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METHODS FOR GLYCOSGINOPHYLIPIDS OBTAINING AND THEIR APPLICATION
专利权人:
NESHNL TAJVEN YUNIVERSITI
发明人:
LYAN Pi-Khuej (US),ЛЯН Пи-Хуэй (US)
申请号:
RU2013136531
公开号:
RU0002636587C2
申请日:
2012.01.05
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: pharmacology.SUBSTANCE: method for preparation of a compound of formula , where R1 is OH, X is C8 alkylene, R3 is OH or H, R4 is OH or H, R5 is aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that when R3 is H and R4 is H, then R5 is phenyl substituted with one or two groups independently selected from -F, -Cl, -Br, -OCH3, -OCH(CH3)2, -OPh, -OPh(4-F), 2-(5-F)-pyridinyl, -CF3, -NO2, -N(CH3)2 and 3-(6-F)-O-pyridinyl; or R5 is pyridinyl substituted by a group independently selected from -F- or -OPh (4-F); when R3 is H and R4 is OH, then R5 is phenyl substituted by a group independently selected from -F- or -OCH3, or R5 is phenyl substituted by two -F; when R3 is OH and R4 is OH, then R5 is phenyl substituted by one or two groups independently selected from -F or -OCH3; includes: (a) formula compound reacting with a formula compound in the presence of Lewis acid to form a formula compound, wherein PG is a hydroxyl protecting group and LG is a thiol-containing leaving group of the formula:, , or ; (b) formula (5) compound reduction to obtain a formula compound; (c) formula (3) compound combination with a formula compound, where X is C8 alkylene or C8 alkenylene to provide a formula compound and deprotection of the formula (2) compound, where PG is a hydroxyl protecting group, by hydrogen under hydrogenation catalysis conditions to obtain the formula (1) compound.EFFECT: new compounds, effective as ligands for natural killer T cells, new efficient methods for their production and new antiviral, antibacterial, antineoplastic agents based on them are proposed.23 cl, 39 ex, 1 tbl, 9 dwgИзобретение относится к способам получения альфа-гликосфинголипидов и новым альфа-гликосфинголипидам, фармацевтическим композициям на их основе, применимым в фармацевтической промышленности. Способ получения соединения формулы (1)где R1 представляет собой ОН, X представляет собой С8 алкилен, R3 представляет собой ОН или Н, R4 представляет собой ОН или Н,
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