A Divergent Synthesis of Substituted 2-Aminoimidazoles from 2-Aminopyrimidines
摘要:
A new divergent and efficient synthesis of substituted 2-aminoimidazoles 5 and 6 has been developed starting from the readily available 2-aminopyrimidines 1 and alpha-broinocarbonyl compounds 2, Using conventional heating or microwave irradiation. Thus, the cleavage of 1,2,3-substituted imidazo[1,2-a]pyrimidin-1 -iumsalts 4 with hydrazine or secondary amines led to 1,4,5-trisubstituted 2-aminoimidazoles 5, when the hydrazinolysis of 2-hydroxy-2,3-dihydro-1H-imidazo[1,2-a]pyrimidin-4-ium salts 3, followed by a novel Dimroth-type rearrangement, resulted in formation of 2-amino-1H-imidazoles 6. The relevant pathway of transformations was identified by characterization of the intermediates.
[EN] COMPOUNDS FOR THE TREATMENT OF HEPATITIS C<br/>[FR] COMPOSÉS POUR LE TRAITEMENT DE L'HÉPATITE C
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2010030592A1
公开(公告)日:2010-03-18
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
[EN] COMPOUNDS FOR THE TREATMENT OF HEPATITIS C<br/>[FR] COMPOSÉS UTILISABLES POUR LE TRAITEMENT DE L'HÉPATITE C
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2011112191A1
公开(公告)日:2011-09-15
The disclosure provides compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
[EN] COMPOUNDS FOR THE TREATMENT OF HEPATITIS C<br/>[FR] COMPOSÉS DESTINÉS AU TRAITEMENT DE L'HÉPATITE C
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2011112186A1
公开(公告)日:2011-09-15
The disclosure provides ten specific compounds with a basic structure of pyrazolo [1, 5-a] pyridine, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
[EN] BENZOFURAN DERIVATIVES FOR THE TREATMENT OF HEPATITS C<br/>[FR] DÉRIVÉS DE BENZOFURANNE DANS LE TRAITEMENT DE L'HÉPATITE C
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2012003164A1
公开(公告)日:2012-01-05
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity agamst hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
Efficient One-Pot, Two-Step, Microwave-Assisted Procedure for the Synthesis of Polysubstituted 2-Aminoimidazoles
作者:Denis S. Ermolat'ev、Eugene V. Babaev、Erik V. Van der Eycken
DOI:10.1021/ol062421c
日期:2006.12.1
A microwave-assisted, one-pot, two-step protocol was developed for the construction of polysubstituted 2-aminoimidazoles. This process involves the sequential formation of imidazo[1,2-a]pyrimidinium salts from readily available 2-aminopyrimidines and alpha-bromocarbonyl compounds, followed by opening of the pyrimidine ring with hydrazine. [reaction: see text]