著者

小林 義郎 岩崎 成夫 関根 康雄 富岡 清

出版者

公益社団法人 日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.26, no.11, pp.1113-1118, 1990-11-01 (Released:2018-08-26)

著者

小林 義郎

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.100, no.8, pp.779-791, 1980-08-25 (Released:2008-05-30)

参考文献数

18

被引用文献数

1

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Studies on organic fluorine compounds in our laboratory are summarized. New methods for the synthesis of fluorine compound are as follows ; 1) fluorination of alcohols with fluorophosphoranes, 2) trifluoromethylation of aromatic and aliphatic halides with trifluoromethyl halides and copper powder, and 3) cycloaddition reaction with novel fluorine reagents like hexafluorobutyne. Reactions of trifluoromethyl aromatic compounds were investigated thoroughly, and some interesting characters of fluorine compounds were revealed. Trifluoromethylated valence bond isomers of aromatic compounds were synthesized, and some novel reactions of these highly strained compounds were shown. The characteristics that a fluorine atom is a small substituent and that a carbon-fluorine bond is very strong were used to study the metabolism of vitamin D3. Some interesting reactions by use of fluorine compounds as synthetic reagents are also discussed.

著者

小林 義郎 熊懐 稜丸 大沢 昭緒 山田 猛

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.20, no.8, pp.1839, 1972-08-25 (Released:2008-03-31)

被引用文献数

15 20

著者

小林 義郎 熊懐 稜丸 大沢 昭緒 村上 慎一 中野 隆治

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.26, no.4, pp.1247-1249, 1978-04-25 (Released:2008-03-31)

被引用文献数

31 45

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Photochemical trifluoromethylation of pyridine gave a mixture of three (trifluoromethyl) pyridines. Pyrrole and N-methylpyrrole were trifluoromethylated in α-position. Benzene gave very low yield of benzotrifluoride.

著者

小林 義郎 熊懐 稜丸 佐藤 進 原 伸祀 近見 永一

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.18, no.11, pp.2334-2339, 1970-11-25 (Released:2008-03-31)

被引用文献数

39 65

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Trifluoromethyl iodide reacts with aryl halide in the presence of copper powder to give aryltrifluoromethane derivatives in a fairly good yield. This newly observed reaction is applicable to heterocyclic halides as well as benzene derivatives. Activities of halides are in the following order of readiness : iodide>bromide>chloride. Effects of solvents and natures of copper were examined.

著者

小林 義郎 田口 武夫

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.43, no.11, pp.1073-1082, 1985-11-01 (Released:2009-11-13)

参考文献数

70

被引用文献数

12 13

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Studies on fluorine-modified vitamin D3 analogs : the design, synthesis and biological activity are reviewed. On the basis of the metabolism of vitamin D3 and the characteristic features of fluorine and fluorinated compounds, fluorine-modified vitamin D3 analogs were designed, synthesized and their biological activity was investigated to clarify the physiological significance of the metabolic hydroxylation of vitamin D3.

著者

小林 義郎 熊懐 稜丸 榛沢 雄二

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.37, no.3, pp.183-196, 1979-03-01 (Released:2009-11-13)

参考文献数

50

被引用文献数

2 2

---

Trifluoromethyl group shows a stabilizing effect on the compounds which would be unstable if they had no trifluoromethyl group. This review is concerned with two faces of the chemistry of trifluoromethylated valence bond isomers of aromatic compounds : Diels-Alder and 1, 3-dipolar reactions planned for the conversion of hexakis (trifluoromethyl) benzvalene to the corresponding tetrahedrane and the synthesis of new valence bond isomers of heteroaromatic compounds. In the former, the tetrahedrane itself could not yet be isolated, but the formation of tetrakis (trifluoromethyl) cyclobutadiene and new valence isomers of oxepin was confirmed. In the latter, Dewar thiopene, Dewar pyrrole, Dewar pyridine, and diphosphabenzvalene with trifluoromethyl groups were synthesized and their reactions were discussed. The effect of trifluoromethyl group is not limited to the strained compound. Thus, tetrakis (trifluoromethyl) -1, 4-diphosphabenzene, the first example of diphosphabenzenes, was synthesized.

著者

小林 義郎

出版者

東京大学

巻号頁・発行日

1959

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博士論文

著者

赤羽 健司 上條 哲聖 飯塚 欣二 田口 武夫 小林 義郎 木曽 良明 梅山 秀明

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.36, no.9, pp.3447-3452, 1988-09-25 (Released:2008-03-31)

参考文献数

31

被引用文献数

3 4

---

The structure-activity relationship of acyl-His-trifluorinated leucinol derivatives as inhibitors of human renal renin is discussed based upon the tertiary structure of human renin, which was deduced from the crystal structure of penicillopepsin by assuming structural similarity. The structural requirements for the inhibitors and possible interactions at the renin binding site are discussed.

著者

小林 義郎

出版者

清和大学短期大学部

雑誌

清和女子短期大学紀要 (ISSN:02873141)

巻号頁・発行日

vol.28, pp.67-72, 2000-01-31

著者

小林 義郎 熊懐 稜丸 田口 武夫

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.38, no.11, pp.1119-1129, 1980-11-01 (Released:2010-01-22)

参考文献数

36

被引用文献数

3 4

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First, characteristics of a carbon-fluorine bond from the biological point of view are summarized with some examples : mimic effect, protective fluorination, irreversible conjugation with enzyme, increased lipophilicity and so on are presented. Secondly, some approaches to biologically active compounds utilizing the above characteristics are shown by the examples of trifluoromethylated nucleoside derivatives and fluorinated vitamin D3 analogues.