发明名称 METHODS FOR PREPARING DERIVATIVES OF PIPERAZINE AND INTERMEDIATE SUBSTANCE
摘要 FIELD: organic chemistry, chemical technology, medicine. ^ SUBSTANCE: invention proposes a method for synthesis of derivatives of piperazine, namely, N-arylpiperazines of the formula (VI): wherein R, Ar and Aryl are given in the invention claim. Method involves interaction of compound of the formula (I) with NH2R' and the following conversion of synthesized intermediate substance of the formula (II) to the end compound. Except for, invention proposes a method for synthesis of intermediate substance N1-(2'-pyridyl)-1,2-alkanediaminesulfamic acid of the formula (II) wherein R and R' have values given in the invention claim by above given the reaction scheme. Also, invention involves compound of the formula (II) and its optical isomers. Except for, invention relates to a method for synthesis of intermediate compound of the formula (V) from intermediate substance of the formula (II) and to a method for synthesis of N-arylpiperazines of the formula (VI) from intermediate compound of the formula (V). Invention provides using intermediate substance of the formula (II) for synthesis of chiral piperazine derivatives that display activity with respect to 5-HT1A receptors by the stereoselective and convergent manner. ^ EFFECT: improved methods of synthesis, valuable biological property of compounds. ^ 11 cl, 11 ex
申请公布号 RU2314294(C2) 申请公布日期 2008.01.10
申请号 RU20040130314 申请日期 2003.03.10
申请人 UAJT 发明人 CHAN ANITA VAJ-JIN;FEJGEL'SON GREGG BRAJAN;ZELDIS DZHOZEF;DZHIRKOVSKI IVO
分类号 C07D213/74;A61K31/444;A61P25/00;C07D213/75;C07D213/76;C07D401/12;C07D405/12;C07D405/14 主分类号 C07D213/74
代理机构 代理人
主权项
地址