- Design and synthesis of an Fmoc-SPPS-compatible amino acid building block mimicking the transition state of phosphohistidine phosphatase
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The synthesis of a sulfonamide-based transition-state (TS) analogue of enzymatic phosphohistidine dephosphorylation as an amino acid building block is presented, together with the proof-of-concept of its incorporation into peptides. Key features include f
- Eerland, Martijn F.,Hedberg, Christian
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experimental part
p. 2047 - 2052
(2012/04/23)
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- Imidazole compounds, processes for their preparation, pharmaceuticals based on these compounds and some intermediates
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Imidazole compounds of the formula I STR1 in which R1 =alkyl, R2 and R3 =H, halogen or alkyl, X=OH or an amide radical having certain substituents, processes for their preparation and pharmaceuticals based on these compounds, in particular for the prophylaxis and treatment of circulatory disturbances, especially of disturbances of the microcirculation and of the disorders resulting therefrom, and some novel intermediates for the preparation of the compounds of the formula I, which are 1-methyl-, 1,2-dimethyl- and 1-ethyl-4-imidazolesulfonyl chloride.
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- SULFONATION OF SUBSTITUTED AZOLES WITH SULFUR TRIOXIDE IN DICHLOROETHANE
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A novel method has been developed for the synthesis of sulfonic acids of five-membered heterocycles containing two heteroatoms, with a solution of sulfur trioxide in 1,2-dichloroethane.High yields of the required products are obtained, under conditions which are mild in comparison with those used in earlier methods.The mechanism of sulfonation is discussed, and some azole.SO3 complexes have been obtained and described.
- Bochkareva, T. P.,Passet, B. V.,Popov, K. R.,Platonova, N. V.,Koval'chuk, T. I.
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p. 1084 - 1089
(2007/10/02)
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