CHUANGXINMYCIN DERIVATIVE AND ITS PRODUCTION

摘要

PROBLEM TO BE SOLVED: To obtain the subject new derivative having strongly antibacterial actions on gram-positive bacteria such as Staphylococcus aureus by subjecting a 1-hydropyrroloindole-6,8-dione derivative to Vilsmeier reaction, then ring formation reaction through dehydration and hydrolyzing the resultant substance. ;SOLUTION: This chuangxinmycin derivative (e.g. 3,4-dihydro-8- methylyrrolo[3,4-g]thiopyrano[4,3,2-cd]indole-4-carboxy-7,9-dione) is shown by formula I (R is a hydrocarbon group), shows specifically antibacterial actions on gram-positive bacteria such as Staphylococcus aureus and is effective for treating diseases caused by MRSA. The compound is obtained by subjecting a 1-hydropyrrolo[3,4-g]indole-6,8-dione derivative of formula II (R' is a hydrocarbon group) to Vilsmeier reaction, then formulating the reaction product at the 3-position, ring formation reaction through dehydration to form a compound of formula III and hydrolyzing the resultant substance to convert an ester group to a carboxyl group.;COPYRIGHT: (C)1998,JPO