- Synthesis of 3-deazathiamine
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An efficient ten-step synthesis of deazathiamine is described. The synthesis starts from commercially available α-acetyl-γ-butyrolactone and proceeds via deamination of the key aminothiophene 6. The Gewald synthesis of thiophenes is shown to give a mixture of isomeric products with the unsymmetric ketone used here and so a modified procedure giving a single isomer is developed.
- Hawksley, Daniel,Griffin, David A.,Leeper, Finian J.
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- A green synthesis method for vitamin B1 intermediates
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The present invention discloses a green synthesis method of vitamin B1 intermediates, in the presence of a catalyst α - acetyl - γ - butyrolactone under aerobic conditions, reacted in a solvent, to form α - hydroxyacetyl - γ - butyrolactone, and then into the reaction system into hydrogen chloride, in turn substitution reaction and water decarboxyl reaction, to generate vitamin B1 intermediates, i.e., 3-chloro-5-hydroxy-2-pentanone, the catalyst comprises copper salt Lewis acid The method of synthesizing 3-chloro-5-hydroxy-2-pentanone of the present invention can be more environmentally friendly, the equipment corrosive is small and has a higher yield, and can be carried out in one pot, the operation is simpler, the production cost is lower, and it is more suitable for industrial applications.
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Paragraph 0013; 0052-0085; 0088-0091
(2022/01/04)
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- Synthesis of [thiazolium-2,2′-14C2]-SAR97276A from [14C]-thiourea
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[thiazolium-2,2′-14C2]-SAR97276A, a bis(thiazolium) antimalarial development candidate, was synthesized from [ 14C]-thiourea with an overall radiochemical yield of 15%. The synthetic route involves a modified procedure for the synthesis of [ 14C]-sulfurol, also a key intermediate in thiamine synthesis, which was developed due to unlabelled chemistry proving irreproducible with the radiolabelled substrate. Copyright
- Herbert, John M.,Le Strat, Franck,Oumeddour, Delphine G.,Passey, Stephen C.,Taylor, Keith,Whitehead, David M.
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experimental part
p. 89 - 92
(2011/10/02)
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