- A Strategy for the Triarylation of Pyrrolopyrimidines by Using Microwave-Promoted Cross-Coupling Reactions
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New pyrrolo[2,3-d]pyrimidines that have aryl groups at the 2-, 4-, and 6-positions were prepared by the arylation reaction of 4-chloro-7-methyl-2-(methylthio)-6-phenylpyrrolo[2,3-d]pyrimidine (6) and the corresponding arylboronic acid under Suzuki-Miyaura conditions followed by a second arylation under Liebeskind-Srogl cross-coupling conditions. A parallel study that began with the C-2 chemoselective arylation of 6 under Liebeskind-Srogl conditions followed by a Suzuki-Miyaura coupling at C-4 was carried out, and the results of each route were compared. All of the tranformations were performed under microwave irradiation. Several triarylpyrrolopyrimidines were readily prepared from 4,6-dichloro-2-(methylthio)pyrimidine (2) in excellent yields by using effective cross-coupling reactions. An advantage of this method is its tolerance towards various substituted aryl groups.
- Prieur, Vanessa,Pujol, M. Dolors,Guillaumet, Gérald
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- Discovery of High-Affinity Inhibitors of the BPTF Bromodomain
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The dysfunctional bromodomain PHD finger transcription factor (BPTF) exerts a pivotal influence in the occurrence and development of many human diseases, particularly cancers. Herein, through the structural decomposition of the reported BPTF inhibitor TP-
- Lu, Tian,Lu, Haibo,Duan, Zhe,Wang, Jun,Han, Jie,Xiao, Senhao,Chen, HuanHuan,Jiang, Hao,Chen, Yu,Yang, Feng,Li, Qi,Chen, Dongying,Lin, Jin,Li, Bo,Jiang, Hualiang,Chen, Kaixian,Lu, Wenchao,Lin, Hua,Luo, Cheng
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p. 12075 - 12088
(2021/09/02)
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