TRIFLUOROMETHYLPYRROLOINDOLE DERIVATIVE AND ITS PRODUCTION

摘要

PURPOSE:To obtain a new compound useful as a low-toxic antitumor agent having both antimicrobial and antitumor activities, high selectivity to cancer cells, and also effectiveness to solid tumors. CONSTITUTION:This derivative is a compound expressed by formula I or formula II [R<1> is an alpha-amino acid residue or expressed by formula III (X<1> to X<3> are each H, OH, OR<3>, etc.; R<3>is a 1-6C alkyl, etc.; (n) is 0-2); R<2> is a protective group for H or OH; Y is a halogen, allenesullonyloxy, etc.], an optically active substance or salt thereof, e.g. 3-[5-[(benzofuran-2-ylcarbonyl)amino]-1H-indol-2- ylcarbonyl]-1-chloromethyl-5-hydroxy-8-trifluoromethyl-1,2,3,6tetrahyd ropyrrolo [3,2-e]indole. The derivative is obtained by deprotecting a compound expressed by formula IV (R<8> is a protective group for H or OH; R<9> is an amino-protecting group) and then acylating the resultant compound.