Preparation method of tadalafil nitrosamine impurity

By using a specific solvent and nitrosating agent under mild conditions for nitrosation reaction, the problem of low yield in the preparation of tadalafil nitrosamine impurities was solved, and the preparation of high-purity impurities was achieved, meeting the needs of toxicological research and drug quality control, and improving drug safety and regulatory compliance.

CN121318968APending Publication Date: 2026-01-13RUYUAN HEC PHARM
View PDF 1 Cites 0 Cited by

Patent Information

Application Number
CN202511356014.1
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-09-22
Publication Date
2026-01-13

AI Technical Summary

Technical Problem

The existing technology for preparing tadalafil nitrosamine impurities has low yield and low purity, making it difficult to meet the needs of batch analysis. It also lacks reliable standards, which affects drug quality control and regulatory compliance.

Method used

The nitrosation reaction is carried out under mild and controllable conditions using specific organic solvents and nitrosating agents, including the use of nitrites or nitrite esters as nitrosating agents, combined with acidic reagents and different solvents. By optimizing reaction parameters and post-processing methods, high-purity nitrosamine impurities can be prepared efficiently.

Benefits of technology

This method achieves high yield and high purity preparation of tadalafil nitrosamine impurities, providing key materials for toxicological studies and drug safety testing, meeting qualitative and quantitative analysis requirements, and ensuring drug quality and compliance.

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure CN121318968A_ABST
    Figure CN121318968A_ABST
Patent Text Reader

Abstract

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of a tadalafil nitrosamine impurity. The invention discloses an efficient preparation method of two key nitrosamine impurity compounds of tadalafil. According to the method, nitrosation reaction is performed by adopting a specific reagent, directional synthesis of target impurities is realized under mild and controllable reaction conditions, and the method has the remarkable advantages of simplicity and convenience in operation, high product yield, high purity and the like. According to the method, the problem that related impurities are difficult to obtain is successfully solved, and a key material is provided for toxicological research or qualitative and quantitative research of the tadalafil nitrosamine impurities. The prepared impurity compound can be applied to nitrosamine genotoxic impurity detection and methodological development of tadalafil raw material medicines, preparations and intermediates thereof, and has important value for guaranteeing the safety and compliance of medicines.
Need to check novelty before this filing date? Find Prior Art

Citation Information

Patent Citations

  • Preparing method of phosphodiesterase 5 inhibitor tadalafil

    CN103980275A