发明名称 INDOLE CROSS-COUPLING METHOD
摘要 FIELD: chemistry. ^ SUBSTANCE: invention relates to a method of producing a compound of general formula 1 ^ ^ by reacting a substituted indole derivative I' ^ ^ with a heteroarylzinc halide of formula: or a diheteroarylzinc of formula: ^ where: L denotes Br, Cl; R denotes (C1-C8)alkyl; X denotes (C3-C8)cycloalkyl; Y denotes a 6-member heteroaryl with one or two N atoms; Z denotes HO2C-, (C1-C8)alkyl-O2C-, (C1-C6)alkyl-HNC(O)-, or in the presence of a Pd metal catalyst, a ligand selected from Ph3P, n-Tol3P, Cy3P, tpet-Bu3P, Cy2P(Ph-Ph), dppfh and dppb, in a solvent selected from tetrahydrofuran, dimethylformamide, N-methylpyrrolidone or any other combination thereof, at temperature between ambient temperature and 100C. The invention also describes intermediate compounds. ^ EFFECT: high efficiency of the method. ^ 12 cl, 3 dwg, 2 tbl, 4 ex
申请公布号 RU2430916(C2) 申请公布日期 2011.10.10
申请号 RU20060135543 申请日期 2005.03.07
申请人 BERINGER INGEL'KHAJM FARMAS'JUTIKLZ, INK. 发明人 KKHODABOKUS AKHMAD;LI GUJSHEHN;LU CHZHISJUJ;ROSHANGAR FRANK;SENANAJAKE KRIS KH'JU;SHEHN' MIN
分类号 C07D209/24;C07D209/30;C07D401/04;C07D417/02 主分类号 C07D209/24
代理机构 代理人
主权项
地址