Related Experiment Video
Updated: May 29, 2025
Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Synthesis and Characterization of 3-S-impurities in Timolol Maleate
Dejun Zhou1, Keyang Wang2, Yuying Zhang1
1The key Laboratory of Chinese Medicine Research and Development in Hebei Province, Traditional Chinese Medicine Institute of Chengde Medical University, Chengde, 067000, China.
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.
More Related Videos
10:42Preparation of N-2-alkoxyvinylsulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
06:18Syntheses, Crystallization, and Spectroscopic Characterization of 3,5-Lutidine N-Oxide Dehydrate
Published on: April 24, 2018
Related Concept Videos
01:27Open Angle Glaucoma: Treatment
Drugs such as carbonic anhydrase inhibitors, α2- and...
01:16Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...