- Phosphorylamides, their preparation and use
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A phosphorylamide derivative represented by the general formula (I): STR1 wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.
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- Synthesis of furan and thiophene analogs of duocarmycin SA
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Total synthesis of furan and thiophene analogs 6 and 7 of duocarmycin SA was achieved in racemic forms, starting from methyl 4,5-dibromo-2-furan- and thiophenecarboxylates (15a and 15b). Lithio derivatives 12a (a series: X = O) and 12b (b series: X = S) were reacted with the aldehyde 22 for preparation of 25a and 25b, and successive synthetic operations, including Heck reaction of 25a and 25b to obtain 26a+27a and 26b+27b, and B ring aromatization, 28a and 28b→31a and 31b, based on our previous total synthesis of duocarmycin SA, afforded 36a and 36b. Treatment of 36a and 36b with potassium carbonate in methanol directly afforded cyclopropapyrroloindole derivatives 38a and 38b, whose condensation with the 5,6,7-trimethoxy-2-indolecarbonyl unit completed the synthesis of (±)-6 and (±)-7.
- Muratake, Hideaki,Okabe, Kazuaki,Takahashi, Michiko,Tonegawa, Miyuki,Natsume, Mitsutaka
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p. 799 - 806
(2007/10/03)
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- SYNTHESIS OF SOME FURYL- AND THIENYLACRYLATES OR DIACRYLATES AND ACRYLIC ACIDS BY THE PALLADIUM CATALYSED VINYLATION OF SUBSTITUTED BROMOFURANS AND BROMOTHIOPHENES
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Furyl- and thienylacrylates (8-14) and acrylic acids (8a,10a-14a) are prepared in moderate yields by palladium catalysed coupling of substituted bromofurans and bromothiophenes with ethyl acrylate.
- Karminski-Zamola, Grace,Dogan, Jasna,Bajic, Miroslav,Blazevic, Jelena,Malesevic, Miroslav
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p. 759 - 768
(2007/10/02)
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