressures of 10-5 to 10-6 torr was converted to the ß-rhombohedral modification at 1000 °or above. The extent of conversion depended on the time of treatment and was inhibited by the presence of 50 torr of argon or 30 torr of nitrogen. It is concluded that the conversion takes place by a surface diffusion mechanism. The stepwise development of a ß-rhombohedral X-ray diffraction pattern suggests that massive amorphous boron may be a microcrystalline deposit of this particular modification of the element.
Twenty-six new CY-( alkglaminomethyl)-2-phenyl-4-quinolinemethanols have been synthesized for evaluation of their antimalarial activity. Kine new 2-phenylcinchoninic acids were prepared together with the several intermediates leading to the amino alcohols. An anomalous orientation effect of methoxy substitution in the anilines used in the Doebner reaction for the preparation of cinchoniriic acids was noted. In the environment of the Doebner reaction the methoxy group became a meta-directing group rather than ortho,para directing. The position of the methoxy substitution in the 2-phenyl-4-quinolinemethanols prepared influenced the basicity of the quinoline nitrogen. The heterocyclic nitrogen in 2-(4-methoxyphenyl)-and 7-methoxy-2-phenyl-substituted 4-quinolinemethanols was seemingly equivalent in base strength to the aliphatic tertiary nitrogen in the amino alcohol side chain in contrast to similar compounds in which there was chloro substitution in these positions. Twenty of the compounds have been tested for antimalarial activity toward Plasmodium berghei in mice. Single doses of from 40 to 640 mg/kg prolonged the life of infected mice to at least 30 days, whereas the survival time of controls was 7.0 f 0.5 days. The one dioctylamino derivative was inactive a t a dose of 640 mg/kg. The diethylamino-1-methylbutylamino derivative was toxic a t a dose of 40 mg/kg. The compounds were phototoxic to albino mice a t dosage levels from 5 to 400 mg/kg. ( I ? ) A . 1, \ViI~ls, Ow. Reaclzons, 2, 107 (lW4). Jlay 196s ANTIMALARIAL 2-PHE,hjYL-4-61UINoLl~~M~~l~HANOL8 429 -----A -COCl Reaction Yield,
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