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Article ; Online: Enantioselective Approach for Expanding the Three-Dimensional Space of Tetrahydroquinoline to Develop BET Bromodomain Inhibitors.

Lespinasse, Marie-Ange / Wei, Kaiyao / Perrin, Justine / Winkler, Matthias / Hamaidia, Sieme / Leroy, Alexis / Macek Jilkova, Zuzana / Philouze, Christian / Marche, Patrice N / Petosa, Carlo / Govin, Jérôme / Emadali, Anouk / Wong, Yung-Sing

Chemistry (Weinheim an der Bergstrasse, Germany)

2022  Volume 28, Issue 64, Page(s) e202202293

Abstract: The pharmaceutical industry has a pervasive need for chiral specific molecules with optimal affinity for their biological targets. However, the mass production of such compounds is currently limited by conventional chemical routes, that are costly and ... ...

Abstract The pharmaceutical industry has a pervasive need for chiral specific molecules with optimal affinity for their biological targets. However, the mass production of such compounds is currently limited by conventional chemical routes, that are costly and have an environmental impact. Here, we propose an easy access to obtain new tetrahydroquinolines, a motif found in many bioactive compounds, that is rapid and cost effective. Starting from simple raw materials, the procedure uses a proline-catalyzed Mannich reaction followed by the addition of BF
MeSH term(s) Stereoisomerism ; Quinolines ; Antineoplastic Agents ; Catalysis
Chemical Substances 1,2,3,4-tetrahydroquinoline (CCR50N1Z9G) ; Quinolines ; Antineoplastic Agents
Language English
Publishing date 2022-09-13
Publishing country Germany
Document type Journal Article
ZDB-ID 1478547-X
ISSN 1521-3765 ; 0947-6539
ISSN (online) 1521-3765
ISSN 0947-6539
DOI 10.1002/chem.202202293
Database MEDical Literature Analysis and Retrieval System OnLINE

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