Nucleoside phosphinate compounds and compositions
First Claim
1. A compound of formula ##STR107## where R1 is hydrogen or Q, wherein Q is a protecting group;
- R2 is hydrogen, a C1 -C8 aliphatic radical, a C6 -C15 aromatic radical, a C3 -C8 cycloaliphatic radical, a C7 -C13 araliphatic radical, an alkali metal ion or an ammonium ion;
R3 and R4 are independently hydrogen, halogen or hydroxy;
R5 is C6 -C10 aryloxythiocarbonyloxy, the C6 -C10 aryl group being unsubstituted substituted, or R5a ;
R5a is hydrogen, fluorine, chlorine, hydroxy. --OR8, --OCOR8 or silyloxy substituted by three C1 -C15 hydrocarbyl groups;
.R6 is hydrogen, a C1 -C10 aliphatic radical. a C6 -C15 aromatic radical, a C7 -C16 araliphatic radical, --COR9, --SO2 R9 or silyl substituted by three C1 -C15 hydrocarbyl groups;
R7 is a monovalent nucleoside base radical, hydroxyl, --OR8 or --OCOR8, andR8 and R9 are independently a C1 -C10 aliphatic radical, a C3 -C8 cycloaliphatic radical, a C6 -C15 aromatic radical or a C7 -C16 araliphatic radical;
orR5 and the indicated R6 O-- together denote an isopropylidenedioxy group or R5 and R7 together denote an isopropylidenedioxy group, provided that when R5 and R7 together denote an isopropylidenedioxy group, R1, R2, R3, R4 and R6 are not all hydrogen.
1 Assignment
0 Petitions
Accused Products
Abstract
A compound of formula ##STR1## where R1 is hydrogen or a protecting group Q;
R2 is hydrogen, a C1 -C8 aliphatic radical, a C6 -C15 aromatic radical, a C3 -C8 cycloaliphatic radical, a C7 -C13 araliphatic radical, an alkali metal ion or an ammonium ion;
R3 and R4 are independently hydrogen, halogen or hydroxy;
R5 is C6 -C10 aryloxythiocarbonyloxy, the C6 -C10 aryl group being unsubstituted or substituted, or R5a ;
R5a is hydrogen, fluorine, chlorine, hydroxy, --OR8, --OCOR8 or silyloxy substituted by three C1 -C15 hydrocarbyl groups;
R6 is hydrogen, a C1 -C10 aliphatic radical, a C6 -C15 aromatic radical, a C7 -C16 araliphatic radical, --COR9, --SO2 R9 or silyl substituted by three C1 -C15 hydrocarbyl groups;
R7 is a monovalent nucleoside base radical, hydroxyl, --OR8 or --OCOR8, and
R9 are independently a C1 -C10 aliphatic radical, a C3 -C8 cycloaliphatic radical, a C6 -C15 aromatic radical or a C7 -C16 araliphatic radical; or
R5 and the indicated R6 O-together denote an isopropylidenedioxy group or R5 and R7 together denote an isopropylidenedioxy group, provided that when R5 and R7 together denote isopropylidenedioxy, R1 R2, R3 R4 and R6 are not all hydrogen. The disclosure further relates to a method of preparing the compounds of formula I by reacting a olefinic acetonide with a phosphinate compound and to the use of the compounds of formula I as pharmaceutical agents.
216 Citations
10 Claims
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1. A compound of formula ##STR107## where R1 is hydrogen or Q, wherein Q is a protecting group;
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R2 is hydrogen, a C1 -C8 aliphatic radical, a C6 -C15 aromatic radical, a C3 -C8 cycloaliphatic radical, a C7 -C13 araliphatic radical, an alkali metal ion or an ammonium ion; R3 and R4 are independently hydrogen, halogen or hydroxy; R5 is C6 -C10 aryloxythiocarbonyloxy, the C6 -C10 aryl group being unsubstituted substituted, or R5a ; R5a is hydrogen, fluorine, chlorine, hydroxy. --OR8, --OCOR8 or silyloxy substituted by three C1 -C15 hydrocarbyl groups;
.R6 is hydrogen, a C1 -C10 aliphatic radical. a C6 -C15 aromatic radical, a C7 -C16 araliphatic radical, --COR9, --SO2 R9 or silyl substituted by three C1 -C15 hydrocarbyl groups; R7 is a monovalent nucleoside base radical, hydroxyl, --OR8 or --OCOR8, and R8 and R9 are independently a C1 -C10 aliphatic radical, a C3 -C8 cycloaliphatic radical, a C6 -C15 aromatic radical or a C7 -C16 araliphatic radical;
orR5 and the indicated R6 O-- together denote an isopropylidenedioxy group or R5 and R7 together denote an isopropylidenedioxy group, provided that when R5 and R7 together denote an isopropylidenedioxy group, R1, R2, R3, R4 and R6 are not all hydrogen. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
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Specification