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HRID 331321Erstellt: 25. Oktober 2026

Triphenylphosphine → 6-[2-(1,1-dioxothiomorpholin-4-yl)ethoxy]-3-(3,5-difluorophenyl)-2-(pyridin-3-yl)-1H-inden-1-one

https://huagongshe.com/reaction/331321

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktTriphenylphosphineHCID 11776—
EduktDiisopropyl azodicarboxylateHCID 5363146—
Edukt4-(2-Hydroxyethyl)-1lambda~6~,4-thiazinane-1,1-dioneHCID 21874811—
Edukt2-bromo-6-hydroxy-3-phenyl-1H-inden-1-oneHCID 70306176—
Edukt3-(3,5-difluorophenyl)-6-hydroxy-2-(pyridin-3-yl)-1H-inden-1-oneHCID 70317432—
Produkt6-[2-(1,1-dioxothiomorpholin-4-yl)ethoxy]-3-(3,5-difluorophenyl)-2-(pyridin-3-yl)-1H-inden-1-oneHCID 51002042—

Reaktionsschritte

The procedure of Step 6 of Example 1 was repeated except for using 3-(3,5-difluorophenyl)-6-hydroxy-2-(pyridin-3-yl)-1H-inden-1-one obtained in Step 1 of Example 64 as a starting material instead of 2-bromo-6-hydroxy-3-phenyl-1H-inden-1-one, 4-(2-hydroxyethyl)thiomorpholine-1,1-dioxide (2.0 eq) instead of 4-(2-hydroxyethyl)morpholine, using 2 equivalents of PPh3 and DIAD, and being stirred for 13 h to provide 6-[2-(1,1-dioxothiomorpholin-4-yl)ethoxy]-3-(3,5-difluorophenyl)-2-(pyridin-3-yl)-1H-inden-1-one, which was treated with HCl/dioxane following the same procedure in Step 8 of Example 1 (40% for 2 steps).

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08877747B2
Quelldatensatzuspto-grants-2014_11
ORD IDord-29c45d38f96b47feb9884b78f171a199
Quellennotizuspto-grants-2014_11