VUD GEHVIN DZHEFFRI,ВУД Гэвин Джеффри,VESTVUD ROBERT,ВЕСТВУД Роберт
申请号：
RU2010150153/04
公开号：
RU0002509084C2
申请日:
2009.05.08
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
FIELD: biotechnologies.SUBSTANCE: invention refers to a method for obtaining a compound of formula 682, which is in a crystalline form, where the above method involves the following: (i) treatment of the compound of formula 682-9 with palmitic anhydride mixed with H2O/dioxane so that the compound of formula 682 is formed (ii) treatment of the product obtained at stage (i) with methanol so that the compound of formula 682 is obtained in the form of solvate with methanol (Form K) (iii) extraction of the compound of formula 682, which has been obtained at stage (ii) in the form of solvate with methanol (Form K) (iv) optional cleaning of the product of stage (iii) by recrystallisation. Besides, the invention proposes a method for obtaining the compound of formula 682-4, where the above method involves the following: (i) conversion of the compound of formula 682-1 to the compound of formula 682-2 by treatment of the above compound of formula 682-1 with 1,3-dichloro-1,1,4,4-tetraisopropyldisiloxane (CIPS) in pyridine (ii) conversion of the above compound of formula 682-2 to the compound of formula 682-3 by treatment of the above compound of formula 682-2 with acetic anhydride to EtOH and (iii) conversion of the above compound of formula 682-3 to the compound of formula 682-4 by treatment of the above compound of formula 682-3 with an oxidiser, preferably with free radical 2,2,6,6-tetramethylpiperidinyloxy (TEMPO) and NaOCl. Further aspects of the invention refer to use of the above methods for obtaining 2-cyano-2-deoxy-N4-palmitoyl-1-β-D-arabinofuranosylcytosine, pyrimidine nucleoside, and are suitable for treatment and/or prevention of cancer.EFFECT: improvement of compounds.22 cl, 1 tbl, 1 exНастоящее изобретение относится к способу получения соединения формулы 682, которое находится в кристаллической форме, где указанный способ включает: (i) обработку соединения формулы 682-9 пальмитиновым ангидридом в смеси Н2О/диоксан с образованием соединения формулы 682 (ii) обрабо
