Nucleoside phosphinate compounds and compositions

Details Nucleoside phosphinate compounds and compositions Nucleoside phosphinate compounds and compositions

1994-02-28

1996-04-16

Robinson, Douglas W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 48, 514 51, 536 261, 536 267, 536 268, A61K 3170

Patent

active

055082700

ABSTRACT:
A compound of formula ##STR1## where R.sup.1 is hydrogen or a protecting group Q;
R.sup.2 is hydrogen, a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.7 -C.sub.13 araliphatic radical, an alkali metal ion or an ammonium ion;
R.sup.3 and R.sup.4 are independently hydrogen, halogen or hydroxy;
R.sup.5 is C.sub.6 -C.sub.10 aryloxythiocarbonyloxy, the C.sub.6 -C.sub.10 aryl group being unsubstituted or substituted, or R.sup.5.sub.a ;
R.sup.5.sub.a is hydrogen, fluorine, chlorine, hydroxy, --OR.sup.8, --OCOR.sup.8 or silyloxy substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;
R.sup.6 is hydrogen, a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.16 araliphatic radical, --COR.sup.9, --SO.sub.2 R.sup.9 or silyl substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;
R.sup.7 is a monovalent nucleoside base radical, hydroxyl, --OR.sup.8 or --OCOR.sup.8, and
R.sup.9 are independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical or a C.sub.7 -C.sub.16 araliphatic radical; or
R.sup.5 and the indicated R.sup.6 O-together denote an isopropylidenedioxy group or R.sup.5 and R.sup.7 together denote an isopropylidenedioxy group, provided that when R.sup.5 and R.sup.7 together denote isopropylidenedioxy, R.sup.1 R.sup.2, R.sup.3 R.sup.4 and R.sup.6 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.

REFERENCES:
Tetrahedron Letters, vol. 28, No. 31, pp. 3623-3626, (1987).
Collection of Czechoslovak Chemical Communications, vol. 54, pp. 1055-1066, (1989).
Tetrahedron Letters, vol. 30, No. 19, pp. 2567-2570, (1989).
Chem. Abst. 69(9): 36381p (1968).
R. L. Whistler et al. Journal of Organic Chemistry vol. 33 No. 6, Jun. 1968 pp. 24.
Chem. Abst. vol. 99. No. 11, 88502t (1983).
Chem. abst. vol. 112, 36339N (1990).
Chem. abst. vol. 119, 96051s (1993).
H. Tanaka et al. Tetrahedron Letters vol. 30, No. 19 pp. 2567-2570 (1989).

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