Nickel-Catalyzed Dearomative Arylboration of Indoles: Regioselective Synthesis of C2- And C3-Borylated Indolines
Indole dearomatization is an important strategy to access indolines: a motif present in a variety of natural products and biologically active molecules. Herein, a method for transition-metal catalyzed regioselective dearomative arylboration of indoles to
Brown, M. Kevin,Crook, Phillip F.,Kuniyil, Rositha,Liu, Peng,Trammel, Grace L.
supporting information
p. 16502 - 16511
(2021/10/20)
Palladium catalyzed tandem alkenyl- and aryl-C-N bond formation: A cascade N-annulation route to 4-, 5-, 6- and 7-chloroindoles
A series of trihalogenated alkenylbenzenes undergo consecutive palladium catalyzed inter- and intramolecular amination reactions to deliver a series of 1-functionalized mono-chloroindoles. 4-, 5-, 6- and 7-Chloroindoles can all be prepared; carbamates, anilines and amines can be employed as the N-nucleophile.
Henderson, Luke C.,Lindon, Matthew J.,Willis, Michael C.
experimental part
p. 6632 - 6638
(2010/10/03)
2-PHENYL-INDOLES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS
The present invention is directed to 2-phenyl-indole compounds (A), their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in treating a patient suffering from a PGD2-mediated disorder including, but not li
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Page/Page column 49
(2008/06/13)
Asymmetric Deprotonations: Lithiation of N-(tert-Butoxycarbonyl)indoline with sec-Butyllithium/ (-)-Sparteine
The asymmetric lithiation of N-Boc indoline (1) with s-BuLi/(-)-sparteine and subsequent substitution provides the 2-substituted N-Boc indolines 3 and 5-11 with excellent enantiomeric ratios and in variable yields. The asymmetric lithiation-substitution sequence with N-Boc-7-chloroindoline (12) provides products 13-19 with good enantiomeric ratios. Mechanistic investigation establishes that the enantioselectivities arise from an initial asymmetric deprotonation to provide the enantioenriched and configurationally stable organolithium intermediates (S)-28 and (S)-29, which react stereoselectively with electrophiles.
Bertini Gross, Kathleen M.,Jun, Young M.,Beak, Peter
p. 7679 - 7689
(2007/10/03)
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