Microwave-assisted synthesis of 4-chloro-N-(naphthalen-1-ylmethyl)-5-(3-(piperazin-1-yl)phenoxy)thiophene-2-sulfonamide (B-355252): a new potentiator of Nerve Growth Factor (NGF)-induced neurite outgrowth |
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| Authors: | Williams Alfred L Dandepally Srinivasa R Gilyazova Nailya Witherspoon Sam M Ibeanu Gordon |
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| Institution: | a Department of Pharmaceutical Sciences, North Carolina Central University, Durham, NC 27707, USA
b Biomanufacturing Research Institute and Technology Enterprise, North Carolina Central University, Durham, NC 27707, USA |
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| Abstract: | The synthesis of 4-chloro-N-(naphthalen-1-ylmethyl)-5-(3-(piperazin-1-yl)phenoxy)thiophene-2-sulfonamide (B-355252) using an MW-assisted nucleophilic aromatic substitution (SNAr) reaction will be discussed. Utilization of this method allowed for the rapid generation of B-355252 heteroaryl ether core structure in the presence of cesium carbonate in dimethylformamide or tripotassium phosphate in N-methyl-2-pyrrolidone in 94% yield. Evaluation of B-355252 enhancement of nerve growth factor’s ability to stimulate neurite outgrowths was determined using NS-1 cells. |
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| Keywords: | Microwave synthesis Nucleophilic aromatic substitution Nerve growth factor Neurite outgrowth |
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