J. Hon
2013
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0
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Journal
China Medical Herald
Abstract
Objective To design and synthesize 1-(pyridin-3-yloxyl)-3-(4-phenylpiperazin-1-yl)-propan-2-ol derivatives with α1 receptor antagonistic activity.Methods In the presence of NaH,3-(pyridin-3-yloxyl)-1,2-epoxypropane(3) was prepared from 3-hydroxylpyridine derivatives(1) and 3-chloro-1,2-epoxypropane(2) in DMF at 60℃,followed by epoxy cleavage with phenylpiperazine,leading to the synthesis of 1-(pyridin-3-yloxyl)-3-(4 phenylpiperazin-1-yl)-propan-2-ol derivatives(4).The structures of target compounds were confirmed by MS,1Hand13C-NMR data.Results 1-(pyridin-3-yloxyl)-3-(4-phenylpiperazin-1-yl)-propan-2-ol derivatives were synthe sized by two steps.The compounds showed potent α1 receptor antagonistic activity.Conclusion The reported method is effective to the synthesis of 1-(pyridin-3-yloxyl)-3-(4-phenylpiperazin-1-yl)-propan-2-ol derivatives with total yield above 68%.