SuzukiMe: A Tactically Mild Methylation Reagent
Тип публікації :
Препринт
Дата випуску :
3 квітня 2026 р.
Автор(и) :
Ryan Harbit
Luiz Paulo Melchior de Oliveira Leão
Serhii V. Korobko
Svitlana Sotnik
Dmytro M. Volochnyuk
Serhiy V. Ryabukhin
Joel M. Smith
eKNUTSHIR URL :
Журнал :
ChemRxiv
Цитування :
[APA 7] Ryan, H., Luiz, P. M., Serhii, V. K., Svitlana, S., Dmytro, M. V., Serhiy, V. R., & Joel, M. S. (2026). SuzukiMe: A Tactically Mild Methylation Reagent. ChemRxiv,. https://doi.org/10.26434/chemrxiv.15001572/v1
[ДСТУ] SuzukiMe: A Tactically Mild Methylation Reagent / H. Ryan та ін. ChemRxiv. 2026. DOI: 10.26434/chemrxiv.15001572/v1 (дата звернення: 11.09.2026).
A mild, efficient, and practical method for the methylation of aryl bromides and triflates utilizing activated boronate nucleophiles is described. The mildness of this cross-coupling reaction relies on the unique utilization of a preactivated, but stable mixed lithium dialkyl boronate salt that displays high reactivity and selectivity in B-alkyl Suzuki coupling events. The reaction requires no exogenous hydroxide or alkoxide base, rendering it tolerant of substrates that would typically undergo degradation under canonical Suzuki alkylation events. Amidst a broad scope that includes the late-stage methylation of natural products and drug scaffolds, this reaction also improves upon tactically similar Suzuki alkylations that suffer from low yields and/or conversion. In addition, applications in isotopic labeling were explored along with a high-throughput substrate screening assay that further unveils the breadth of this transformation, demonstrating the immense potential for these unique nucleophiles in programmatic cross-coupling.
Якщо не вказано інше, ця робота розповсюджується на умовах ліцензії Attribution 4.0 International