PURPOSE: To safely mass-produce in one stage an indoloquinone derivative useful as an intermediate for an antitumor agent by reacting an indole derivative with an iodobenzene bistrihalogenoacetate or iodobenzene bismethylacetate.
CONSTITUTION: This method for producing an indoloquinone derivative expressed by formula III (R1 and R2 are each a lower alkyl) is to react an indole derivative expressed by formula II (R3 is H or amino) with an iodobenzene bistrihalogenoacetate or an iodobenzene bismethylacetate expressed by formula I (X is H or a halogen). The compound expressed by formula III can safely be synthesized in a large amount and the process can be shortened by using the compound expressed by formula I. The compound expressed by formula III is used as a useful synthetic intermediate for 5-(1- aziridinyl)-3-(hydroxymethyl)-2-[(E)-hydroxy-1-propenyl]-1-methyl-4,7-indoledione, expressed by formula IV and having the antitumor activity.
SAKAGUCHI AKIHIKO
MASUDA YOSHIAKI
OGASA TAKEHIRO
KASAI MASAJI
TOMIOKA SHINJI
