Silyl ethers of rapamycin

Details Silyl ethers of rapamycin Silyl ethers of rapamycin

C - Chemistry, Metallurgy

07

H

C07H 23/00 (2006.01) C07F 7/10 (2006.01) C07F 7/18 (2006.01) C07H 19/24 (2006.01)

Patent

CA 2063962

AHP-9801 ABSTRACT A compound of the structure Image wherein R1 is -SiR3R4R5; R2 is hydrogen or -SiR3R4R5; and R3. R4. and R5 are each, independently, alkyl, alkenyl, aralkyl, triphenylmethyl, or phenyl which by virtue of its of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections. This invention also provides a method of using rapamycin 42-[O-[(1,1-dimethylethyl)-dimethylsilyl] ether for the preparation of 31-substituted rapamycin derivatives.

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