- Photobase generator
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The object of the present invention is to provide a photobase generator capable of efficiently generating amines (tertiary amines and amidine) high in catalytic activity by sensing light with a wavelength of from 350 to 500 nm (especially, from 400 to 500 nm). The present invention is a photobase generator characterized in being represented by general formula (1) or (2). Y+ is a quaternary ammonio group of general formula (3) to (5), and X? is a counter anion selected from among a borate anion, a phenolate anion, and a carboxylate anion.
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Page/Page column 27
(2013/02/27)
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- Synthesis of N-(9H-xanthen-9-yl)aminoalkanamide and N-(9H-thioxanthen-9-yl)aminoalkanamide derivatives and their in vitro evaluation as potential intercalators and antitumor drugs
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A series of new N-(9H-xanthen-9-yl)aminoalkanamide and N-(9H-thioxanthen-9-yl)aminoalkanamide derivatives was synthesized and evaluated as potential intercalators by measuring their DNA binding affinity. They were also tested for cytotoxic activity against L1210. The results suggest that the cytotoxicity of these molecules was not due to an intercalating mechanism.
- Filippatos,Papadaki-Valiraki,Todoulou,Jacquemin-Sablon
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- Synthesis and antitumor activity of some new 2-chloroethylnitrosoureas
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The synthesis of a series of N-(2-chloroethyl)-N'-(9H-xanthen-9-yl)-N-nitrosoureas and N-(2-chloroethyl)-N'-(9H-thioxanthen-9-yl)-N-nitrosoureas is described. The title compounds were evaluated against NSCLCN6 L16 bronchial epidermoid carcinoma in vitro and some of them were found to be active. N-(2-chloroethyl)-N'-(2-methoxy-9H-xanthen-9-yl)-N-nitrosourea (8e) was active against leukemia P388 tumor system in mice.
- Filippatos,Papadaki-Valiraki,Roussakis,Verbist
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p. 451 - 456
(2007/10/02)
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- Gas phase generation and cyclisation reactions of some o-substituted phenyl radicals
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Flash vacuum pyrolysis of the allyl esters 2 (X=O, S, CH2, CO) at 900°C (10-2 Torr) gives dibenzofurans, dibenzothiophenes, fluorenes, and fluorenones respectively as the major products. The mechanism involves the phenyl radical intermediates 1 which equilibrate by intramolecular hydrogen transfer via six-membered transition states, prior to cyclisation.
- Cadogan,Hutchison,McNab
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p. 7747 - 7762
(2007/10/02)
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- TRICYCLIC NEUROLEPTICS: SYNTHESIS OF METABOLITES OF ISOFLOXYTHEPIN AND SOME RELATED COMPOUNDS
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The isofloxythepin(I) metabolite IV was synthesized via the acids IX and XI and the esters X and XII.The enamine VIII was prepared from 3-fluoro-8-(2-propyl)dibenzothiepin-10(11H)-one by two methods and was reduced to I.Cloflumide (II) was obtained by reaction of 2,10-dichloro-7-fluoro-10,11-dihydrodibenzothiepin with 3-(1-piperazinyl)propionamide and was oxidized to the sulfoxide XVI.The unsaturated analogue XVII of clopithepin (III) was prepared from 2-chlorodibenzothiepin-10(11H)-one by reaction with 2-bromoethanol in the presence of 4-toluenesulfonic acid in boiling benzene and by the following substitution reaction with 2-(1-piperazinyl)ethanol.An improved synthesis of 6-methyldibenzothiepin-10(11H)-one (XIX) was elaborated.The acid XXVII was synthesized and cyclized with polyphosphate ester.A mixture of compounds was formed from which the ketone XXXVI was isolated and processed by reaction with formamide and formic acid at 200 deg C.One of the products was characterized as the formamide XXXIII and was reduced with lithium aluminium hydride to a basic product supposed to be XXXIV.A series of by-products was isolated and characterized.The enamine VIII (VUFB-17156) was found to be a strong neuroleptic agent, similar to isofloxythepin (I).The enol ether XVII (VUFB-17733) was characterized as a mild, practically noncataleptic neuroleptic agent.
- Sindelar, Karel,Jilek, Jiri,Pomykacek, Josef,Valenta, Vladimir,Hrubantova, Marta,et al.
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p. 2282 - 2303
(2007/10/02)
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- Methyl substituted thioxanthones and thioxanthone-10,10-dioxides
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The preparation of all four monomethylthioxanthones and their corresponding dioxides is described.A previously published synthesis of the 2- and 3-methylthioxanthones by Gilman and Diehl has been shown to produce the 2- and 4-methyl isomers.
- Brindle, Ian D.,Doyle, Paul P.
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p. 1869 - 1871
(2007/10/02)
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- Studies in Rearrangement of 2-(Arylthio)benzohydroxamic Acids to the Corresponding 2-(Arylsulphinyl)benzamides
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2-(2'-Methoxyphenylthio)-(III)-, 2-(4'-methoxyphenylthio)-(IV)-, 2-(2'-methylphenylthio)-(V)- and 2-(4'-methylphenylthio)-(VI)-benzohydroxamic acids on treatment with polyphosphoric acid yield 2-(2'-methoxyphenylsulphinyl)-(VII)-, 2-(4'-methoxyphenylsulphinyl)-(VIII)-, 2-(2'-methylphenylsulphinyl)-(IX)- and 2-(4'-methylphenylsulphinyl)-(X)-benzamides respectively, illustrating the generality of rearrangement reported earlier .The rearrangement can also be effected with other reagents like xylene-P2O5, perchloric acid- gl. acetic acid and trifluoracetic acid. 2-Methylthiobenzohydroxamic acid (XI) and 4-(phenylthio)benzohydroxamic acid (XII) when treated with PPA yield benzothiazolone (XIII) and 4-aminodiphenyl sulphide (XIV).Experimental evidence has been presented which points to a concerted mechanism for the intramolecular oxygen transfer.
- Dhareshwar, G. P.,Chhaya, P. N.,Hosangadi, B. D.
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p. 831 - 835
(2007/10/02)
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