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Synthesis 2016; 48(24): 4495-4508
DOI: 10.1055/s-0036-1588588
DOI: 10.1055/s-0036-1588588
paper
Synthesis of Novel Fluorinated Multisubstituted Pyrimidines and 1,5-Benzodiazepines via Fluorinated N,S-Acetals
Further Information
Publication History
Received: 22 April 2016
Accepted after revision: 08 August 2016
Publication Date:
09 September 2016 (online)
Abstract
An efficient and novel approach using highly versatile but less exploited monofluorinated α-oxoketene N,S-acetals as synthons for the synthesis of novel fluorinated multisubstituted pyrimidines and 1,5-benzodiazepines by cyclization with guanidine nitrate and o-phenylenediamine, respectively, has been developed. The synthesized compounds, which carry additional functional groups that allow further functionalization, are of considerable interest as building blocks in medicinal chemistry. X-ray crystallographic studies confirmed the formation of the desired cyclized product.
Supporting Information
- Supporting information for this article is available online at http://dx.doi.org/10.1055/s-0036-1588588.
- Supporting Information
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