公开(公告)号：JPH02304063A

公开(公告)日：1990-12-17

申请号：JP12225089

申请日：1989-05-16

Applicant: TOSOH CORP

Inventor： KUBO AKINORI ,  KITAHARA YOSHIYASU ,  MIYAKE TOSHIO ,  KATSUURA KIMIO

IPC: C07D215/40 ,  A61K31/47 ,  A61K31/535 ,  A61P31/12 ,  C07D401/04

Abstract: NEW MATERIAL:An 8-position nitrogen-substituted 5,6-hydroquinoline-5,6-dione shown by formula I [R1, R2 and R3 are H or 1 to 6C alkyl; A is CH2CH2, CH2 OCH2, CH2CHR8CH2 (R8 is H or 1 to 6C alkyl), and a case wherein R1, R2 and R3 are H and A is CH2CH2CH2 or CH2OCH2 is omitted]. USE:Useful as a reverse transcriptase effective as a medicine for infectious diseases of retrovirus, having low toxicity. PREPARATION:The subject substance can be produced by a well-know method, for example, 6-hydroxy-2-methylquinoline is dissolved in methanol and pyrrolidine and cupric acetate are added to the solution by cooling with ice while stirring. The mixture is stirred while introducing an oxygen gas. The solvent of the reaction solution is distilled away under reduced pressure to give the objective compound shown by the formula.