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Abstract #125721 Published in IGR 25-2
Synthesis and Characterization of 3-S-impurities in Timolol Maleate
Zhou D; Wang K; Zhang Y; Liu X; Mao XCurrent organic synthesis 2025; 0:
BACKGROUND: Timolol maleate is clinically used for the treatment of hypertension, angina pectoris, tachycardia, and glaucoma. OBJECTIVE: The aim of this study was to enhance the safe use of timolol maleate and investigate a synthesis method for 3-S-timolol, a newly identified impurity in timolol API (Active Pharmaceutical Ingredients). METHODS: (S)-3-(tert-butylamino)propane-1,2-diol (1) was used as a raw material. 3-S-timolol maleate (7) was synthesized through a five-step reaction. Overall yield was 57.7%, with a purity of 98%. RESULTS: The structure of the target compound was confirmed via analysis of its 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, and high-resolution mass spectrometry spectra. CONCLUSION: The synthesis method was straightforward and yielded a high-purity product suitable for use as a reference in the analysis and identification of timolol maleate-related substances.
The key Laboratory of Chinese Medicine Research and Development in Hebei Province, Traditional Chinese Medicine Institute of Chengde Medical University, Chengde, 067000, China.
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