Synthesis 2015; 47(10): 1405-1412
DOI: 10.1055/s-0034-1380277
paper
© Georg Thieme Verlag Stuttgart · New York

A Convenient Synthesis of N,N-Dimethylformamidines from Sulfonamides

Yantao Chen*
AstraZeneca Innovative Medicines Cardiovascular and Metabolic Diseases, 431 83 Mölndal, Sweden   eMail: yantao.chen@astrazeneca.com   eMail: yantaochen.se@gmail.com
,
Henrik Gradén
AstraZeneca Innovative Medicines Cardiovascular and Metabolic Diseases, 431 83 Mölndal, Sweden   eMail: yantao.chen@astrazeneca.com   eMail: yantaochen.se@gmail.com
,
Carl-Johan Aurell
AstraZeneca Innovative Medicines Cardiovascular and Metabolic Diseases, 431 83 Mölndal, Sweden   eMail: yantao.chen@astrazeneca.com   eMail: yantaochen.se@gmail.com
,
James Gibson
AstraZeneca Innovative Medicines Cardiovascular and Metabolic Diseases, 431 83 Mölndal, Sweden   eMail: yantao.chen@astrazeneca.com   eMail: yantaochen.se@gmail.com
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Publikationsverlauf

Received: 10. Dezember 2014

Accepted after revision: 06. Februar 2015

Publikationsdatum:
03. März 2015 (online)


Abstract

N,N-Dimethylformamidines were synthesized from sulfonamides using the Vilsmeier reagent as a cleavage activator. The reactions were performed under mild conditions achieving good to excellent yields. The chemistry presented can also be used as a deprotection strategy when amines or anilines are protected with sulfonyl groups, such as the tosyl group.

Supporting Information