METHOD FOR THE PREPARATION OF 2'-DEOXY-2',2'-DIFLUOROCYTIDINE

METHOD FOR THE PREPARATION OF 2'-DEOXY-2',2'-DIFLUOROCYTIDINE

Provided is an improved method for stereoselectively preparing 2′-deoxy-2′,2′-difluorocytidine of formula (I), which includes reacting a 1-halo ribofuranose compound with a nucleobase of formula (IV) in a solvent to obtain a nucleo side of formula (II) with removal of a silyl halide ((alkyl)3SiX (X=...

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Bibliographische Detailangaben
Hauptverfasser: LEE, JAE CHUL, PARK, GHA SEUNG, KIM, CHEOL KYONG, BANG, HYO-JEONG, LEE, JAEHEON, KIM, HAN KYONG, CHANG, YOUNG-KIL, LEE, GWAN SUN, CHOI, CHANG-JU, LEE, HOE CHUL, LEE, MOONSUB
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
DERIVATIVES THEREOF
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
SUGARS
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Beschreibung
Zusammenfassung:Provided is an improved method for stereoselectively preparing 2′-deoxy-2′,2′-difluorocytidine of formula (I), which includes reacting a 1-halo ribofuranose compound with a nucleobase of formula (IV) in a solvent to obtain a nucleo side of formula (II) with removal of a silyl halide ((alkyl)3SiX (X=halide)); and deprotecting the nucleoside of formula (II) to obtain 2′-deoxy-2′,2′-difluorocytidine of formula (I). 2′-Deoxy-2′,2′-difluorocytidine of formula (I) is effective for treating various cancers such as non-small cell lung (NSCLC), pancreatic, bladder, breast or ovarian cancers.