Toward a Scalable Synthesis and Process for EMA401, Part I: Late Stage Process Development, Route Scouting, and ICH M7 Assessment

Authors :: Wietfeld Bernhard
Xiangguang Tian
Yong Zhang
Franck Mallet
Richard Kaehny
Cheng Li
Leo A. Hardegger
Bo Yu
Jeannine Stäuble
Lei Shi
Barbara Bianchi
Florian Andreas Rampf
Jialiang Li
Stephan Lanz
Christoph Spoendlin
Christine Zepperitz
Xuesong Zhang
Shangjun Teng
Chunlong Cai
Yao Yang
Roger Humair
Alexandre Grand-Guillaume Perrenoud
Source :: Organic Process Research & Development. 24:1743-1755
Publication Year :: 2020
Publisher :: American Chemical Society (ACS), 2020.
Abstract: We present the enantioselective synthesis of sodium (3S)-5-(benzyloxy)-2-(diphenylacetyl)-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (EMA401, olodanrigan), an angiotensin II type 2 anta...

Subjects :: Process development
Chemistry
Organic Chemistry
Late stage
EMA401
Physical and Theoretical Chemistry
Combinatorial chemistry
Angiotensin II
Phenylalanine derivatives

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