- Divergent Synthesis of Marine Natural Products Siphonodictyal B, Corallidictyals C/D, and Liphagal Based on the Early Presence of an Aldehyde Group Instead of a Late-Stage Introduction
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An iodine-promoted sunlight-induced olefin Z/E isomerization reaction together with a palladium-catalyzed direct cross-coupling reaction of a drimanal hydrazone and an iodobenzaldehyde, without touching the aromatic aldehyde group, facilitated a divergent and expeditious access to bioactive marine natural products siphonodictyal B, corallidictyals C/D, and liphagal based on the early presence of an aldehyde group instead of a late-stage introduction.
- Wang, Jun-Li,Li, Hui-Jing,Wu, Yan-Chao
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p. 8716 - 8723
(2018/06/11)
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- ISOINDOLINE COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE
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Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta- associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.
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Paragraph 0469; 0471
(2015/09/23)
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- Reactivity assessment of chalcones by a kinetic thiol assay
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The electrophilic nature of chalcones (1,3-diphenylprop-2-en-1-ones) and many other α,β-unsaturated carbonyl compounds is crucial for their biological activity, which is often based on thiol-mediated regulation processes. To better predict their biological activity a simple screening assay for the assessment of the second-order rate constants (k2) in thia-Michael additions was developed. Hence, a clear structure-activity relationship of 16 differentially decorated hydroxy-alkoxychalcones upon addition of cysteamine could be established. Moreover, amongst other naturally occurring α,β-unsaturated carbonyl compounds k2 values for curcumin and cinnamaldehyde were gained while cinnamic acids or esters gave no or very slow reactions.
- Amslinger, Sabine,Al-Rifai, Nafisah,Winter, Katrin,W?rmann, Kilian,Scholz, Rebekka,Baumeister, Paul,Wild, Martin
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supporting information
p. 549 - 554
(2013/03/13)
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- Modular total syntheses of lamellarin G trimethyl ether and lamellarin S
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Modular total syntheses of the title compounds 2 and 3 are reported. The key pyrrolic building block 8 was prepared from the readily accessible pyrrole 6 via a di-iodination/mono-deiodination sequence. Suzuki-Miyaura cross-coupling of compound 8 with boronate ester 9 afforded lactone 10. Bromination of compound 10 followed by N-alkylation under Mitsunobu conditions afforded the fully substituted pyrrole 13 that engaged in a second Suzuki-Miyaura cross-coupling reaction with boronic acid 14 to give compound 15. Hydrolysis of the ester moiety within the last compound afforded acid 16 that engaged in a decarboxylative Heck cyclization process to give lamellarin G trimethyl ether (3). A related sequence of reactions starting from building block 8 and using the isopropoxy-substituted arenes 22, 25 and 27 has allowed for the completion of the first total synthesis of lamellarin S (2). The first total synthesis of the marine alkaloid lamellarin S is described.
- Hasse, Katrin,Willis, Anthony C.,Banwell, Martin G.
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experimental part
p. 88 - 99
(2011/03/21)
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- The first total synthesis of kynapcin-24 by palladium catalysis
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The synthesis of kynapcin-24, which can be isolated from the Korean mushroom Polyozellus multiflex Murr, is achieved in 12% overall yield from commercially available 3,4-dihydroxybenzaldehyde by a route in which the longest linear sequence is only 14 step
- Yang, Ling-Yi,Chang, Chia-Fu,Huang, Yu-Chao,Lee, Yean-Jang,Hu, Chao-Chin,Tseng, Tsui-Hwa
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experimental part
p. 1175 - 1179
(2009/12/05)
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- Pyrimidine, quinazoline, pteridine and triazine derivatives
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This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
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Page/Page column 43
(2008/06/13)
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- In vitro metabolism of 4-benzylisoquinolines, analogs of papaverine
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A comparative study was made on sliced Rat liver of the in vitro disappearance of papaverine, PV 2 6,7-dimethoxy-4-(parachlorobenzyl)isoquinoline and its mono and di isopropoxy derivatives. Data show that papaverine and PV 2 are equally sensitive to oxygenases, although 7 mono and 6,7 di-isopropoxy derivatives are much less so, being more bulky and undergo in enzymic O-dealkylation less easily. The data also show that PV 2 and 6-isopropoxy desmethoxy PV 2 disappear at the same rate, more readily than the 7 isopropoxy isomer. This confirms the in vivo results previously reported. The antispasmodic in vitro activity of these compounds is reported.
- Coulomb,Lussiana,Plat,Viel,Midol-Monnet
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p. 957 - 977
(2007/10/02)
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