- NOVEL ANTIMALARIA AGENT CONTAINING HETEROCYCLIC COMPOUND
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Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula -C(=O)-NH- or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
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Page/Page column 64
(2008/06/13)
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- NOVEL ANTIFUNGAL AGENT COMPRISING HETEROCYCLIC COMPOUND
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The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula -NH-C(=O)-, a group represented by the formula -C(=O)-NH-, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].
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Page/Page column 72
(2010/11/08)
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- Five membered ring analogues of nifedipine - Part 1: 2-Nitro-3-furanecarbaldehyde and 2-nitro-3-thiophenecarbaldehyde in the Hantzsch pyridine synthesis
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The heterocyclic aldehydes 4 in the Hantzsch pyridine synthesis afforded dependent on the choosen variation, either the 1,4-dihydropyridines (DHP) 5, the 1,2-DHP 6 or the 1,2,3,4-tetrahydropyrimidines (THPM) 7 as main products. 5-7 were dehydrogenated to the corresponding heteroaromatics 8-10 by cerium(IV). The lactames 11 and 12 were isolated by appropiate reduction of the nitro group from 8 and 9 by neighbour group participation of an ester function. The synthesis of 12 represents for the second time the evidence of an 2-aminofurane compound. 11 and 12 were converted with phosphorous oxychloride to form the annulated chloronaphthyridines 13 and 14 which were cyclized with sodium azide to yield the tetrazoles 15 and 16. The half wave potentials E1/2 of the DHP and THPM 5-7 were determined by anodic oxidation with the rotating platinum electrode using difference pulse voltammetry (DPV). These are comparable with those of the 2-nitrophenyl analogues.
- Goerlitzer,Dobberkau
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p. 386 - 391
(2007/10/03)
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- Dihalomethylation of Nitroarenes via Vicarious Nucleophilic Substitution of Hydrogen with Trihalomethyl Carbanions
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Trichloro- and tribromomethyl carbanions generated by deprotonation of haloforms with potassium tert-butoxide in a THF-DMF mixture at ca. -70 deg C react with a variety of carbocyclic and heterocyclic nitroarenes according to the vicarious nucleophilic substitution scheme.The reaction provides an efficient and convenient way for the direct introduction of dihalomethyl substituents ortho and para to the nitro group, which in turn can be hydrolyzed to produce nitroaryl aldehydes.
- Makosza, M.,Owczarczyk, Z.
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p. 5094 - 5100
(2007/10/02)
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- DIRECT FORMYLATION OF NITROARENES VIA VICARIOUS NUCLEOPHILIC SUBSTITUTION OF HYDROGEN
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A new method of synthesis of nitroaromatic aldehydes via vicarious nucleophilic substitution of hydrogen with dichloromethyl group and its hydrolysis is described.
- Makosza, M.,Owczarczyk, Z.
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p. 3021 - 3022
(2007/10/02)
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