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中国化学（英文版）
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2026年16期
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Modular Enantioselective Synthesis of Tetrahydropyridazines by Palladium-Catalyzed Aminoalkenylation/Aminoarylation Reaction
Modular Enantioselective Synthesis of Tetrahydropyridazines by Palladium-Catalyzed Aminoalkenylation/Aminoarylation Reaction
摘要
Chiral 1,4,5,6-tetrahydropyridazine core has emerged as valuable structural motifs in drug discovery,and has been recognized that the identified stereocenter of this structure has a significant impact on activity.Nevertheless,the catalytic asymmetric synthesis of such frameworks with clearly defined stereocenters remains a significant challenge,primarily due to the inherent difficulty in achiev-ing stereo control during the cyclization process,as well as the limited availability of broadly applicable efficient catalytic system.In this work,a novel palladium-catalyzed enantioselective aminoalkenylation and aminoarylation of γ,δ-unsaturated hydrazones with aryl or alkenyl halides is described.The use of a sterically demanding Xu-Phos ligand ensures excellent chemoselectivity and enanti-oselectivity.This protocol provides an efficient and practical strategy for the synthesis of structurally diverse chiral tetrahydro-pyridazines bearing alkenyl and aryl functionalities in good yields and high enantioselectivities under mild reaction conditions.Nota-bly,preliminary mechanistic investigations indicate that the syn-azapalladation was found to be the dominant pathway and might elu-cidate the high enantioselectivity in the cyclization process.
年，卷(期)：
2026, 44(16)
机标分类号：
TN929.52
R28
O643.1
在线出版日期：
2026年10月30日
