| 摘要 |
The present invention relates to a method for the preparation of a compound of formula (I) or pharmaceutically acceptable salts thereof and intermediates thereof, comprising the steps of: a) halogenating a compound of formula (II), resulting in compound of formula (IIa), b) reacting a compound of formula (IIa) at its 14 position with the thiol moiety of a peptide of formula (III), optionally in the presence of a suitable linker, to obtain said compound of formula (I), wherein R1 represents OH, NH2 or NH-peptide; R2 represents H or -CO-peptide; R3 represents OCH3, OH or H; R4 represents H, or COCF3; R5 represents OH, O-tetrahydropyranyl or H; R6 represents OH or H; R7 represents H, OH, OCO(CH2)3CH3 or OCOCH(OC2H5)2; R8 represents OH or H; R9 represents OH or H; R10 represents a halogen and L is an optional suitable linker arm.
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