The process of obtaining amino alcohols and their application in the preparation of the antibiotics chloramphenicol and thiamphenicol, fluoranfenicol

摘要

"The process of obtaining amino alcohols and their application in the preparation of the antibiotics chloramphenicol and thiamphenicol, fluoranfenicol".The present invention relates to a process for obtaining the form of aminoalcou00f3is racu00eamica and the application of the past as substrate for the preparation of broad spectrum antibiotics used.Even today, for the treatment of various types of bacterial infections, especially those causdas by Gram positive microorganisms multiresistentes.The racu00eamicos amino alcohols are prepared in five steps.A synthesis step allows for the preparation of additional antibiotics chloramphenicol (I), fluoranfenicol (II) and Thiamphenicol (III)With a chemical yield compatible with the methodologies described above.Antibiotics are prepared through the use of a common route of synthesis.Using a process easy to reproduce from methyl acrylate and 4 - nitrobenzaldeu00eddo or 4 - methylsulphonyl - benzaldehyde.The reagents used in the preparation of substrates are all commercial and of low cost.The catalyst used in the process (DABCO) besides low cost has a very low impact on the environment, because it can be recovered.In this case the two centers estereoquu00edmicos of antibiotic are prepared during the synthesis.In this overview we carry out the control of stereochemistry on obtaining isomer syn with a control that can be considered moderate.However this isomer can be easily separated from the mixture by using conventional chromatographic methods.The antibiotics obtained in its resolution through the use of methods known, which can allow the preparation of antibiotics in their pure forms enantiomericamente,Using the same sequence of reactions described in this invention.Alternatively, the use of adducts bayils - Hillman (V and VI) enantiomericamente pure also allows the preparation of antibiotics in their pure forms enantiomericamente.But there are ways of solving chemical known to adducts of Baylis - Hillman, this process can also allow access to all antibiotics in their pure forms enantiomericamente.