N-(2-(2-Methoxyphenylthio)benzyl)-2-aryloxyethylamines:Synthesis and evaluation for dual 5-HT_(1A)/SSRI activities

The design, synthesis and biological evaluation of N-（2-（2-methoxyphenylthio） benzyl）-2-aryloxyethyl amines with dual 5-HT1A/SSR/activities are reported. Compound 8e displays the best dual activities and is a promising lead compound for further SAR studies.

New 3-(4-arylpiperazin-1-yl)-1-(benzo[b]thiophen-3-yl)-2-methylpropanol derivatives:Synthesis and evaluation for dual 5-HT1A/SSRI activities

A series of 3-（4-arylpiperazin-1-yl）-1-（benzo[b]thiophen-3-yl）-2-methylpropanol derivatives were designed and synthesized based on 5-HT1A/SSRI drugs design strategies.The synthesized compounds were evaluated for their dual 5-HT1A/5-HTT activities.

1-[2-(2-Methoxyphenylthio) benzyl]-4-arylpiperazines derivatives:Synthesis and evaluation for dual 5-HT_(1A)/SSRI activities

A series of 1-[2-（2-methoxyphenylthio） benzyl]-4-arylpiperazines derivatives was designed and synthesized based on 5-HT1A/ SSRI drugs design strategies. The synthesized compounds were evaluated for their dual 5-HT1A/5-HTT activities. 2007 Ai Jun Li. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

Arylpiperazine derivatives of diphenylsulfide:Synthesis and evaluation for dual 5-HT_(1A)/SSRI activities

The design, synthesis and biological evaluation of a novel series of arylpiperazine derivatives of diphenylsulfide with dual 5- HT1A/SSRI activities are reported. The target compounds exhibit low to moderate 5-HT transporter affinity and moderate to high 5- HT1A affinity, Compound 13a shows moderate dual activities and is a promising lead compound for further structure-activity relationships studies.

1-(N-(2-(2-Methoxyphenylthio)benzyl)-N-methylamino-3-aryloxypropan-2-ols:Synthesis and evaluation for dual 5-HT_(1A)/SSRI activities

A series of 1-（N-（2-（2-methoxyphenylthio）benzyl）-N-methylamino-3-aryloxypropan-2-ols derivatives were designed and synthesized based on 5-HT1A/SSRI drugs design strategies. The synthesized compounds were evaluated for their dual 5-HT1A/ 5-HTT activities. 2007 Ai Jun Li. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

Facile Synthesis of Five-membered Phosphoroheterocycles Bearing N-P-N and S-P-N Moieties

New reactions of Lawesson reagent (LR) with alpha -hydroxy (amino)nitriles have been studied. The experimental results showed that the five-membered phosphoroheterocycles 2 and 4 bearing N-P-N or S-P-N moiety could be readily prepared in high yields. Meanwhile, the possible mechanism of the reactions was also discussed.

Stereoselective Addition of N-Alkylhydroxylamines to α,β-Unsaturated Nitro Compounds

N-Alkylhydroxylamines have been shown to undergo a stereospecific cis addition to 1-phenyl-2 -nitropropene compounds, whereas the corresponding O-alkylhydroxylamines give no diastereoselectivity. The concerted addition mechanism was provided to explain the difference.

Approach to N-Alkoxy-2-oxoindole for Mimicing SERMs Structure

Treatment of N-alkoxyamides with bis（trifluoroacetoxy）iodobenzene generated electron deficient nitrogen species, which readily cyclized onto aromatic ring to give N-alkoxy-2- oxoindoles. The effect of different substituent on aromatic ring to the electrophilic substitution was studied.