177017-69-5Relevant articles and documents
INDOLE AHR INHIBITORS AND USES THEREOF
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, (2018/11/22)
The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
Asymmetric amination of tetralone and chromanone derivatives employing ω-transaminases
Pressnitz, Desiree,Fuchs, Christine S.,Sattler, Johann H.,Knaus, Tanja,Macheroux, Peter,Mutti, Francesco G.,Kroutil, Wolfgang
, p. 555 - 559 (2013/06/05)
Various (S)-selective and (R)-selective ω-transaminases were investigated for the amination of 1- and 2-tetralone and derivatives as well as of 3- and 4-chromanone. All ketones tested were aminated to give the corresponding enantiopure amines (ee > 99%) employing at least one of the enzymes investigated. In most of the cases the (S)- as well as the (R)-enantiomer was obtained in optically pure form. The amination of 3-chromanone was performed on a 100 mg scale leading to optically pure (R)-3-aminochromane (ee > 99%) with complete conversion and 78% isolated yield.
Artificial multi-enzyme networks for the asymmetric amination of sec-alcohols
Tauber, Katharina,Fuchs, Michael,Sattler, Johann H.,Pitzer, Julia,Pressnitz, Desiree,Koszelewski, Dominik,Faber, Kurt,Pfeffer, Jan,Haas, Thomas,Kroutil, Wolfgang
, p. 4030 - 4035 (2013/04/10)
Various artificial network designs that involve biocatalysts were tested for the asymmetric amination of sec-alcohols to the corresponding α-chiral primary amines. The artificial systems tested involved three to five redox enzymes and were exemplary of a range of different sec-alcohol substrates. Alcohols were oxidised to the corresponding ketone by an alcohol dehydrogenase. The ketones were subsequently aminated by employing a ω-transaminase. Of special interest were redox-neutral designs in which the hydride abstracted in the oxidation step was reused in the amination step of the cascade. Under optimised conditions up to 91 % conversion of an alcohol to the amine was achieved. Trickle-down effect: The asymmetric amination of sec-alcohols to the corresponding α-chiral primary amines was performed with a biocatalytic cascade whereby the various steps were interconnected through the cofactors/cosubstrates. In a redox-neutral cascade and under optimised conditions, up to 91 % conversion of an alcohol to the amine was achieved. Copyright