114 Volume 3 • Issue 1 • 1000117 Madridge J Nov Drug Res. ISSN: 2641-5232 Madridge Journal of Novel Drug Research Research Article Open Access Regioselective C-H Borylation of C (sp 2 )-H Bond Hua-Qing Jing, Jon C Antilla and Hong-Liang Li* Institute for Molecular Design and Synthesis, School of Pharmaceutical Science and Technology, Health Science Platform, Tianjin University, Nankai District, Tianjin, China Article Info *Corresponding author: Hong-Liang Li Institute for Molecular Design and Synthesis School of Pharmaceutical Science and Technology Health Science Platform, Tianjin University Nankai District, Tianjin China E-mail: lhl522508@126.com Received: January 30, 2019 Accepted: February 19, 2019 Published: February 26, 2019 Citation: Jing HQ, Antilla JC, Li HL. Regioselective C-H Borylation of C (sp 2 )-H Bond. Madridge J Nov Drug Res. 2019; 3(1): 114-119. doi: 10.18689/mjndr-1000117 Copyright: © 2019 The Author(s). This work is licensed under a Creative Commons Attribution 4.0 International License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Published by Madridge Publishers Abstract C-H activation reactions have become a powerful method to direct functionalization of alkyl, alkenyl, and aryl C-H bonds over the past few decades. Among of them, Iridium catalyzed transformation of aryl C-H bonds to C-B bonds is one of the most useful method. However, a central challenge in these reactions is controlling their site selectivity. Over the past decade, some methods have been developed to accomplish regio- selective C-H borylation by catalysts or substrates modification. In this paper, some methods developed in recent years to realize ortho-, meta-, and para-selective C-H borylation will be summarized and their strategy and mechanism of these methods will be discussed. Keywords: Iridium; Regioselective; C-H borylation; Non-covalent bond interaction. Introduction Carbon-Carbon bond are the molecular “bricks and mortar” from which diverse architectures in living organisms and manmade materials are constructed. In the field of organic chemistry, there are numerous methods for carbon-carbon bond construction, which have been developed, ranging from traditional nucleophilic reaction to metal catalyzed reaction for formation of C-C bond. Among of them, Suzuki-Miyaura reaction has become one of the most powerful method for the construction of C-C bond since its discovery in 1979 [1]. Arylboron is an important reagent for participating in this reaction. In addition, organoboron reagents as versatile intermediates have been extensively used in synthetic chemistry because it can be converted to more complex molecules by further transformations, such as Chan-Lam-Evans coupling, [2-4] and oxidation [5-7]. Therefore, developing a highly effective method for synthesis of organoboron reagents is very desirable. Traditional methods to obtain organoboron reagents are these three methods (Scheme 1), which contains synthesis from organolithium or organomagnesium, hydroboration of alkenes or alkynes and haloboration of terminal alkynes [8]. However, there are some limitations of these methods. For example, the synthesis from organometallics usually requires stoichiometric amounts of strong base such as n-BuLi and a harsh lower temperature to use in the reaction. As for the reactions of hydroboration and haloboration, boron atom always adds to the terminal position of alkenes or alkynes. It is difficult to obtain internal boron reagents form these two methods. Besides, these three methods also are not in accordance with the rule of atomic economy. The development of transition metal catalyzed C-H borylation provides a good way for preparation of organoboron reagents, especially for aromatic boron reagents. ISSN: 2641-5232