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Citation: Zhang Huaiyuan, Tang Rongping, Wu Jiawei, Hu Yulai. A Novel Synthetic Method for Flibanserin[J]. Chemistry, ;2018, 81(11): 1048-1051. shu

A Novel Synthetic Method for Flibanserin

1.
Lan Zhou Petrochemical Polytechnic Lanzhou 730060
2.
Northwest Normal University Lanzhou 730070

Received Date: 28 June 2018
Accepted Date: 16 August 2018

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A novel and efficient synthesis of flibanserin was reported. One pot reaction of benzaldehyde, N-phenyl hydroxylamine and trimethylsilyl cyanide promoted by diacetoxyiodobenzene was used to construct benzimidazolones, which is the key skeleton structure of flibanserin. Subsequently, it is reacted with 1, 2-dibromoethane to generate compound 8, which hydrolyzed in concentrated hydrochloric acid to produce intermediate 9. At last, intermediate 9 was reacted with 10 to obtain flibanserin with a total yield of 29%. The structure of all compounds was characterized by ¹H NMR, ¹³C NMR and HRMS. This method has the advantages of inexpensive raw material, little byproduct and moderate yield.
- Flibanserin,
- Diacetoxyiodobenzene,
- Benzimidazolones,
- Synthesis
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