Development and Production of an Enantioselective Tetrahydroisoquinoline Synthesis Enabled by Continuous Cryogenic Lithium-Halogen Exchange

Kevin P. Cole,Mark D. Argentine,Edward W. Conder,Radhe K. Vaid,Pengyao Feng,Mo Jia,Ping Huang,Peng Liu,Baoquan Sun,Sam Tadayon,Cheng Zhu,Ruiheng Zhu

Development and Production of an Enantioselective Tetrahydroisoquinoline Synthesis Enabled by Continuous Cryogenic Lithium-Halogen Exchange

2020

Kevin P. Cole
Mark D. Argentine
Edward W. Conder
Radhe K. Vaid
Pengyao Feng
Mo Jia
Ping Huang
Peng Liu
Baoquan Sun
Sam Tadayon
Cheng Zhu
Ruiheng Zhu

Route invention, process development, and production of 185 kg of a key tetrahydroisoquinoline intermediate for the dopamine D1 receptor positive allosteric modulator mevidalen are reported. The sy...

Keywords:

Tetrahydroisoquinoline
Enantioselective synthesis
Lithium
Halogen
Organic chemistry
Chemistry
Flow chemistry
Dopamine receptor D1
Allosteric modulator
process development

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