abstract |
Epothilone derivatives (I) are new. They are prepared from a number of new and known starting compounds. Epothilone derivatives of formula (I) are new. R<1>a, R<1>b = H, 1-10C alkyl, aryl, 7-20C aralkyl or together form (CH2)m; m = 2-5; R<2>a, R<2>b = have the same meanings as R<1>a and R<1>b, provided that when D-E is CH2-CH2 or Y is O, then R<2>a and R<2>b are not H or CH3; R<3>, R<5> = H, 1-10C alkyl, aryl or 7-20C aralkyl; R<4>a, R<4>b have the same meanings as R<1>a, R<1>b or R<2>a, R<2>b; D-E = CH2-CH2, CH=CH, C?=C, epoxy, CH(OH)-CH(OH) or CH(OH)-CH2; R<6>, R<7> = H, or together form a bond or an O atom; R<8> = H, 1-10C alkyl, aryl or 7-20C aralkyl, which are all optionally substituted; X = O, two OR<23> groups, a 2-10C alkylene- alpha , w-dioxy group, H/OR<9> or CR<10>R<11>; R<23> = 1-20C alkyl; R<9> = H or a protecting group; R<10>, R<11> = H, 1-10C alkyl, aryl or 7-20C aralkyl, or together form a 5-7 membered carbocycle; Y = one O or two H atoms; Z = one O atom or H/OR<12>; and R<12> = H or a protecting group. |