专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:US-3954771-A 优先权日:1972-06-16 标题 :Process for the preparation of 2H-3-isoquinolones 发明人:GEERTS JEAN-PIERRE JULES; LINZ RAYMOND ARMAND 权利人:UCB SA 摘要:A process for the preparation of 2H-3-isoquinolones having the formula ##SPC1## n Wherein R 1 and R 2 are each hydrogen, halogen, lower alkyl, lower alkoxy, aryl, haloaryl, alkylaryl or alkoxyaryl; R 3 and R 4 are each hydrogen, lower alkyl, lower alkoxyalkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl, or halo-aralkyl, which comprises cyclizing an N-formyl-2-phenyl-acetamide of the formula ##SPC2## n Wherein R 1 , R 2 , R 3 and R 4 have the same meaning as above, with a cyclodehydration agent. Said 2H-3-isoquinolones are useful as starting materials e.g. in the synthesis of 1,4-dihydro-1,4-etheno-isoquinolin-3(2H)-ones which are valuable chemotherapeutic agents in the treatment of disorders of the central nervous system, such as troubles of wakefulness, disorders of equilibrium and vertigo.
专利号:EP-1200824-A4 优先权日:1999-06-15 标题 :SOLID PHASE SYNTHESIS OF N, N-DISUBSTITUTED DIAZACYCLOALKYLCARBOXY DERIVATIVES
专利号:US-4041077-A 优先权日:1975-05-27 标题 :N-benzyl-2,2-dimethoxy-acetamides 发明人:GHOSEZ LEON; ROSSEY GUY; DIDDEREN FREDDY 权利人:UCB SA 摘要:N-benzyl-2,2-dimethoxy-acetamides having the formula ##STR1## and processes for preparing the same. These acetamides are useful for the production of 2H-3-isoquinolones by acid cyclization and said 2H-3-isoquinolones are in turn useful as starting materials inter alia in the synthesis of 1,4-dihydro-1,4-etheno-isoquinolin-3(2H)ones, which are valuable chemotherapeutic agents as disclosed in U.S. Pat. No. 3,781,436.
专利号:WO-9967192-A2 优先权日:1998-06-24 标 题 :PROCESS FOR THE SOLID PHASE SYNTHESIS OF ALDEHYDE, KETONE, OXIME, AMINE, HYDROXAMIC ACID AND α,β-UNSATURATED CARBOXYLIC ACID AND ALDEHYDE COMPOUNDS
专利号:EP-1089958-A4 优先权日:1998-06-24 标题:SOLID PHASE SYNTHESIS OF ALDEHYDE, KETONE, OXIME, AMINE, HYDROXAMIC ACID AND CARBOXYLIC ACID COMPOUNDS $ g (a), $ g (b) -UNSATURES AND ALDEHYDE