Epothilons C and D, preparation and compositions

Epothilon derivative of formula 3

• wherein
• R=H, C1-4alkyl;
• R1, R2=H, C1-6alkyl, C1-6acyl, benzoyl, C1-4trialkylsilyl, benzyl, phenyl, or benzyl or phenyl each substituted by C1-6alkoxy, C6alkyl, hydroxy or by halogen;
• the alkyl and acyl groups contained in the radicals are straight-chain or branched radicals, and X generally represents —C(O)—, —C(S)—, —S(O)—, —CR1R2— or —SiR2—, wherein R, R1 and R2 are as defined above and R1 and R2 may also together form an alkylene group having from 2 to 6 carbon atoms;
• and Y and Z are either identical or different and each represents hydrogen, halogen, pseudohalogen, OH, O—(C1-6)acyl, O—(C1-6)alkyl or O-benzoyl, or together form the O atom of an epoxy group or one of the C—C bonds of a C═C double bond.

Epothilon derivative of formula 6

• wherein
• R=H, C1-4alkyl;
• R1=H, C1-6alkyl, C1-6acyl, benzoyl, C1-4trialkylsilyl, benzyl, phenyl, or benzyl or phenyl each substituted by C1-6alkoxy, C6alkyl, hydroxy or by halogen;
• the alkyl and acyl groups contained in the radicals are straight-chain or branched radicals;
• and Y and Z are either identical or different and each represents hydrogen, halogen, pseudohalogen, OH, O—(C1-6)acyl, O—(C1-6)alkyl or O-benzoyl, or together form the O atom of an epoxy group or one of the C—C bonds of a C═C double bond.

Epothilon derivative of formula 7

• wherein
• R=H, C1-4alkyl;
• R1, R2, R3, R4=H, C1-6alkyl, C1-6acyl, benzoyl, C1-4trialkylsilyl, benzyl, phenyl, or benzyl or phenyl each substituted by C1-6alkoxy, C6alkyl, hydroxy or by halogen;
• the alkyl and acyl groups contained in the radicals are straight-chain or branched radicals;
• and Y and Z together form the O atom of an epoxy group or one of the C—C bonds of a C═C double bond.