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Convenient preparation of 4-aryl-2-(heteroarylamino)pyrimidines and 4-anilino-2-(heteroarylamino)pyrimidines

✍ Scribed by Brian I. Bliss; Feryan Ahmed; Subashree Iyer; Weimin Lin; Joel Walker; He Zhao

Book ID
104097744
Publisher
Elsevier Science
Year
2010
Tongue
French
Weight
973 KB
Volume
51
Category
Article
ISSN
0040-4039

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✦ Synopsis

4-Aryl-2-anilinopyrimidines and 2,4-dianilinopyrimidines are privileged structures found in many druglike molecules and biologically active compounds. A method for the quick assembly of novel 4-aryl-and 4-anilino-2-(heteroarylamino)pyrimidines via Buchwald-Hartwig N-arylations at elevated temperatures under sealed tube conditions is reported. This method's convenience and practicality is demonstrated through the preparation of several novel non-nucleoside reverse transcriptase inhibitor (NNRTI) analogues.

📜 SIMILAR VOLUMES

ChemInform Abstract: Convenient Preparat
ChemInform Abstract: Convenient Preparation of 4-Aryl-2-(heteroarylamino)pyrimidines and 4-Anilino-2-(heteroarylamino)pyrimidines.
✍ Brian I. Bliss; Feryan Ahmed; Subashree Iyer; Weimin Lin; Joel Walker; He Zhao 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 36 KB

## Abstract It is demonstrated that non‐nucleophilic heteroarylamines undergo Buchwald—Hartwig N‐arylation with 4‐substituted 2‐chloropyrimidines to afford drug‐like derivatives including analogues (VIc,d) of the reverse transcriptase inhibitor dapivirine.