Wolfgang SIEGEL,Stephanie RENZ,Michael PUHL,Andreas WOELFERT
申请号：
MX2018009515
公开号：
MX2018009515A
申请日:
2017.02.02
申请国别(地区):
MX
年份:
2018
代理人:
摘要：
The present invention relates to a process for producing 2-O-fucosyllactose, to the intermediates obtainable by this process and to the use of these intermediates. Production comprises the reaction of a protected fucose of general formula (I) with a tri-(C1-C6-alkyl)silyl iodide to form a protected 1-iodofucose followed by reaction of the protected 1-iodofucose with a compound of general formula (I I), in the presence of at least one base and deprotection of the obtained coupling product to obtain 2-O-fucosyllactose. The variables are defined as follows: Raand Rb are identical or different and represent -C(=O)-C1-C6-alkyl or -C(=O)-phenyl, wherein phenyl is unsubstituted or optionally comprises 1 to 5 substituents or Ra and Rb together represent a -(C=O)- radical or a substituted methylene radical -C(RdRe)-, Rc represents an RSi radical or benzyl, wherein benzyl is unsubstituted or optionally bears 1, 2 or 3 substituents, RSi represents a radical of formula SiRfRgRh, wherein Rf, Rgand Rh are identical or different and represent, for example C1-C8-alkyl, R1 represents a -C(=O)-R11 radical or a SiR12R13R14 radical, R2 are identical or different and represent for example C1-C8-alkyl, R3 are identical or different and represent for example C1-C8-alkyl or both radicals R3 together represent linear C1-C4-alkenyl which is unsubstituted or bears 1 to 6 methyl groups as substituents.La presente invención se refiere a un método para preparar 2-O-fucosil lactosa, en donde los intermediarios se obtienen mediante este método y el uso de estos intermediarios. La preparación comprende la reacción de una fucosa protegida de la Fórmula general (I) con un yoduro de tri(C1-C6-alquil)sililo para obtener una 1-iodofucosa protegida, y luego la reacción de la 1-iodofucosa protegida con un compuesto de la Fórmula general (II), en presencia de al menos una base, y la desprotección del producto de acoplamiento resultante para obtener 2-O-fucosil lactosa. (ver Formulas). En este contexto, las
