METHODS FOR PREPARING DERIVATIVES OF PIPERAZINE AND INTERMEDIATE SUBSTANCE Russian patent published in 2008 - IPC C07D213/74 C07D213/75 C07D213/76 C07D401/12 C07D405/14 A61K31/444 A61P25/00

Abstract RU 2314294 C2

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-HT_1A receptors by the stereoselective and convergent manner.

EFFECT: improved methods of synthesis, valuable biological property of compounds.

11 cl, 11 ex

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RU 2 314 294 C2

Authors

Chan Anita Vaj-Jin

Fejgel'Son Gregg Brajan

Zeldis Dzhozef

Dzhirkovski Ivo

Dates

2008-01-10—Published

2003-03-10—Filed