Real-Time Monitoring of Multistep Batch and Flow Synthesis Processes of a Key Intermediate of Lifitegrast by a Combined Spectrometer System with Both Near-Infrared and Raman Spectroscopies Coupled to Partial Least-Squares.

Process analytical technology (PAT) has been successfully applied in numerous chemical synthesis cases and is an important tool in pharmaceutical process research and development. PAT brings new methods and opportunities for the real-time monitoring of chemical processes. In multistep synthesis, real-time monitoring of the complex reaction mixtures is a significant challenge but provides an opportunity to enhance reaction understanding and control.

Practical Synthesis of 5,7-Dichlorotetrahydroisoquinoline-6-carboxylic Acid-Key Intermediate of Lifitegrast (Xiidra).

In the present study, a practical method for synthesizing the key intermediate 5,7-dichlorotetrahydroisoquinoline-6-carboxylic acid () of Lifitegrast was proposed. First, an investigation was conducted into the utilization of the impurity and recrystallization method in the synthesis of 5,7-dichlorotetrahydroisoquinoline (·HCl) via Friedel-Crafts cyclization. Through the screening of different protection groups, a previously unreported quaternary ammonium salt () was isolated with a 95.

Syntheses, antifeedant activity, and QSAR analysis of new oxa(thia)diazolyl 3(2H)-pyridazinones.

Twenty-eight new oxa(thia)diazolyl 3(2H)-pyridazinone derivatives were synthesized. Some compounds showed good chronic growth activities against the armyworm, Pseudaletia separata (Walker). Their EC50 values were determined in vivo.