- Synthesis of Pyranocyclopentaindolines Representing the Western Sections of Janthitrem B, JBIR-137, and Shearinine G
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The synthesis of the ABCD tetracyclic partial structures of the fungal indole diterpenes janthitrem B, JBIR-137, and shearinine G is reported. The route starts from 5-formylated indoline that is coupled to a dihydropyran moiety, followed by Prins cyclization. A diene was obtained that was oxygenated in a divergent manner. The hydroxylated tetracyclic western half of janthitrem B was obtained in eight steps and 10 % overall yield. We also share our experience with alternative approaches passing via alkynylated precursors. This includes the gold-catalyzed cycloisomerization of a 6-ethynyl-5-prenylindoline.
- Fresia, Marvin,Lindel, Thomas
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- METHODS FOR TREATING HEPATITIS C
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In accordance with the present invention, compounds that inhibit viral replication, preferably Hepatitis C Virus (HCV) replication, have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the treatment
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Page/Page column 447
(2010/10/20)
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- New antiproliferative benzoindolinothiazepines derivatives
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New benzoindolinothiazepines containing a piperazine moiety are described as potent antiproliferative agents against PC3 human prostatic cell lines. This activity could be explained by an accumulation of cells in G1 phase.
- Laconde, Guillaume,Depreux, Patrick,Berthelot, Pascal,Pommery, Nicole,Henichart, Jean-Pierre
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p. 167 - 172
(2007/10/03)
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- Synthesis of substituted benzoindolinothiazepines using 5- And 6-nitroindolines
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The synthesis of benzoindolothiazepine compounds was investigated using Friedel-Crafts reactions conditions from indolines. The amine function of indolinic identity was protected to avoid an alkylation of this function by methyl iodide. It was observed that the treatment of the desired amines with commercially available methyl chlorosulfanoylbenzonate resulted in the formation of sulfonamide compounds. It was also observed that the cyclization of the carboxylic acid under Friedel-Crafts conditions resulted in the formation of the desired tetracycles.
- Laconde,Depreux,Berthelot,Henichart
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- Synthesis of linear tripeptides for right-hand segments of complestatin
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This paper concerns a synthetic study of the right-hand segment of complestatin, an inhibitor of gp120-CD4 receptor. The effective synthesis of four important precursors for the right-hand segment of complestatin is described. Two of them are the precurso
- Yamada, Yaeko,Akiba, Ai,Arima, Shiho,Okada, Chiharu,Yoshida, Kiminari,Itou, Fumihiro,Kai, Toshitsugu,Satou, Toshiko,Takeda, Kazuyoshi,Harigaya, Yoshihiro
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p. 1277 - 1290
(2007/10/03)
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- Indoles
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A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: wherein A, B, C, D, T, Y, and Z each represent a methine or a nitrogen linkage; R1, R2, R3, R4, and R5 each represent a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3. The compounds have serotonin antagonism. They are therefore clinically useful as medicaments, in particular, for treating, ameliorating, and preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.
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- Photo-induced rearrangement of 1-ethoxy-2-phenylindole
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Photoirradiation of 1-ethoxy-2-phenylindole in methanol afforded 3- and 6-ethoxy-2-phenylindoles. The structural determination of the latter is carried out by direct comparison of its spectral data with those of the authentic 4-, 5-, 6-, and 7-ethoxy-2-phenylindoles, whose syntheses are also included.
- Yamada, Koji,Somei, Masanori
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p. 2481 - 2484
(2007/10/03)
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