Shet Harshita, Patel Manisha, Waikar Jyoti M, More Pavan M, Sanghvi Yogesh S, Kapdi Anant R
Department of Chemistry, Institute of Chemical Technology, Nathalal Parekh Road, Matunga, Mumbai, 400019, India.
Department of Chemistry, Institute of Chemical Technology-Indian Oil Odisha Campus, IIT Kharagpur Extension Centre, Mouza Samantpuri, Bhubaneswar, 751013, Odisha, India.
Chem Asian J. 2023 Jan 3;18(1):e202201006. doi: 10.1002/asia.202201006. Epub 2022 Nov 26.
The dimethylamino functionality has significant importance in industrially relevant molecules and methodologies to install these efficiently are highly desirable. We report herein a highly efficient, room-temperature dimethylamination of chloroheteroarenes performed via the in-situ generation of dimethylamine using N,N-dimethylformamide (DMF) as precursor wiith a large substrate scope that includes various heteroarenes, purines as well as commercially relevant drugs such as altretamine, ampyzine and puromycin precursor.
二甲氨基官能团在与工业相关的分子中具有重要意义，因此非常需要能够高效引入这些官能团的方法。我们在此报告了一种高效的、室温下通过使用N,N-二甲基甲酰胺（DMF）作为前体原位生成二甲胺来对氯杂芳烃进行二甲氨基化反应，该反应具有广泛的底物范围，包括各种杂芳烃、嘌呤以及如六甲蜜胺、安吡嗪和嘌呤霉素前体等具有商业相关性的药物。
