Famciclovir is a purine nucleoside oral prodrug, officially launched in 1993, mainly used in the treatment of herpes zoster. After taking Famciclovir, the deacetylated group is oxidized to form Penciclovir, which contacts with viral and bacterial in the human body to convert into Penciclovir Mitsubishi acid, thereby inhibiting the replication of viral DNA and achieving antiviral effects. With the continuous improvement of medical level, the synthesis process of Famciclovir drug substance is also constantly innovating and improving, especially in the field of green pharmaceutical technology. Based on this, the main focus of this study is on green pharmaceutical technology, using materials such as 2-amino-6-chloropurine and 3-bromopropan-1,1,1-tricarboxylic acid triethyl ester as raw materials. The synthesis process is used to measure Famciclovir, and the time parameters, reaction temperature, and other factors in the synthesis process are analyzed and optimized. The appropriate steps and processes in the entire process are pooled and optimized to ultimately improve the synthesis process. While ensuring its drug properties, the synthesis process is optimized to improve the reaction yield and reduce the use of organic solvents, thereby improving production efficiency and quality.

Famciclovir;Drug substance;Synthesis process;Improvement

[1] Zhejiang Pharmaceutical Co., Ltd. Xinchang Pharmaceutical Factory. Synthesis method of impurity C in Famciclovir: CN201610408626.5 [P]. 2020-07-21. [2] Fan Yi, Pu Tong, Li Jianjun, et al. Development of green synthesis process for antiviral drug Famciclovir [Z]. Zhejiang Chetou Pharmaceutical Co., Ltd. 2016. [3] Ji Li, Jin Xin, Lao Xuejun, et al. Synthesis of two dehydroxylated impurities in Famciclovir [J]. Chinese Journal of Medicinal Chemistry, 2017,27 (2):128-132.

Wang,Rui (1979-10), Han nationality, female, an intermediate engineer with a bachelor’s degree in Taizhou, Zhejiang, Research direction: Steroid hormone synthesis or cost reduction and efficiency enhancement, Unit: Zhejiang Shenzhou Pharmaceutical Co., Ltd.

DOI： https://doi.org/10.62639/sspjinss09.20240102

Published： 2024