著者

長瀬 博 河合 孝治

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.47, no.4, pp.374-383, 1989-04-01 (Released:2009-11-13)

参考文献数

40

被引用文献数

1 3

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Abnormal enolization reaction of naltrexone was found and the reactivity was applied to the syntheses of highly selective opioid receptor antagonists. Further, structure activity relationship of these antagonists was discussed.

著者

植木 正彬

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.44, no.3, pp.219-228, 1986-03-01 (Released:2009-11-13)

参考文献数

52

被引用文献数

1 1

---

Since the discovery of two endogenous opioid peptides, Met-and Leu-enkephalins, a lot of works have been done to develop better analgesics without side-reactions. By now many highly potent analogues of enkephalins have been designed and synthesized. But, pure analgesics have not so far been obtained. It is mainly because of the complexity of opioid ligands and their interactions with multiple receptors. In addition recent knowledge of enhancing effects of peptidase inhibitors on the potency of opioid peptides prompts us to reexamine all the accumulated pharmacological data.

著者

福山 勝

出版者

社団法人 有機合成化学協会

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.23, no.8, pp.700-712, 1965-08-01 (Released:2011-03-01)

参考文献数

77

著者

辻 篤子

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.61, no.5, pp.530-531, 2003-05-01

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「おもしろいなあ.だって, グリーンとケミストリーって, ほとんど逆の概念でしょう?」.科学部のある記者が, 「グリーンケミストリー」の話を聞いてこんな感想をもらした.2年前の秋のことだ.さらにその記者は続けて, 「つまりは, 化学のイメージ挽回作戦ですね」.なるほどそういう見方もあるのかと, ちょっと驚いたが, 化学物質による環境汚染や毒性と結びつけて考えられがちな化学のイメージを考えれば, さほどとっぴな見方ではないかもしれないと, 思い直した.この記者は文科系出身, とくに化学にくわしいというわけではなかったが, それだけに, ごく普通の感覚に近いといえるかもしれない.

著者

木村 午朗 近岡 貞志

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.23, no.3, pp.241-247, 1965

被引用文献数

1

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1, 7-Diaminoheptane has been synthesized from 1, 7-dichloroheptene-3 through ammonolysis followed by hydrogenation. For the formation of the desirable primary amine in the ammonolysis reaction, the following conditions have been proved favorable: use of liguid ammonia with or without a small amount of water or an organic solvent rather than aqueous ammonia, use of an excessive amount of ammonia, reaction temperatures above 80°C, in case of aqueous ammonia and above 60°C, in case of liquid ammonia, the effects of temperature upon yield being small over the range 100-140°C, and efficient agitation to ensure thorough contact of the reactants. The maximum yield of 1, 7-diaminoheptene-3, however, was 72-73%. Attempts to improve the yield resulted in the formation of secondary and tertiary polyamine by-products. 1, 7-Diaminoheptene-3 thus obtained was readily hydrogenated into 1, 7-diaminoheptane in 96% yield in the presence of Raney nickel catalyst under the atmospheric pressure as well as under pressure. Condensation polymerization of 1, 7-diaminoheptene-3 and that of 1, 7-diaminoheptane with urea proceeded smoothly and white solid polyureas with good spinning properties were obtained. The former polyurea showed m.p. 216°C, d<SUP>20</SUP>4 1.13 and the latter, m.p. 260°C, d<SUP>20</SUP> 1.12. The melting point of the polyurea obtained from 1, 9-noname. thylenediamine fell between that of the two polymers, and the specific gravity of the former was approximately 5% less than that of the latter two. The fiber of 1, 7-diaminoheptene-3 polyurea as well as that of 1, 7-diaminoheptane polyurea showed a slightly better dyeing properties with acidic and dispersing dyes than 1, 9-nonamethylenediamine polyurea, though other properties of those three types of fiber were alike.

著者

中山 重蔵

出版者

社団法人 有機合成化学協会

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.28, no.2, pp.132-143, 1970-02-01 (Released:2010-01-28)

参考文献数

62

被引用文献数

1 4

著者

藤野 政彦

出版者

社団法人 有機合成化学協会

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.52, no.5, pp.439-444, 1994-05-01 (Released:2009-11-16)

参考文献数

6

被引用文献数

1

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Biologically active peptide have potential therapeutic applications in the treatment of diseases caused by peptide deficiency. However, there are only a few peptide drugs, Elcitonin (a calcitonin derivatives for osteoporosis, Asahikasei), Hirutonin (TRH tartrate for prolonged disturbance of consciousness, Takeda) and Leuplin (a highly potent LH-RH derivative for prostate cancer/endometriosis, Takeda) There are two serious drawbacks to using peptide derivatives as drugs : their poor oral bioavailability and their short duration of activity. Although the latter can be overcome by studing various derivatives, the development of orally active peptide derivatives is almost impossible. I would like to describe briefly the process of the research and development of “Leuplin Depot”, once-a-month depot type formulation of super agonist of LH-RH.

著者

松田 知子 原田 忠夫 中村 薫

出版者

社団法人 有機合成化学協会

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.59, no.7, pp.659-669, 2001-07-01 (Released:2010-01-22)

参考文献数

17

被引用文献数

3 4

---

Biocatalyst has been attracted increasing attention for asymmetric synthesis due to the high enantioselectivities and environmentally friendliness. We have been developing methods using a fungus, Geotrichum candidum, which has many enzymes catalyzing the enantioselective oxidation and reduction reactions of non-natural substrates. These enzymes in the resting or dried cells were used in an organic solvent, supercritical carbon dioxide, or aqueous media for oxidation, reduction or deracemization reactions. The usefulness of these methods was also demonstrated in the preparation, on a multi-gram scale, of optically pure alcohols.The effect of fluorine substituents on the enantioselectivity of the reduction using the dried cell was also investigated thoroughly, and it was found that the reduction of trifluoromethyl ketones affords (S) -trifluoromethyl carbinols in excellent ee, whereas the reduction of methyl ketones gives the corresponding alcohols of the opposite configuration in excellent ee. The enzymes in the cells were separated to investigate the origin of different enantioselectivities between the methyl and trifluoromethyl ketones.

著者

鈴木 啓介

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.46, no.4, pp.367-377, 1988-04-01 (Released:2009-11-13)

参考文献数

28

被引用文献数

11 20

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Contrary to the firm and long-standing credence on the involvement of racemization, the “cationic” 1, 2-rearrangement reactions may proceed stereospecifically under suitable reaction conditions to allow the complete 1, 2-chirality transfer. This fact provides a solid basis for the development of a novel and useful synthetic reactions to achieve the highly selective acyclic steoeocontrol. This paper deals with a survey of the new synthetic methodology based on the novel 1, 2-rearrangements under Lewis acidic conditions as well as the newly exploited silicon-directed relative streocontrol, which would find a broad applicability in the highly stereoselective synthesis of a wide variety of useful compounds including chiral pheromones, macrolides, and so on.

著者

平川 芳彦

出版者

社団法人 有機合成化学協会

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.35, no.5, pp.325-331, 1977-05-01 (Released:2009-11-13)

参考文献数

10

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Sulfur (S) is an element of 15th largely existed in earth's crust, 10th in universe, and 7th in human body. S circulates the environmental sphere in various chemical forms, but SO2 in atmosphere is largely responsible by human burning of S contained fuels and minerals. Underground resources of S and production type of S differ country by country. S content in crude oil varies ranging from less than 0.1% to more than 5% in every oilfield. Large S content unexpected from biological source theory of oil origin might be explained by that melted mineral origin elementary S in underground has met and dissolved into highly aromatic or naphthenic fractions of crude oil and secondarily converted to S compounds. Though supply of S as fertilizer to fields has been decreased, but SO2 has played an important role of natural supply of S to the earth, especially in highly populated metropolitan areas.

著者

長谷川 元 三浦 剛毅 渡谷 哲朗 洪 南基

出版者

社団法人 有機合成化学協会

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.56, no.9, pp.773-780, 1998-09-01 (Released:2009-11-16)

参考文献数

52

被引用文献数

1 1

---

To date, the resolution of racemic mixture via diastereomeric salt formation has been the most commonly used industrial technique.We have synthesized and applied new resolving agents for industrial application. Practical approach to the developments is as follows. Optically active 2-phenoxypropionic acid and tartranilic acid are readily employed for the resolution of bases, and 1-benzylamino-3-phenoxy-2-propanol for the resolution of acids.

著者

大饗 茂 北尾 弟次郎

出版者

社団法人 有機合成化学協会

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.19, no.12, pp.880-899, 1961-12-01 (Released:2010-10-20)

参考文献数

117

被引用文献数

2

著者

時田 澄男

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.45, no.11, pp.1129-1140, 1987-11-01 (Released:2009-11-13)

参考文献数

129

被引用文献数

1 1

---

It is becoming commonplace for organic chemists to have their own microcomputers. In this article, softwares for such users to carry out two or three dimentional input to a computer, graphic display of molecular structures, and molecular orbital calculations are reviewed (129 references).

著者

中馬 寛

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.45, no.11, pp.1098-1106, 1987-11-01 (Released:2009-11-13)

参考文献数

62

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The function of a bioactive peptide is often dictated by the bioactive conformation that fits into its receptor. Conformational energy calculations (Molecular Mechanics) as well as various experimental methods have been used for this purpose. On the other hand, recent molecular dynamics simulations of proteins have provided us the new dynamic picture of protein structures. These theoretical methods are thought to play an important role in elucidating the receptor mediated events of bioactive peptides and in the drug design based on their conformations.The objectives of this review are (1) to provide an introduction to the field of conformational energy calculations and molecular dynamics for peptides; (2) to explain how we can find the bioactive conformation by using conformational energy calculations; and (3) to describe the application of the above methods for defining the bioactive conformation of an opiate peptide, Morphiceptin, as one example.

著者

桐野 修 高山 千代蔵

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.45, no.11, pp.1107-1118, 1987-11-01 (Released:2009-11-13)

参考文献数

40

被引用文献数

1 3

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This article describes the structure-activity relationships of (i) herbicidal N-benzylphenylacetamides, (ii) herbicidal N-chloroacetyl-N-phenylglycinates, (iii) herbicidal N-phenylureas, (iv) herbicidal N-benzylacylamides, (v) herbicidal and fungicidal N-benzylacylamides, and (vi) fungicidal N-phenylimides analyzed quantitatively with substituent parameters and regression techniques. The activity-activity correlations between activities against different species of weeds and fungi are examined on the basis of structure-activity relationships. The application for the design of new agrochemicals with wide-spectrum and/or selectivity is discussed.

著者

高橋 由雅 佐々木 慎一

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.45, no.11, pp.1087-1097, 1987-11-01 (Released:2010-01-22)

参考文献数

15

被引用文献数

3

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It is well known that chemical structure diagram or three-dimensional structure of a compound molecule involves much information related to biological activity, reactivity, or various physicochemical properties on itself. It is a very important thing in a wide range of chemical research to compare the chemical compounds on the basis of such structural information. Especially, in the area of structure-activity studies, to investigate structural feature such as functional groups or substructural fragments, common to a group of chemical compounds exhibiting a particular biological activity often provides us with very useful and objective information which may be resulted in hypothetical pharmacophore.In this article, a couple of approaches for the automated recognition of common structural patterns among drug molecules will be described. One is related to the maximal common substructure search which can be used to find some topological pharmacophore, and the other one is for the common geometrical pattern search in which three-dimensional geometry of molecules are taken account. The latter approach may be used to identify a certain topographical or three-dimensional pharmacophore. The basic algorithms and related software systems will be summarized with some illustrative examples.

著者

中村 栄一 深沢 義正

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.45, no.11, pp.1044-1054, 1987-11-01 (Released:2009-11-13)

参考文献数

63

被引用文献数

1 1

---

合成反応の予測性を高めることは研究の目的, 環境を問わず, 有機合成の大きな目標である。これまでも有機合成化学者は試行錯誤から得た経験に反応論や構造論を加味して反応の予測性を高める努力を行ってきた。最近顕著になってきた新しい流れは, 理論計算を合成化学者自身が行うことでこの問題にアプローチしようとする考え方である。過去数年間における計算機や情報ネットワークの普及は目ざましく, 10年前には大型計算機センターでしか出来なかった理論計算, 特に分子力学 (MM) 計算が今や実験室の片隅で行える時代となったことがその背景である。分子や反応に関する情報を計算機によって求める方法としては非経験的分子軌道 (MO) 計算がもっとも優れているが, 今日合成ターゲットとなっているような大きな化合物に関する情報をこの方法で得ることは事実上困難である。パラメータ上の制約のためにまだ比較的限られた化合物への適用しか許されないとはいえ, 計算の速さと簡単さの点でMM計算が1つの現実的な選択である。MM計算から求められる情報は基底状態の分子のある配座でのエネルギーと, そこでの分子の形態である。この2種類の情報を用いて反応生成物の分布の予想と結果の合理的解釈を行うことが計算の目的である。種々のMM計算プログラムが開発されてきたが, 最近の有機合成での応用例は殆んどAllingerらのMM2プログラムが使われている。本総説では身近になったMM2プログラムの有機合成での適用例についてまとめてみたい。

著者

深澤 義正 灰野 岳晴

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.54, no.5, pp.419-426, 1996-05-01 (Released:2009-11-16)

参考文献数

39

被引用文献数

3 4

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有機合成の標的化合物は複雑な構造を持っているものが多く一般に多段階の反応を経て合成されることが多い。それらの合成経路のうち重要な反応についてその生成物が立体化学を含めて正しく予測されれば, 合成経路の確立に大いに役立ち有機合成の経済効率の向上に著しく寄与するものと思われる。したがって, 信頼性の高い反応予測技術の開発は非常に重要である。ここで紹介した非経験的分子軌道計算と分子力学計算を組み合わせた遷移状態モデリング法やMC法を用いた溶媒和計算は, その信頼性の高さからいって十分現実的な使用に耐え得るものと思われ今後の発展が期待される。

著者

深澤 義正 笛吹 修治

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.55, no.12, pp.1124-1133, 1997-12-01 (Released:2009-11-16)

参考文献数

28

被引用文献数

3 4

---

Determination of significantly populated conformers in an extremely flexible molecule such as macrocycles is a matter of long standing interest. We have developed a useful and very reliable method for the conformational analysis using a combination of molecular mechanics calculations and chemical shift simulation method. The method utilizes the calculation of the change in chemical shift of a proton produced by nearby substituents. The induced chemical shifts due to anisotropy effect of aromatic ring have been proven to be a useful geometrical probe of structures. Examples of the successful conformational analysis for macrocyclophane and supramolecular complexes of calixarenes with apolar guests including C60 and C70 are presented.

著者

北原 武 宮下 晃

出版者

社団法人 有機合成化学協会

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.46, no.2, pp.179-179, 1988-02-01 (Released:2009-11-13)