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胍与双亲电试剂的缩合反应：高氮杂环的形成。

Condensation reactions of guanidines with bis-electrophiles: Formation of highly nitrogenous heterocycles.

作者信息

Arnold David M, Laporte Matthew G, Anderson Shelby M, Wipf Peter

机构信息

University of Pittsburgh, Center for Chemical Methodologies and Library Development, Pittsburgh, PA 15260, USA.

出版信息

Tetrahedron. 2013 Sep 9;69(36):7719-7731. doi: 10.1016/j.tet.2013.04.127.

DOI:10.1016/j.tet.2013.04.127
PMID:23976798
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3746774/
Abstract

2-Amino-1,4-dihydropyrimidines were reacted with bis-electrophiles to produce novel fused bi-pyrimidine, pyrimido-aminotriazine, and pyrimido-sulfonamide scaffolds. In addition, a quinazoline library was constructed using a guanidine Atwal-Biginelli reaction with 1-(quinazolin-2-yl)guanidines. The product heterocycles have novel constitutions with high nitrogen atom counts and represent valuable additions to screening libraries for the discovery of new modulators of biological targets.

摘要

2-氨基-1,4-二氢嘧啶与双亲电试剂反应，生成新型稠合双嘧啶、嘧啶并氨基三嗪和嘧啶并磺酰胺骨架。此外，利用胍基阿特瓦尔-比吉内利反应，用1-(喹唑啉-2-基)胍构建了一个喹唑啉文库。产物杂环具有含氮原子数高的新型结构，是生物靶点新调节剂筛选文库的宝贵补充。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/3c1237c08e24/nihms475562f14.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/3c1237c08e24/nihms475562f14.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/409ec3beafb7/nihms475562f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/8975dea8eee7/nihms475562f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/84ca1e00d36b/nihms475562f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/8f257c008bd2/nihms475562f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/799791640ed4/nihms475562f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/99fdb925268f/nihms475562f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/2aff278189a4/nihms475562f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/7a327e1cae3d/nihms475562f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/2eab13246606/nihms475562f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/054d1058df2c/nihms475562f10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/2eab4ac9f00f/nihms475562f11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/fdc94f04b439/nihms475562f12.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/7f50c4d8b2bc/nihms475562f13.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac98/3746774/3c1237c08e24/nihms475562f14.jpg

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