Late Stage CH Activation of a Privileged Scaffold; Synthesis of a Library of Benzodiazepines | Zendy

Khan Raysa | Zendy; Felix Robert | Zendy; Kemmitt Paul D. | Zendy; Coles Simon J. | Zendy; Day Iain J. | Zendy; Tizzard Graham J. | Zendy; Spencer John | Zendy

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Late Stage CH Activation of a Privileged Scaffold; Synthesis of a Library of Benzodiazepines

Author(s) -

Khan Raysa,

Felix Robert,

Kemmitt Paul D.,

Coles Simon J.,

Day Iain J.,

Tizzard Graham J.,

Spencer John

Publication year - 2016

Publication title -

advanced synthesis and catalysis

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.541

H-Index - 155

eISSN - 1615-4169

pISSN - 1615-4150

DOI - 10.1002/adsc.201501009

Subject(s) - chemistry , alkylation , metabolite , combinatorial chemistry , hydrogen–deuterium exchange , scaffold , stereochemistry , medicinal chemistry , organic chemistry , catalysis , biochemistry , database , computer science , hydrogen

A library of over twenty 5‐(2‐arylphenyl)‐1,3‐dihydro‐2 H ‐1,4‐benzodiazepin‐2‐ones has been formed by a microwave‐mediated late‐stage palladium‐catalysed arylation of 1,4‐benzodiazepines using diaryliodonium salts. This can also be applied to nordazepam (7‐chloro‐5‐phenyl‐1,3‐dihydro‐2 H ‐1,4‐benzodiazepin‐2‐one), the active metabolite of diazepam, and subsequent N‐alkylation and/or H/D exchange allows further diversification towards elaborated pharmaceuticals and their 3,3′‐deuterated analogues.

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