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

Baenziger, Markus and Langlois, Audrey and Gschwend, Bjoern and Wickendick, Regina and Baierl, Marcel and Kovacic, Nikola and Haller, Michael and Schuerch, Friedrich and Shen, Xiaodong and Fu, Peng and Lianhe , Coauthor and 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

Abstract

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.

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: 08 Sep 2020 00:45
URI: https://oak.novartis.com/id/eprint/42052

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