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The preparation of 8-[4-[4-(2-pyrimidinyl)-1-piperaziny]butyl]-8-azaspiro[4,5] decane-7,9-dione hydrochloride

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Abstract

8-[4-[4-(2-Pyrimidinyl)-1-piperaziny]butyl]-8-azaspiro [4,5] decane-7,9-dione hydrochloride (buspirone hydrochloride) was obtained in one pot with a 51.8% overall yield. The key intermediate, 1-(2-pyrimidinyl) piperazine, was synthesized through chlorination and cyclization condensation reaction with diethanolamine as initial material. This modified protocol has the notable advantages of mild reaction condition, convenient operation, and high overall yield.

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Acknowledgments

We greatly acknowledge the generous financial support by grants from the Natural Science Foundation of the Zhejiang Province (Y4090045, R4090358) and the Research Foundation of Education Bureau of Zhejiang Province (Y200908295).

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Authors and Affiliations

  1. State Key Laboratory of Chemical Engineering (Zhejiang University), Department of Chemical and Biological Engineering, Zhejiang University, Hangzhou, 310027, People’s Republic of China

    Hu Luo, Chao Qian, Xinzhi Chen & Chaohong He

  2. Research Institute for Innovation in Sustainable Chemistry, National Institute of Advanced Industrial Science and Technology (AIST), AIST Tsukuba West, 16-1 Onogawa, Tsukuba, Ibaraki, 305-8569, Japan

    Wei Xia

Authors
  1. Hu Luo
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  2. Wei Xia
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  3. Chao Qian
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  4. Xinzhi Chen
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  5. Chaohong He
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Correspondence to Chao Qian.

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Luo, H., Xia, W., Qian, C. et al. The preparation of 8-[4-[4-(2-pyrimidinyl)-1-piperaziny]butyl]-8-azaspiro[4,5] decane-7,9-dione hydrochloride. Res Chem Intermed 37, 1041–1045 (2011). https://doi.org/10.1007/s11164-011-0311-1

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  • DOI: https://doi.org/10.1007/s11164-011-0311-1

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