Stereoselective synthesis of (2s,3s,4r)-4-amino-3-hydroxy-2-methyl-pentanoic acid, an amino acid constituent of bleomycin, by aldold condensation)
Masatoshi NaritaMasami OtsukaSusumu KobayashiMasaji OhnoYōji UmezawaHajime MorishimaSei-ichi SaitoTOMOHISA TAKITAHAMAO UMEZAWA
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Allyltitanocene complexes can be generated by reacting pentafulvenes with DIBAL-H and Cp2TiCl2. Their coupling with aldehydes affords homoallylic alcohols in a highly regio- and stereoselective manner. The potential of this method for the stereoselective synthesis of cyclopentane derivatives is illustrated.
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目的:学习保护的效果一 导出triptolide ， novelcompound ，( 5R ) -5-hydroxytriptolide(LLDT-8),on 导致bleomycin 的肺 fibrosis.Methods : C57BL/6 micereceived bleomycin 的 intratracheal 注射并且然后与 LLDT-8 被对待( 0.5,1,2mg/kg ， ip )为 7 或 14 连续 days.The 身体重量损失和观察的肺索引 augmentationwas 从前每日；包括微分房间的煽动性的反应在 bronchoalveolar lavage 数 ofneutrophils ，巨噬细胞，和淋巴细胞液体( BALF )，啜
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The indication for treatment with Bleomycin in gynaecological tumors is as yet not well defined. At present Bleomycin is primarily used for advanced gynaecological malignancies. Results of our investigations show that the individual affinity of gynaecological tumors to Bleomycin is very variable. In subsequent investigations it should therefore be determined whether the accumulation of radio-Bleomycin and the sensitivity of a gynaecological malignant tumor to Bleomycin therapy show a positive correlation. The probable chances of success of a course of chemotherapy with Bleomycin could then be predicted.
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A remarkably stereoselective reduction of a γ-hydroxyketone with two equiv. of lithium triethylborohydride has been observed and this effect has been suggested to originate from 'chelation control'; the reaction has been utilised in a short stereoselective synthesis of ancistrofuran.
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Intralesional injection of bleomycin sulphate is a safe and almost completely effective treatment for warts. One thousand and fifty-two warts were injected with bleomycin sulphate, resulting in a cure rate of 99.23% after 12 weeks. No systemic manifestations of bleomycin toxicity were observed during the trial. After failure of injection of saline, it would appear that it is the cytotoxic effect of bleomycin and not the physical interference with the wart that effects the cure.
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人膀胱癌の1つの治療体系の確立を目的として, 温水潅流法による温熱 (Hyperthermia) 療法 (42～43℃) の臨床的検討を行つた. 温熱単独, 温熱と bleomycin の併用療法, 温熱と放射線の併用療法, 温熱と放射線と bleomycin の3者併用療法の4通りの療法を受けた34例の膀胱癌 (移行上皮癌) 患者につき, 治療効果, 副作用, 生体免疫能におよぼす影響につき検討を行つた.温熱単独では6例中2例に, 温熱と bleomycin の併用では4例中1例に, 温熱と放射線の併用では9例中5例に, 温熱と放射線と bleomycin の3者の併用では15例中12例に, 腫瘍の明らかな縮小や消失の治療効果が認められた.副作用は膀胱刺激症状, 尿道痛が主なものであり, 重篤な副作用は認められなかつた.PHAや Con Aによるリンパ球幼若化能等を指標として生体免疫能におよぼす温熱療法の影響を検討した. 温熱と放射線の併用, および温熱と放射線と bleomycin の3者併用療法を受けた患者のこれら指標は, 治療の経過に伴つて抑制されたが, 放射線単独療法を受けた患者のそれとは差が認められなかつた.これらより, 膀胱癌の温熱療法に特に温熱と放射線と bleomycin の3者の併用療法は充分臨床応用が可能と考えられた.
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Abstract In the presence of a catalytic amount of several trityl salts, 2,3,5-tri-O-benzyl-d-ribofuranose smoothly reacted with alcohols to give various β-ribofuranosides in high yields with high stereoselectivity while reversed stereoselectivity was observed in the coexistence of lithium perchlolate.
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