Pd-Catalyzed microwave-assisted synthesis of phosphonated 13α-estrones as potential OATP2B1, 17β-HSD1 and/or STS inhibitors

Pd-Catalyzed microwave-assisted synthesis of phosphonated 13α-estrones as potential OATP2B1, 17β-HSD1 and/or STS inhibitors

Novel 2- or 4-phosphonated 13α-estrone derivatives were synthesized via the Hirao reaction. Bromo regioisomers (2- or 4-) of 13α-estrone and its 3-benzyl or 3-methyl ether were reacted with diethyl phosphite or diphenylphosphine oxide using Pd(PPh3)4 as catalyst under microwave irradiation. The infl...

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Bibliographic Details
Main Authors: Rebeka Jójárt, Szabolcs Pécsy, György Keglevich, Mihály Szécsi, Réka Rigó, Csilla Özvegy-Laczka, Gábor Kecskeméti, Erzsébet Mernyák
Format: Article
Language:English
Published: Beilstein-Institut 2018-11-01
Series:Beilstein Journal of Organic Chemistry
Subjects:
catalysis
enzyme
13α-estrone
Hirao reaction
17β-HSD1 inhibition
OATP2B1
STS
Online Access:https://doi.org/10.3762/bjoc.14.262

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