Polymer Supported Synthesis of Multi-substituted Pyrimidine-4-one Derivatives via Pbf-activated Thiourea

Chemical Research in Chinese Universities ›› 2011, Vol. 27 ›› Issue (2): 221-223.

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Polymer Supported Synthesis of Multi-substituted Pyrimidine-4-one Derivatives via Pbf-activated Thiourea

LI Ji-zhen*, KOU Jing-ping and MI Yu-hua

College of Chemistry, Jilin University, Changchun 130021, P. R. China

Received:2010-06-21 Revised:2010-08-27 Online:2011-03-25 Published:2011-03-09
Contact: LI Ji-zhen E-mail:ljz@jlu.edu.cn
Supported by:
Supported by the Scientific Forefront and Interdisciplinary Innovation Project of Jilin University, China(No.421031531412) and the Jilin Provincial Research Foundation for Basic Research, China(No.3D109K856604).

Abstract

Abstract: Efficient polymer supported synthesis of multi-substituted pyrimidine-4-one derivatives was described. Target products were produced from fluorenylmethoxycarbonyl(Fmoc) protected β-amino acid loaded on hydro- xymethyl resin through deprotection, N-alkylation, guanidine formation, and cleavage of 2,2,4,6,7-pentamethyl dihydrobenzofuran-sulfonyl(Pbf) by trifluoracetic acid(TFA) followed with cyclization. The procedure has the advantages of easy operation, mild reaction conditions, and forming multiple substituents.

Key words: Guanidine, Polymer supported synthesis, Pyrimidine, Amino acid, Thiourea

LI Ji-zhen*, KOU Jing-ping and MI Yu-hua. Polymer Supported Synthesis of Multi-substituted Pyrimidine-4-one Derivatives via Pbf-activated Thiourea[J]. Chemical Research in Chinese Universities, 2011, 27(2): 221-223.

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Polymer Supported Synthesis of Multi-substituted Pyrimidine-4-one Derivatives via Pbf-activated Thiourea

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