| 摘要 |
1357449 Furoquinoline compounds SCHERINGAG 15 June 1971 [18 June 1970] 28006/71 Heading C2C The invention comprises compounds of formula (and the salts of those compounds where R<SP>1</SP> is H), wherein R and R<SP>1</SP> are each H or alkyl, and A is in which X-Y-Z is -OCH 2 CH 2 -, or -COOCO-. These compounds are prepared by (1) heating at above 200‹ C. the corresponding 2,2 - di - (alkoxycarbonyl)vinylamino - benzofuran or -isobenzofuran, or heating in presence of POCl 3 followed by hydrolysis of the initial product, (2) (where X-Y-Z is -OCH 2 CH 2 -) catalytically hydrogenating the fully unsaturated analogue, (3) optionally transesterifying, hydrolysing or N-alkylating the product of methods (1) and (2). 5-Amino-2,3-dihydrobenzofuran is prepared by reduction (H 2 /Pd-C) of 5 - nitrobenzofuran. Therapeutic compositions, preferably administered orally, comprise compounds of Formula I which are active against staphylococci and Gramnegative bacteria. |
