Journal
ACS OMEGA
Volume 4, Issue 27, Pages 22601-22612Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.9b03417
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Funding
- UCL Graduate School
- EPSRC [EP/K005030/1, EP/P020410/1] Funding Source: UKRI
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Herein, we report the transformation of readily accessed acyl hydrazides into protected 2-aminobenzophenones via a two-step process involving an aryne-based molecular rearrangement followed by a one-pot addition-elimination procedure. The assembly of the scaffold is tolerant of a wide variety of functional groups, and the carbamate group on the product can be facilely removed to afford highly valuable 2-aminobenzophenones. Application of the protocol was demonstrated in the synthesis of neurological medicine phenazepam.
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