X. Lian
2014
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Journal
Guangzhou Chemical Industry
Abstract
3-Chloromethyl-1,2,4-triazolin-5-one was one kind of material that was used in the production Aprepitant or Fosaprepitant. In order to simplify process,the cost was reduced and the yield was enhanced,using cheap materials and reduced reaction steps comparing with other process reported by papers. The operations were classical and simple. The intermediate was avoided degradation. The process was optimized and the costs were reduced. Especially,the alcoholysis and cyclization were combined to a one-pot reaction,which reduced the amount of solvent and reaction steps. The yield of one-pot reaction reached to 85. 39%. The HPLC purity reached to 99%,the content reached to 99%,and the material was suitable for industrial production.