- Synthesis and biological evaluation of unnatural derivatives of narciclasine: 7-aza-nornarciclasine and its N-oxide
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Several unnatural derivatives of narciclasine were prepared in which the C-7 carbon was replaced with nitrogen. The 7-aza derivative and its N-oxide were prepared by the coupling of iodopicolinic acid with a conduramine unit derived chemoenzymatically from bromobenzene. Intramolecular Heck reaction was used to construct the isocarbostyryl ring system. The compounds were submitted to biological screening against cancer cell lines. Full experimental and spectra data are provided for all new compounds.
- Vshyvenko, Sergey,Reisenauer, Mary Rose,Rogelj, Snezna,Hudlicky, Tomas
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Read Online
- Heteroaryl amide derivative and use thereof as TGR5 agonist
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The invention belongs to the technical field of medicines, and in particular relates to a heteroaryl amide TGR5 agonist compound represented by formula (I) and pharmaceutically acceptable salts, esters, stereoisomers or prodrugs thereof, wherein R1, R2, R
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Paragraph 0246; 0247; 0248
(2017/06/02)
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- Piperazine Heteroaryl Derivatives as Gpr38 Agonists
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The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Z, X and B are as defined in the specification. The compounds are partial or full agonists at the GPR38 receptor. Pharmaceutical compositions comprising the compounds, methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.
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Page/Page column 13
(2009/01/24)
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- PIPERAZINE HETEROARYL DERIVATES AS GPR38 AGONISTS
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The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, (I) wherein R1, R2, R3, R4, R5, R6, Z, X and B are as defined in the specification. The compounds are partial or full agonists at the GPR38 receptor. Pharmaceutical compositions comprising the compounds, methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.
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Page/Page column 38-39
(2010/11/25)
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- ADAMANTYL DERIVATES AS P2X7 RECEPTOR ANTAGONISTS
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The invention provides compounds of formula (I) pharmaceutically acceptable salt or solvate thereof, in which R1, A1, m and A are as defined in the specification; a process for their preparation; pharmaceutical compositions containin
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Page/Page column 120-121
(2010/10/20)
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- Directed lithiation of unprotected pyridinecarboxylic acids: Syntheses of halo derivatives
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Deprotonation of all isomeric lithium pyridinecarboxylates and subsequent trapping with hexachloroethane or iodine afforded straightforward access to chloro- and iodopyridinecarboxylic acids, respectively. Starting from lithium 5-bromonicotinate, the introduction of an iodine atom at C4 and further halogen migration allowed the potential of this method to be extended to the synthesis of more elaborate derivatives.
- Lazaar, Jalal,Rebstock, Anne-Sophie,Mongin, Florence,Godard, Alain,Trécourt, Fran?ois,Marsais, Francis,Quéguiner, Guy
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p. 6723 - 6728
(2007/10/03)
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- Application of organolithium compounds in organic synthesis. Part 19. Synthetic strategies based on aromatic metallation. A concise regiospecific synthesis of 3-halogenated picolinic and isonicotinic acids
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The synthesis of the halogenated picolin- and isonicotinalides (3) and (4) via metallation (n-BuLi) of the anilides (1) and (2) and then the reaction of the generated bis-lithiated anilides with halogenating agents (CCl3-CCl3, CH2Br-CH2Br, I2) followed by subsequent acidic hydrolysis of (3) and (4), as a way of regiospecific transformation of picoline and isonicotine acids into their C3-halogenated derivatives, is described.
- Epsztajn,Plotka,Grabowska
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p. 1075 - 1086
(2007/10/03)
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