89791-47-9Relevant articles and documents
Ketoreductase/Transaminase, One-Pot, Multikilogram Biocatalytic Cascade Reaction
Burns, Michael,Bi, Wenying,Kim, Hui,Lall, Manjinder S.,Li, Chao,O'Neill, Brian T.
, p. 941 - 946 (2021/03/01)
A biocatalytic cascade to produce tert-butyl ((2R,4R)-2-methyltetrahydro-2H-pyran-4-yl)carbamate 6 has been demonstrated at the multikilogram scale. In this reaction, a racemic ketone is resolved by reducing the undesired ketone using a ketone reductase (KRED). The reduction is stereospecific for the 2-position of substrate (2S)-ketone leaving the (2R)-ketone unreacted. After the (2S)-ketone has been depleted, a transaminase is added to catalyze the enantioselective transamination of the ketone, resulting in formation of the (2R, 4R)-amine 6. The product is recovered from the aqueous reaction after Boc protection.
NOVEL IMIDAZO[4,5-C]QUINOLINE DERIVATIVES AS LRRK2 INHIBITORS
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Page/Page column 53; 54; 55, (2018/09/28)
The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
Utilizing on- and off-line monitoring tools to follow a kinetic resolution step during flow synthesis
Farley, Kathleen A.,Reilly, Usa,Anderson, Dennis P.,Boscoe, Brian P.,Bundesmann, Mark W.,Foley, David A.,Lall, Manjinder S.,Li, Chao,Reese, Matthew R.,Yan, Jiangli
, p. 348 - 354 (2017/03/16)
In situ reaction monitoring tools offer the ability to track the progress of a synthetic reaction in real time to facilitate reaction optimization and provide kinetic/mechanistic insight. Herein, we report the utilization of flow NMR, flow IR, and other off-line spectroscopy tools to monitor the progress of a flow chemistry reaction. The on-line and off-line tools were selected to facilitate the stereoselective kinetic resolution of a key racemic monomer, which lacked a chromophore, making conventional reaction monitoring difficult. Copyright