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Mono- and Difluoromethylation of 3(2H)-Pyridazinones
Organic Letters ( IF 4.9 ) Pub Date : 2024-09-12 , DOI: 10.1021/acs.orglett.4c03002 Ziyue Zhu 1 , Jiaqi Tang 1 , Samantha Kyriazakos 1 , Alexander Knieb 1 , Yijie Xu 1 , Chao Zhang 1 , G K Surya Prakash 1
Organic Letters ( IF 4.9 ) Pub Date : 2024-09-12 , DOI: 10.1021/acs.orglett.4c03002 Ziyue Zhu 1 , Jiaqi Tang 1 , Samantha Kyriazakos 1 , Alexander Knieb 1 , Yijie Xu 1 , Chao Zhang 1 , G K Surya Prakash 1
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A method for direct N-monofluoromethylation of pyridazinones with S-monofluoromethyl-S-phenyl-2,3,4,5-tetramethylphenylsulfonium triflate is disclosed. A method for the N- and O-difluoromethylated pyridazinones with TMSCF2Br as the only promising difluorocarbene precursor is also reported. Substrates with various relevant functional groups, including analogues of Lynparza, are tolerated under both methods.
中文翻译：
3(2H)-哒嗪酮的单氟甲基化和二氟甲基化
公开了用S-单氟甲基-S-苯基-2,3,4,5-四甲基苯基锍三氟甲磺酸盐直接N-单氟甲基化哒嗪酮的方法。还报道了一种以 TMSCF 2 Br 作为唯一有前途的二氟卡宾前体的N-和O-二氟甲基化哒嗪酮的方法。两种方法均耐受具有各种相关官能团的底物，包括 Lynparza 类似物。
更新日期：2024-09-12
中文翻译：
3(2H)-哒嗪酮的单氟甲基化和二氟甲基化
公开了用S-单氟甲基-S-苯基-2,3,4,5-四甲基苯基锍三氟甲磺酸盐直接N-单氟甲基化哒嗪酮的方法。还报道了一种以 TMSCF 2 Br 作为唯一有前途的二氟卡宾前体的N-和O-二氟甲基化哒嗪酮的方法。两种方法均耐受具有各种相关官能团的底物，包括 Lynparza 类似物。
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