Process for preparing caspofungin and novel intermediates thereof

摘要

The present invention relates to a novel process for preparing the aza cyclohexapeptide compound 1-[(4R,5S)-5-[(2-aminoethyl)amino]-N2-(10,12-dimethyl-1-oxotetradecyl)-4-hydroxy-L-ornithine]-5-[(3R)-3-hydroxy-L-ornithine]-pneumocandin B0 (caspofungin) represented by the following formula 1, which can improve the problem due to a pungent odor and toxicity during the process and can prepare caspofungin as a final product at high yield compared to conventional processes, and to novel intermediates which are used in the preparation process:;

主权项

1. A process of preparing a compound of the following formula 1 or an acid addition salt thereof comprising the step of reacting a compound of the following formula 5 with 1,2-diaminoethane:wherein R1 is —(CH2)nC(═O)OR2, or —(CH2)nC(═O)NH(CH2)mNH2, wherein R2 is H or C1-C3 alkyl, n=1, 2 or 3, and m=1, 2 or 3.