Late Stage Functionalization

Overview

Late-stage functionalization utilizes highly selective reactions to introduce functional groups to advance intermediates under mild selective conditions to diversify substitutions in lead structures for acceleration of chemistry related discoveries.¹ Late-stage functionalization is also used to prepare specific targets that may not be easily accessible by conventional approaches. WuXi AppTec provides unique Integrated Late-stage Functionalization Services to our clients, including:

• Quantum Mechanics (QM) analysis of advanced intermediates available² to access their reactivity and regio-selectivity for C-H activations reaction types of interest, from C-H alkylation, fluorination, halogenation, oxidation to trifluoromethylation
• Synthesis of key intermediates
• High throughput processing in our catalysis or photochemistry laboratories
• Rapid parallel LCMS analysis and purification of reaction samples
• QM and DP4-AI assisted structure assignments for complex structures³

1. Moir, M. et al, Expert Opin Drug Discov., 2019, 14, 1137.

2. Magical Power of Quantum Mechanics

3. Goodman, J.M. et al, Chem. Sci., 2020,11, 4351.