著者
浜名 政和 舟越 和久 執行 洋陸 口野 嘉幸
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.23, no.2, pp.346-350, 1975-02-25 (Released:2008-03-31)
被引用文献数
4 13

The 1, 3-dipolar cycloaddition between quinoline N-oxide (I) and methyl propiolate progressed in the presence of acetic anhydride or hydroquinone to afford methyl α-formyl-2-quinolineacetate (IIa). The reaction with ethyl propiolate in the presence of hydroquinone gave the corresponding ethyl ester (IIb). The reaction of I with methacrylonitrile in the presence of hydroquinone produced cyanohydrin of 2-acetonylquinoline (VIII) or 2-acetonylquinoline (IX) and 2-cyanoquinoline (X). Isoquinoline N-oxide (XI) was less reactive and resisted the reaction with propiolates, but reacted with methacrylonitrile in the presence of hydroquinone to give 1-acetonyl-isoquinoline (XII), 1-cyanoisoquinoline (XIII) and isoquinoline.
著者
浜名 政和 山崎 企善
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.10, no.1, pp.51-54, 1962-01-25 (Released:2008-03-31)
被引用文献数
7 11

Alkaline ferricyanide oxidation of some aromatic N-oxides was examined. Quinoline 1-oxide, lepidine 1-oxide, and isoquinoline 2-oxide were smoothly oxidized to the corresponding N-hydroxy-carbostyrils or-isocarbostyrils. From quinaldine 1-oxide, only a small amount of quinaldinic acid 1-oxide was obtained. In contrast, pyridine and nicotinic acid 1-oxide were not affected by this oxidation procedure.
著者
浜名 政和 山崎 企善
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.11, no.4, pp.415-421, 1963-04-25 (Released:2008-03-31)
被引用文献数
21 31

Quinoline 1-oxides were found to react smoothly with compounds containing reactive hydrogens in the presence of acetic anhydride, producing the corresponding 2-substituted quinolines. The yields were generally good to excellent in the reactions of ethyl cyanoacetate, 1, 3-indandione, diethyl malonate, diethyl nitromalonate, ethyl nitroacetate (e. g. ethyl α-cyano-2-quinolineacetate in 88% yield), but acetone, acetophenone or phenylacetonitrile could not enter into the reaction. The reaction of quinoline 1-oxide using benzoyl chloride instead of acetic anhydride and those of pyridine 1-oxides in the presence of acetic anhydride proceeded similarly but in much lower yields.
著者
浜道 則光 藤多 哲朗 松崎 徹 北尾 有紀 城内 正寿 広瀬 良治
出版者
天然有機化合物討論会実行委員会
雑誌
天然有機化合物討論会講演要旨集 37 (ISSN:24331856)
巻号頁・発行日
pp.79-84, 1995-09-01 (Released:2017-08-18)

Mycestericins D (1), E (3), F (2) and G (4), new immunosuppressants, were isolated from the culture broth of Mycelia sterilia ATCC 20349. The immunosuppressive activities of 1 and 2 exhibited an IC_<50> of 16nM and 120nM against mouse allogeneic mixed lymphocyte reaction (MLR), respectively, while 3 and 4 exhibited an IC_<50> of 13nM and 370nM, respectively. The proposed structures were unambiguously confirmed by spectroscopy, chemical evidence and total synthesis. Their absolute configurations have been determined by comparison of their CD spectra with those of synthetic compounds (R and S)-9 prepared from methyl (2S, 4R)-2-tert-butyl-3-formyl-oxazolidine-4-carboxylate (5) and stearoyl chloride. Thus, mycestericins D (1) and F (2) were assigned to be 2 (S), 3 (S) configurations, while mycestericins E (3) and G (4) were 2 (S), 3 (R) configurations. The first total synthesis of mycestericins have been achieved from 5 and 1,8-octanediole (10). The alkyl chain moiety 21 was prepared in 12 steps from 10 by straightforward reactioin. The key intermediate 22 obtained from 5 and 21 could be converted to the desired final compounds. Stereoselective reduction of the ketone 22 with Zn(BH_4)_2 or NaBH_4 provided the (R)-hydroxy 23, the protecting groups of which were removed with 10% MeOH in CF_3COOH, followed by hydrolysis of 24 to give mycestericin E (3). On the other hand, mycestericin D (1) was synthesized from 22 by deprotection, followed by reduction of 25 with Me_4NBH(OAc)_3 and then hydrolysis of 26. Hydrogenation of mycestericin D (1) and E (3) provided the corresponding F (2) and G (4).
著者
山岸 三郎 小山 泰正 深草 佑一 興村 伸夫 大石 洵一 浜道 則光 新井 正
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.91, no.3, pp.351-357, 1971-03-25 (Released:2008-05-30)
参考文献数
24
被引用文献数
14 21

The metabolites of Streptomyces luteoreticuli KATOH et ARAI were investigated. Four new compounds, luteoreticulin, (V), C19H19O5N, luteothin, (VI), C22H25O5N, metabolite X, (X), C15H12O3N2, and metabolite XI, (XI), C15H14O3N2, were isolated from the acetone extract of the mycelial cake. 1-Methoxyphenazine (VII) and methyl phenazine-1-carboxylate (IX), which were first isolated from natural origin, were obtained in addition to aureothricin (I), thiolutin (II), aureothin (IV), and 1, 6-dimethoxyphenazine (VIII). The other two metabolites (III and XII) were also isolated but not identified.
著者
藤多 哲朗 浜道 則光 内田 秀治 加治 隆史 松本 範正 広瀬 良治 北尾 郁紀 松崎 徹 千葉 健治
出版者
天然有機化合物討論会実行委員会
雑誌
天然有機化合物討論会講演要旨集 38 (ISSN:24331856)
巻号頁・発行日
pp.727-732, 1996-09-02 (Released:2017-08-18)

2-Aminoalcohol was shown to be the minimum essential structure for the immunosuppressive activity of 2-alkyl-2-aminopropane-1,3-diol, which was generated by modification of ISP-I (1: myriocin, thermozymocidin). 2-Aminoalcohols 4a-h were examined for immunosuppressive activity on mouse allogeneic mixed lymphocyte reaction (MLR) in vitro. The series showed a bell-shaped relationship between the activity and the carbon numbers. Among them, 2-aminohexadecanol (4c) was the most potent. In order to investigate relationship between the activity and the configuration at C-2 in 2-aminoalcohol, (R)- and (S)-isomers of 4c, 2-aminoeicosanol (4h) and 2-amino-4-(4-octylphenyl)butanol (5) were prepared and examined for the activity on mouse allogeneic MLR. As a results, the (R)-isomers were more potent the (S)-isomers, and (R)-4c displayed comparably activity to FTY720 (3), which is expected as a powerful candidate for safer immunosuppressant for organ transplantations and for the treatment of autoimmune diseases.
著者
宮田 竜彦
出版者
分子シミュレーション研究会
雑誌
アンサンブル (ISSN:18846750)
巻号頁・発行日
vol.17, no.2, pp.98-104, 2015

溶液の熱力学的安定性を議論する際,最も重要な物理量のひとつは溶媒和自由エネルギーである.3D-RISM 理論は溶質分子周りの溶媒の分布関数を記述する統計力学理論のひとつであり,分布関数から溶媒和自由エネルギーを求めることができる.3D-RISM 理論の問題点のひとつは溶質の内部自由度凍結であるが,著者らはMD 法と組み合わせる方法でこの問題の解決を試みた.また,3D-RISM 理論は精度の問題も抱えている.溶媒和自由エネルギーの高精度化のためには,LJ 項の高精度化が重要であることが既往の研究から示唆されていたが,最近,著者らはLJ 項の高精度化の糸口を見つけた.この発見は,LJ 系においてブリッジ関数の満たすべき必要条件と解釈できるものである.
著者
浜道 則光 宮坂 貞
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.38, no.12, pp.3253-3256, 1990-12-25 (Released:2008-03-31)
参考文献数
21
被引用文献数
1 3

Substituent and solvent effects on the tautomeric equilibration (E/Z) of α-(N-alkyl and -arylaminomethylene)-9-(methoxymethyl)-9H-purine-6-acetonitriles (3a-q) have been studied by means of proton nuclear magnetic resonance spectroscopy in protic and aprotic solvents at 25°C. In chloroform-d these compounda (3a-q) exist mainly as the E-form. On the other hand, in methanol-d4 or dimethylsulfoxide-d6 the alkylamines (3a-c), phenylamine (3e), meta- or para-substituted phenylamines (3f-j) and 2, 6-disubstituted phenylamines (3p and q) exist mainly as the Z-form, while the trityl compound (3d), and ortho-substituted compounds (3k-o) showed a predominance of the E-form.
著者
五島 史行 鈴木 法臣 原 真理子 土橋 奈々 守本 倫子
出版者
一般社団法人 日本耳鼻咽喉科学会
雑誌
日本耳鼻咽喉科学会会報 (ISSN:00306622)
巻号頁・発行日
vol.120, no.3, pp.285, 2017-03-20 (Released:2017-04-19)

掲載号:118巻7号,860-866頁参考文献にしたがって5歳以上と5歳未満の2群に分けて解析せねばならないところを誤って7歳未満と7歳以上に分けて解析したため,上記論文を取り下げたい旨の申請が著者からあり,これを承認した.
著者
清莊臻鳳撰
巻号頁・発行日
vol.[2], 1666
著者
浜道 則光 宮坂 貞
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.38, no.7, pp.2018-2019, 1990-07-25 (Released:2008-03-31)
参考文献数
7
被引用文献数
1 1

6-Dicyanomethylene-9-tetrahydrofuranylpurine (4), which was obtained by the reaction of 9H-1, 6-dihydropurine-Δ6, α-propanedinitrile (3) with 2, 3-dihydrofuran, has been catalytically hydrogenated to the α-(aminomethylene)-9-(tetrahydrofuran-2-yl)-9H-purine-6-acetonitrile (5) in good yield using N, N-dimethylformamide-benzene as a solvent over Pd-C under medium pressure. Substitution of 5 with amines gave the corresponding alkylaminomethylene purines (6 and 7). Reaction of 5 with hydrazine gave the pyrazole derivative (8).
著者
Hiroyasu Kaya Jun Ozaki Hirokazu Okumura
出版者
The Japanese Society of Internal Medicine
雑誌
Internal Medicine (ISSN:09182918)
巻号頁・発行日
pp.0269-17, (Released:2018-03-09)
参考文献数
22
被引用文献数
4

Objective This study retrospectively evaluated fungal dissemination due to hospital reconstruction and explored effective methods of predicting an outbreak. Methods Patients suspected of having invasive aspergillosis were tested for Aspergillus galactomannan antigen before and after reconstruction, and the mean values of three months of testing for positive patients were determined. The characteristics of patients with aspergillosis during this period were also assessed. Results Forty-five patients were positive for Aspergillus antigen (>0.5 cut-off index) from January 2013 to December 2014. Mean Aspergillus antigen values significantly increased following reconstruction (p<0.05). Three patients developed pneumonia due to Aspergillus and were diagnosed with "probable" invasive aspergillosis according to the EORTC/MSG criteria. We also discovered that the anteroom to contain dust was not prefabricated and a negative pressure system to remove dust was not used. After construction of the unit, no new cases of aspergillosis were diagnosed. Conclusion Many Aspergillus spores may be transiently floating during hospital reconstruction. Therefore, monthly surveillance with frequent serum galactomannan antigen testing to predict outbreaks is necessary. Surveillance of all patients in the hematology ward is especially important. Reconsideration of prophylactic antifungals may also be necessary during hospital reconstruction.

1 0 0 0 OA 内寄合留 20巻

出版者
巻号頁・発行日
vol.[6] 寛政十一己未年十一月六日・十八日・廿七日 月番松平周防守,
著者
山中 章義 鞠 錦 笠原 恭子 山本 嘉昭 吉田 彌太郎
出版者
近畿産科婦人科学会
雑誌
産婦人科の進歩 (ISSN:03708446)
巻号頁・発行日
vol.63, no.2, pp.112-120, 2011 (Released:2011-06-27)
参考文献数
50

骨髄異形成症候群 myelodysplastic syndorme (MDS)は,造血幹細胞の異常クローン増殖により汎血球減少と無効造血をきたし,進行性・治療抵抗性のため予後不良な疾患である.MDSは妊娠中に増悪することもあり,子宮内胎児発育遅延や胎児機能不全等の合併症の発生リスクが高くなるとされている.今回われわれはMDS合併妊娠で,分娩周辺期の血小板輸血により母児を安全に管理し得た.本邦での過去の症例51例と合わせて報告する.症例は29歳,初産婦.2年前よりMDSに対し血液内科にて経過観察中であった.白血球や赤血球の著明な減少は認めなかったが,血小板減少を認めていた.近医にて妊娠判明し,妊娠12週で当科紹介受診となった.徐々に血小板が減少したため,妊娠29週より入院管理とした.妊娠中出血傾向を認めなかったため,血小板輸血は行わなかった.妊娠37週1日に選択的帝王切開術施行したが,術直前および術直後に血小板輸血を行い,術中および術後に出血傾向はなかった.母児ともに経過観察中であるが,MDSの増悪や新生児への影響は現在のところ認められていない.これまでのMDS合併妊娠の報告では,治療抵抗性の貧血を認め,妊娠中に初めてMDSと診断された症例が53%(28/52)であった.合併症として妊娠高血圧症候群や胎児機能不全が多い傾向にあった.妊娠時や分娩時に出血傾向はそれほど認められなかったが,ほとんどの症例で血小板輸血を行った.十分な血液製剤が確保できるのであれば,産科的禁忌がない限り経腟分娩は可能と考えるが,高次医療施設での妊娠・分娩管理が必要と考える.妊娠中に治療抵抗性の貧血や血球減少を認めた場合は,血液内科医と連携し速やかに骨髄穿刺にて診断を行い,MDSと診断されれば慎重な妊娠・管理が必要である.〔産婦の進歩63(2):112-120,2011(平成23年5月)〕
著者
小島 拓也 鈴木 教和 社本 英二
出版者
公益社団法人 精密工学会
雑誌
精密工学会学術講演会講演論文集 2011年度精密工学会秋季大会
巻号頁・発行日
pp.315-316, 2011 (Released:2012-03-05)

不等ピッチ/リードエンドミルは自励びびり振動の発生原因である再生効果を抑制し得るが,条件によっては効果的に自励びびり振動を抑制し得ないこともある.本研究では,Multi-Frequencyモデルを用いて,これらの工具を用いた場合の安定限界に対する半径方向切込みの影響について検討した.解析の結果,切込みが浅くモードカップリングが生じにくい条件で自励びびり振動を効果的に抑制し得ることを確認した.