The development of therapeutic medications often relies on late-stage modification of complex or bioactive molecules. To demonstrate the synthetic utility of our procedure, we applied our established reaction conditions to a variety of drug-and natural product-conjugate analogs (Scheme 3). Drug molecules such as probenecid (anti-gout), febuxostat (anti-hyperuricemic drug), L-menthol (decongestants and analgesics), and adapalene (anti-acne agent), conjugated to 1-glucosyl bromides all underwent the desired C2-allylation to form products 7a-7d in 51%-67% yields with moderate stereoselectivity. Terminal olefins conjugated to ibuprofen (nonsteroidal anti-inflammatory drug, NSAID), Mycophenolic acid, glucofuranose, and oleanolic acid were directly used for allylation affording the corresponding products 8a-8d in 44%-60% yields with good stereoselectivity.