7073-69-0Relevant articles and documents
Synthesis method of montelukast sodium intermediate
-
Paragraph 0065; 0066, (2021/03/03)
The invention is applicable to the technical field of medicine synthesis, and provides a synthesis method of a montelukast sodium intermediate. The method comprises the following steps of: generatinga compound II from halogenated benzene under the action
Benzoxaborole Catalyst for Site-Selective Modification of Polyols
Kusano, Shuhei,Miyamoto, Shoto,Matsuoka, Aki,Yamada, Yuji,Ishikawa, Ryuta,Hayashida, Osamu
supporting information, p. 1598 - 1602 (2020/02/11)
The site-selective modification of polyols bearing several hydroxyl groups without the use of protecting groups remains a significant challenge in synthetic chemistry. To address this problem, novel benzoxaborole derivatives were designed as efficient catalysts for the highly site-selective and protecting-group-free modification of polyols. To identify the effective substituent groups enhancing the catalytic activity and selectivity, a series of benzoxaborole catalysts 1a–k were synthesized. In-depth analysis for the substituent effect revealed that 1i–k, bearing multiple electron-withdrawing fluoro- and trifluoromethyl groups, exhibited the greatest catalytic activity and selectivity. Moreover, 1i-catalyzed benzoylation, tosylation, benzylation, and glycosylation of various cis-1,2-diol derivatives proceeded with good yield and site-selective manner.
Spatial anion control on palladium for mild C-H arylation of arenes
Dhankhar, Jyoti,González-Fernández, Elisa,Dong, Chao-Chen,Mukhopadhyay, Tufan K.,Linden, Anthony,?ori?, Ilija
supporting information, p. 19040 - 19046 (2020/11/13)
C-H arylation of arenes without the use of directing groups is a challenge, even for simple molecules, such as benzene. We describe spatial anion control as a concept for the design of catalytic sites for C-H bond activation, thereby enabling nondirected C-H arylation of arenes at ambient temperature. The mild conditions enable late-stage structural diversification of biologically relevant small molecules, and site-selectivity complementary to that obtained with other methods of arene functionalization can be achieved. These results reveal the potential of spatial anion control in transition-metal catalysis for the functionalization of C-H bonds under mild conditions.