Synthesis of N,N-dialkyl-1-(2-alkylthiopyrimidin-4-yl)piperidin- 4-amines as potential heat shock protein inhibitors


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A new efficient method for synthesizing promising heat shock protein inhibitors, N,N-dialkyl- 1-(2-alkylthiopyrimidin-4-yl)piperidin-4-amines, by the reaction of 2-alkyl-4-chlorothiouracils with 4-(N-alkyl-N-methylamino)piperidines was developed. 2-Alkyl-4-chlorothiouracils were synthesized by alkylation of 2-thiouracil with alkyl iodides and subsequent treatment of the intermediates with POCl3. 4-(N-Alkyl-N-methylamino)piperidines were prepared by reductive amination of 1-(tert-butoxycarbonyl)-4-piperidinone with methylamine followed by treatment of the intermediate with the appropriate aldehydes.

作者简介

V. Aldobaev

Research Center for Toxicology and Hygienic Regulation of Biologics – Branch of the State Scientific Center “Institute of Immunology” of the Federal Medical and Biological Agency of Russia

Email: zavi@ioc.ac.ru
俄罗斯联邦, 102A ul. Lenina, Bolshevik, Moscow Region, 142253

M. Prezent

N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences

Email: zavi@ioc.ac.ru
俄罗斯联邦, 47 Leninsky prosp., Moscow, 119991

I. Zavarzin

N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences

编辑信件的主要联系方式.
Email: zavi@ioc.ac.ru
俄罗斯联邦, 47 Leninsky prosp., Moscow, 119991

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