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Sato S Komoto T Kanamaru Y Kawamoto N Okada T Kaiho T Mogi K Morimoto S Umehara N Koda T Miyashita A Sakamoto T Niino Y Oka T 《Chemical & pharmaceutical bulletin》2002,50(2):292-297
New muq-opioid receptor (MOR) agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Among the synthesized compounds, 12-[1-[3-(N,N-dimethylcarbamoyl)-3,3-diphenylpropyl]-4-hydroxypiperidin-4-yl]phenoxy]acetic acid (8: SS620) having phenoxyacetic acid and 4-hydroxypiperidine moieties showed the highest agonist potency on the MOR in an isolated guinea-pig ileum preparation, and it also had selectivity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells compared with the same types of delta- and kappa-opioid receptors (DOR and KOR). In addition, compound 8 showed a 10 times more potent MOR agonist activity than loperamide. Furthermore, compound 8 showed a peripheral analgesic activity in vivo screening on rat. 相似文献
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Sato S Ogura Y Miyanaga A Sugimoto T Tanaka K Moriyama H 《Journal of chromatography. A》2002,956(1-2):53-58
Ion chromatography (IC) has been a powerful tool for measuring ionic species in environmental samples such as tap, river and drain waters. Suppressor modules (membrane and disposable column types) have been used for reducing the background of a baseline. A new type of suppressor device, which has a suppressor resin and switching valve was developed. Fresh ionic resin is introduced into a groove for each analysis to perform the suppression of the working eluent. The eluent composition for obtaining higher sensitivity and better resolutions among ionic species and carbonate ion was also investigated. Although carbonate buffers are used for ion separation in general, the separation of carbonate ion from other ions was not achieved. A borate eluent resulted in good resolutions and higher sensitivity. A new column was also developed for obtaining higher column efficiency and resolution. The optimization of anion separation using a new IC system (IC-2001) that consists of a new suppressor device, an anion-exchange column (TSKgel SuperIC-Anion, 150x4.6 mm), an autosampler, a conductivity cell and a pump in a compact module is described. 相似文献
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Kazuhiko Saigo Yukihiko Hashimoto Kazushi Kinbara Atsushi Sudo 《Journal of Chemical Sciences》1996,108(6):555-573
The review describes the mechanism of chiral discrimination of racemic amines upon crystallization and the induction of chirality
in organic reactions by using them as chiral auxiliaries. In order to form conglomerates, which can be resolved into the two
enantiomers upon alternative seeding, both formation and packing of 21-columns are essentially very important. On the other hand, in order to achieve high efficiency in resolution through diastereomeric
salt formation, which is the most practical method, one of a pair of diastereomeric salts derived from a racemic amine and
an enantiomerically pure resolving agent should at least have two 21-columns and planar boundary surfaces in its crystal structure. On the basis of this knowledge, we developed several artificial
chiral auxiliaries such as erythro-2-amino-1,2-diphenylethanol,cis-2-amino-1-acenaphthenol, andcis-2-amino-3,3-dimethyl-1-indanol. These were found to be very efficient chiral auxiliaries in asymmetric inductions: alkylation
of chiral imines, catalytic borane-reduction, and alkylation of chiral N-acylated oxazolidinone. 相似文献
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The synthetic approach to the protopine alkaloids is described. Efficient construction of the alkaloid models 16a and 16b was accomplished by the general synthetic method consisting of photo-oxygenative ring enlargement of tetrahydrobenzindenoazepines 13a and 13b by singlet oxygen and further elaboration of the resultant 10-membered amido-ketone products 14a and 14b. 相似文献
130.
Photolysis of tris(trimethylsilyl)phenylsilane, in alcohols yielded 1-aikoxy-1-phenyl-2, 2,2-trimethyldisilane, dialkoxyphenylsilane, hexamethyldistlane, and trimethylstlane as major products. The formation of the products was explained by a mechanssm which included the consecutive generatinn of phenyltrimethylsilylsilyleses and alkoxyphenylsilylenes. 相似文献