TUBULYSINS, METHOD FOR PRODUCING THE SAME AND TUBULYSIN PREPARATIONS

摘要

The invention relates to a compound of the following general formula (tubulysin) with the following definitions for R, R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R<8> R<9>, R<10>, R<11>, S, T, U, V, W, X, Y and Z: R = H, C1-4 alkyl, aryl, OR<1>, NR<1>R<2> or NH-(CH2)2-4-; R<1> = H, C1-6 alkyl or aryl; R<2> = H, C1-6 alkyl or aryl; S = H, Hal, NO2 or NHR<3>; U = H, Hal, NO2 or NHR<3>; R<3> = H, HCO or C1-4 alkyl-CO; T = H or OR<4>; R<4> = H, C1-4 alkyl, aryl, COR<5>, P (O) (OR<6>)2 or SO3R<6>; R<5> = C1-6 alkyl, alkenyl, aryl or heteroaryl; R<6> = H, C1-4 alkyl or metal ion; V = H or R<7> or (if W = O) O; R<7> = H, C1-4 alkyl or COR<8>; R<8> = C-1-4 alkyl, alkenyl or aryl; W = H or C1-4 alkyl or (if V = O) O; X = H, C1-4 alkyl, alkenyl or CH20R<9>;< >R<9> = H, C1-4 alkyl, alkenyl, aryl or COR<10>; R<10> = C1-6 alkyl, alkenyl, aryl or heteroaryl; Y = (if Z = CH3 or COR<11>) a free electron pair or (if Z = CH3) O; R<11> = C1-4 alkyl, CF3 or aryl and/or Z = (if Y = O or a free electron pair) CH3 or (if Y = free electron pair) COR<11>.