PRODUCTION OF 1-@(3754/24)2-CARBOXYPHENYL)INDAZOLE DERIVATIVE,申请号JP19920259940-传众专利搜索

PRODUCTION OF 1-@(3754/24)2-CARBOXYPHENYL)INDAZOLE DERIVATIVE

申请公布号：JPH06107641(A)

申请号：JP19920259940

申请日期：1992.09.29

申请公布日期：1994.04.19

申请人：

KYOWA HAKKO KOGYO CO LTD

发明人：IKUTA MASANORI;KATO NOBUYUKI;MIMURA TAKASHI;SUGAYA TORU;KASAI MASAJI;TOMIOKA SHINJI

分类号：B01J27/122;C07B61/00;C07D231/56

主分类号：B01J27/122

摘要：PURPOSE:To obtain a large amount of the subject compound useful as an intermediate for synthesizing a pyrazoloacridone derivative having antitumor activity by reacting a nitroindazole derivative with a benzoic acid derivative in the presence of a copper halide. CONSTITUTION:A compound of formula I (R<1> and R<2> are H, hydroxy, lower alkoxy or benzyloxy; Hal is halogen) is reacted with a compound of formula II [R<3> is CH2X (X is H, hydroxy, lower alkoxy or benzyloxy) or OC(O)R<5> (R<5> is lower alkyl); R<4> is H or nitro] in the presence of a monovalent copper halide (e.g. copper iodide) and a base (e.g. potassium carbonate) in a solvent (e.g. N,N-dimethylformamide) at 50-120 deg.C to give the objective compound of formula III. The amount of the compound of formula II to be used is 1-1.5 equivalent based on the compound of formula I, the amount of the copper halide is 0.01-0.5 equivalent and the amount of the base is 1-2 equivalents.