- Palladium-catalyzed oxalyl amide assisted direct ortho-alkynylation of arylalkylamine derivatives at δ and ε positions
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Palladium-catalyzed oxalyl amide directed ortho-alkynylation of arylalkylamine derivatives is reported for the first time. A wide variety of β-arylethamine and γ-arylpropamine derivatives are compatible with this protocol. This method provides a general means to synthesize substituted alkynylarylalkylamine derivatives, highlighting the ability of oxalyl amide in promoting C-H functionalization at unique δ and ε positions.
- Guan, Mingyu,Chen, Changpeng,Zhang, Jingyu,Zeng, Runsheng,Zhao, Yingsheng
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supporting information
p. 12103 - 12106
(2015/07/28)
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- Neuroprotective or neurotoxic activity of 1-methyl-1,2,3,4- tetrahydroisoquinoline and related compounds
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1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) 1 and various 5- or 6,7-substituted analogues were synthesized and assayed for neurotoxicity towards SH-SY5Y cells. Among mono-substituted derivatives of 1, hydroxyl substitution decreased the toxicity, while methoxyl substitution increased it. Disubstituted derivatives of 1, 5a and 5b, showed the opposite tendency. Hydroxy-1MeTIQ derivatives were tested for neuroprotective activity, and 3b and 4b exhibited greater efficacy than 1. We suggest that hydroxy-1MeTIQ derivatives, especially 4b, may have potential for the treatment of Parkinson's disease.
- Okuda, Katsuhiro,Kotake, Yaichiro,Ohta, Shigeru
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p. 2853 - 2855
(2007/10/03)
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