由β-氟烯醇盐合成4-氨基-5-氟嘧啶和5-氨基-4-氟吡唑。
Synthesis of 4-amino-5-fluoropyrimidines and 5-amino-4-fluoropyrazoles from a β-fluoroenolate salt.
作者信息
Lucas Tobias, Dietz Jule-Philipp, Opatz Till
机构信息
Institute of Organic Chemistry, Johannes Gutenberg-University, Duesbergweg 10-14, 55128 Mainz, Germany.
出版信息
Beilstein J Org Chem. 2020 Mar 20;16:445-450. doi: 10.3762/bjoc.16.41. eCollection 2020.
Abstract
A synthesis of fluorinated pyrimidines under mild conditions from amidine hydrochlorides and the recently described potassium 2-cyano-2-fluoroethenolate was developed. A broad substrate scope was tested and mostly excellent yields were obtained. The synthesis of fluorinated aminopyrazoles from the same fluorinated precursor could be demonstrated but proceeded with lower efficiency.
摘要
开发了一种在温和条件下由盐酸脒和最近描述的2-氰基-2-氟乙烯酸钾合成氟化嘧啶的方法。测试了广泛的底物范围，并且大多获得了优异的产率。可以证明由相同的氟化前体合成氟化氨基吡唑，但效率较低。
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