| 摘要 |
1501438 Fused - pyrimidine - 4(3H) - ones PFIZER Inc 2 May 1975 [5 July 1974] 18583/75 Addition to 1458205 Heading C2C Novel compounds I, II and III and salts thereof in which R is Me, Et, MeCO or COR<SP>0</SP> (where R‹ is OH, alkoxy, hydroxyalkoxy, NH 2 or NHOH); Y is H, alkyl, carbalkoxyalkyl, carboxyalkyl, -(CH 2 ) m -OCOPh or -(CH 2 ) m -OCOalkyl (where m is 2 to 4) with the proviso that when R<SP>0</SP> is NH 2 or NHOH then Y is H; R<SP>1</SP> is H, alkyl or Ph and R<SP>2</SP>, R<SP>3</SP>, R<SP>4</SP> and R<SP>5</SP> are selected from (a), H, alkyl, alkoxy, halo, benzyloxy, MeS and MeSO or (b) OH, SH, alkanoyloxy, benzoyloxy, benzylthio and benzylsulphinyl providing that at least one is selected from (b); are prepared by methods analogous to those described in the parent Specification for compounds where R is COR‹; compounds I (Y= H; R=Me, Et) are prepared oyclizing the appropriate 2 - amino - quinoline - 3 - carboxamide or 2-aminonicotinamide either with Ac 2 O or (EtCO) 2 O or with (EtO) 3 Me or (EtO) 3 Et in the presence of H 2 SO 4 ; compounds I (R= MeCO) are prepared by oxidation of the corresponding compound (R=Et) using SeO 2 ; compounds I where Y Is other than H are prepared by alkylation of such compounds where Y=H using an appropriate alkylating agent. Compounds where R‹ is hydroxyalkyl are prepared by transesterification of compounds where R‹ is alkoxy. Compounds where any one of R 2 , R 3 , R 4 or R 5 is MeSO or B 3 SO are prepared by oxidation of corresponding MeS or B 3 S compound. Compounds where R 2 , R 3 , R 4 or R 5 are B 3 O or B 3 S are debenzylated to give the corresponding OH or SH compounds and these compounds may in turn be acylated to give compounds containing an alkanoyloxy or benzyloxy substituent. Compounds I, II and III have anti-allergy activity and form with a carrier a pharmaceutical composition which may be administered orally, parenterally or by inhalation. |
