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Updated: Sep 19, 2026

Preparation of N-(2-alkoxyvinyl)sulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
[Synthesis and biological activities of new 5-HT2A selective ligands--N-substituted-piperidinyl-4-phenylthioether and
1Department of Medicinal Chemistry of Fudan University, Shanghai 200032, China.
Aim:
A series of 4-piperidinylthioether and sulfone derivatives of 4-[1-hydroxy-1-(2,3-dimethoxyphenyl) methyl]-N-2-(4-fluorophenylethyl) piperidine (MDL 100907) were synthesized in order to find new 5-HT2A selective ligands.
Methods:
Title compounds 2a-2c were synthesized from 2, 3-dimethoxythiophenol and tested for their affinities to 5-HT2A, 5-HT2C, 5-HT6 and 5-HT7 receptors and some other nervous transmitter receptors in vitro.
Results:
Compounds 2a-2c are new compounds. The results of the binding assay demonstrated that they have relatively high selectivity for 5-HT2A receptor in vitro.
Conclusion:
Some sulfur containing analogues of MDL 100907 showed selective affinity to 5-HT2A receptor and are worth further study.
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