- Hexafluoroisopropanol: A powerful solvent for the hydrogenation of indole derivatives. Selective access to tetrahydroindoles or cis-fused octahydroindoles
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Pd/C in HFIP was used to hydrogenate indole derivatives under relatively mild conditions, leading to potential synthetic intermediates of bioactive compounds. Depending on their substitution, tetrahydroindoles or octahydroindoles could selectively be obtained.
- Clarisse, Damien,Fenet, Bernard,Fache, Fabienne
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experimental part
p. 6587 - 6594
(2012/09/08)
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- PHARMACEUTICAL COMPOSITION CONTAINING FUSED HETERO-RING DERIVATIVE
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The present invention provides a compound which indicates a histamine H4 receptor modulating activity.A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is -O-, etc., n is an integer of 0 to 6; X is N(R7)- or -O-; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is-C(R8)= or -N=; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is =O, =S, etc.; B ring is a ring represented by the following formula wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.The present invention provides a compound which indicates a histamine H4 receptor modulating activity. A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R 1 is substituted or unsubstituted alkyl, etc., W is -O-, etc., n is an integer of 0 to 6; X is N(R 7 )- or -O-; R 7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is-C(R 8 )= or -N=; R 8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is =O, =S, etc.; B ring is a ring represented by the following formula wherein R 10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R 11 , R 12a and R 12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.
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Page/Page column 80
(2012/06/18)
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- Anthranilic acid based CCK1 antagonists: The 2-indole moiety may represent a "needle" according to the recent homonymous concept
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Recently we described an innovative class of non-peptide CCK1 antagonists keeping appropriate pharmacophoric groups on the anthranilic acid employed as a molecular scaffold. The lead compound obtained, VL-0395, characterized by the presence of Phe and the 2-indole moiety at the C- and N-termini of anthranilic acid, respectively, is endowed with submicromolar affinity towards CCK1 receptors. Thus, we have prepared and tested on CCK receptors a library of VL-0395 analogues in order to investigate the precise topological and essential key interactions of the 2-indole group of the lead with the CCK1 receptor. The obtained results confirm that this group establishes very specific interactions with this receptor sub-site and may be viewed as a "needle" group.
- Varnavas, Antonio,Lassiani, Lucia,Valenta, Valentina,Berti, Federico,Tontini, Andrea,Mennuni, Laura,Makovec, Francesco
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- SYNTHESIS OF PYRROLE-2-CARBOXYLIC ACIDS AND THEIR N-VINYL DERIVATIVES
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Haloform cleavage of 2-trifluoroacetyl- and N-vinyl-2-trifluoroacetylpyrroles gives pyrrole-2-carboxylic acids and their N-vinyl derivatives in good yields; most of these compounds do not melt between 120-190 deg C, but rather decompose with CO2 evolution.
- Sobenina, L. N.,Sergeeva, M. P.,Mikhaleva, A. I.,Sigalov, M. V.,Korostova, S. E.,et al.
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p. 516 - 520
(2007/10/02)
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