| abstract |
The present invention relates to a process for preparing compounds of formula (I), figure 1. Said compounds are new intermediates for the preparation of epothilone analogs, useful in the treatment of a variety of cancers and other abnormal proliferative diseases. The compounds of the formula (I) can be used to prepare, for example, analogs of the formula (II), Figure 2, which are anticancer agents. A compound of formula (II) wherein: Q is selected from the group of structures indicated in Figure 3; R1, R2, R3, R4 and R5 are selected from the group H, alkyl, substituted alkyl, or aryl and where R1 and R2 are alkyl can be joined to form a cycloalkyl; R6 is selected from the group consisting of H, alkyl, substituted alkyl, aryl, heteroaryl, cycloalkyl, or heterocycle; R7 is hydrogen or SO2R9. It is characterized in that it comprises carrying out a macrolactamization reaction in a compound of formula (I), where: X is NR7R8, N3, N (COR11) COR12 and NR9SO2R10; Q, R1, R2, R3, R4 and R5 are as indicated above; R6 and R7 are selected from the group consisting of H, alkyl, substituted alkyl, aryl, cycloalkyl, or heterocycle. For example: (1S- (1R *, 3R * (E), 7R *, 10S *, 11R *, 12R *, 16S *)) - 7,11-dihydroxy-8,8,10,12,16-pentamethyl -3- (1-methyl-2- (2-methyl-4-thiazolyl) ethenyl) -4-aza-17-oxybicyclo (14.1.0) heptadecane-5,9-dione. |