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Synthesis Development of the selective estrogen receptor degrader (SERD) LSZ102

Baenziger, Markus, Langlois, Audrey, Gschwend, Bjoern, Wickendick, Regina, Baierl, Marcel, Kovacic, Nikola, Haller, Michael, Schuerch, Friedrich, Shen, Xiaodong, Fu, Peng, Lianhe, Coauthor, Eswaran, Sumesh and Devanathan, Krishnaswamy (2020) Synthesis Development of the selective estrogen receptor degrader (SERD) LSZ102. Organic Process Research & Development, 24 (8). pp. 1405-1419. ISSN 1083-61601520-586X


The development of the synthesis of the selective estrogen receptor degrader (SERD) drug candidate LSZ102 from the research synthesis to late phase development synthesis is described in this article. The synthesis of LSZ102 could be significantly improved in regards of overall yield, removal of all chromatographic purifications and number of steps by modifying the original disconnection strategy from a Pd catalyzed Suzuki coupling to a Pd catalyzed conversion of an aryl bromide to a phenol and a Pd catalyzed C-H activation as key step.

The same content will be also shown at 3rd Edition of Unite Scientific Chemistry Conference (USCC-2023) to be held during June 22-23, 2023 in Rome, Italy and two online seminars in March 2021. The corresponding slides are in the upload section.

Item Type: Article
Keywords: Pd catalyzed reactions; Pd-catalyzed C-H activation; benzothiophene-scaffold; SNAr reaction; Pd removal; LSZ102
Date Deposited: 08 Sep 2020 00:45
Last Modified: 30 Nov 2022 00:46