Journal
SYNTHESIS-STUTTGART
Volume 51, Issue 17, Pages 3171-3204Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0037-1611822
Keywords
C-H functionalization; saturated heterocycles; transition metal catalysis; stereoselectivity; regioselectivity
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Funding
- Royal Society for University Research Fellowship [UF140161]
- URF appointed grant [RG150444]
- URF enhancement grant [RGF\ EA\180031]
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Synthetic methods that can readily access saturated heterocycles with different substitution patterns and with control of stereo- and regiochemistry are of huge potential value in the development of new medicinal compounds. Directed C-H functionalization of simple and commercially available precursors offers the potential to prepare diverse collections of such valuable compounds that can probe the different available exit vectors from a ring system. Nonetheless, the presence of the Lewis basic heteroatoms makes this a significant challenge. This review covers recent advances in the catalytic C-H functionalization of saturated heterocycles, with a view to different heterocycles (N, O, S), substitution patterns and transformations. 1 Introduction 2 alpha-C-H Functionalization with Directing Group on Nitrogen 3 C-H Functionalization at Unactivated C(3), C(4), and C(5) Positions 3.1 C-H Functionalization at C(3) with Directing Groups at C(2) 3.2 C-H Functionalization at C(3), C(4), and C(5): Directing Groups at C(4) and C(3) 4 Transannular C-H Functionalization 5 Conclusion
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