NDLI: Late-Stage C–H Arylation of Azepinoindole via Pd/Cu Catalysis: A Step Efficient and Convergent Synthesis of Rucaparib

Content Provider	Scilit
Author	O’Rourke, Galahad Vos, Dirk De Beckers, Igor
Copyright Year	2021
Description	The C–H arylation of indoles holds the promise to shorten synthetic routes in the production of pharmaceuticals. However, late-stage C–H activation reactions often rely on the presence of protecting groups or stoichiometric metal additives. The regiospecific C–H arylation of a highly functionalized azepino[5,3,4-cd]indole scaffold lacking directing groups via Pd(II) and Cu(II) co-catalysis is reported. The direct C–H coupling was demonstrated in the convergent synthesis of rucaparib, an FDA approved anticancer drug.
Related Links	http://www.thieme-connect.de/products/ejournals/pdf/10.1055/s-0037-1610784.pdf
Ending Page	340
Page Count	7
Starting Page	334
ISSN	00397881
e-ISSN	1437210X
DOI	10.1055/s-0037-1610784
Journal	Synthesis
Issue Number	02
Volume Number	54
Language	English
Publisher	Georg Thieme Verlag KG
Publisher Date	2021-09-17
Access Restriction	Open
Subject Keyword	Journal: Synthesis Homogeneous Catalysis Organic Synthesis
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Catalysis

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Late-Stage C–H Arylation of Azepinoindole via Pd/Cu Catalysis: A Step Efficient and Convergent Synthesis of Rucaparib