Patent ID: 6177573
Filing Date: 2001-01-23
Classification: C07B,C07C,C07D,C07F,C08L,C12P

Abstract:
An oxazolidine ester of silylated baccatin III of formula (VII) ##STR9##where X.sub.2 is:(1) --H,(2) --.phi. optionally substituted with 1 or 2(a) --O--X.sub.2-1 where X.sub.2-1 is C.sub.1 -C.sub.3 alkyl,(b) --F, --Cl, --Br, --I;where X.sub.3 is --SO.sub.2 --X.sub.3-1 where X.sub.3-1 is:(1) 4-nitrophenyl,(2) 2,4-dinitrophenyl,(3) 2-benzothiazol,(4) 9-anthracenyl,(5) 5-methyl-1,3,4-thiadiazolyl;where R.sub.6 and R.sub.7 are:(1) R.sub.6 is --H:--H and R.sub.7 is .alpha.-H:.beta.-OR.sub.7-1 where R.sub.7-1 is --Si(R.sub.7-2).sub.3where R.sub.7-2 is C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.7 cycloalkyl or mixtures thereof, and(2) R.sub.6 is R.sub.61 :R.sub.62 and R.sub.7 is R.sub.71 :R.sub.72 where one of R.sub.61 and R.sub.62 and one of R.sub.71and R.sub.72 are taken together to form a second bond between the carbon atoms to which they are attached and the other of R.sub.61 and R.sub.62 is --H, and the other of R.sub.71 and R.sub.72 is --H;where R.sub.10 is:(1) .alpha.-H:.beta.-O--CO--CH.sub.3 and(2) .alpha.-H:.beta.-O--CO--O--CH.sub.2 --CCl.sub.3 ;where R.sub.11, R.sub.12 and R.sub.13 are:(1) R.sub.11 and R.sub.12 are taken together to form a second bond between the carbon atoms to which they are attached and R.sub.13 is --H,(2) R.sub.12 and R.sub.13 are taken together to form a second bond between the carbon atoms to which they are attached and R.sub.11 is --H.