| 摘要 |
Provided are a novel phosphinine oxide derivative and a preparation method thereof, and more specifically, the phosphinine oxide derivative includes an oxaphosphinine oxide derivative and an azaphosphinine oxide derivative.;The phosphinine oxide derivative according to the present invention may have a pharmacological activity and a physiological activity, and may be used as a basic framework of a natural product and may be used for development of new drug and synthesis of various medical supplies.;In addition, according to the preparation method of the phosphinine oxide derivative according to the present invention, various phosphinine oxide derivatives with a high yield may be prepared by a simple synthesis process using an intramolecular annulation between a phosphinic derivative and an alkyne derivative in the presence of a rhodium (Rh) catalyst or a ruthenium (Ru) catalyst and an oxidant. |
| 主权项 |
1. A phosphinine oxide derivative represented by the following Chemical Formula 1: in Chemical Formula (1), X is NR′ or O; R′ is C1-C20 alkyl or C6-C20 aryl; R1 and R2 are each independently hydrogen, C1-C20 alkyl or C6-C20 aryl, or R1 and R2 may be linked to each other by —CR11═CR12—CR13═CR14— or -L-CR15═CR16— to form a fused ring; R11 to R16 are each independently hydrogen, C1-C20 alkyl, halo C1-C20 alkyl, C1-C20 alkoxy, C6-C20 aryl, halogen, C1-C20 alkylcarbonyl or hydroxyl, or may be linked to an adjacent substituent by C2-C7 alkenylene, C2-C7 alkylenedioxy or —CR17═CR18—OC(═O)— to form a fused ring; R17 and R18 are each independently C1-C20 alkyl or C6-C20 aryl; L is NR″, O or S; R″ is hydrogen or C1-C20 alkyl; R3 and R4 are each independently C1-C20 alkyl or C6-C20 aryl; and R5 is C1-C20 alkoxy, C6-C20 aryl or C3-C20 heteroaryl, wherein the alkyl and aryl of R1, R2, R3 and R4, and the alkoxy, aryl, and heteroaryl of R5 may be further substituted with at least one substituent selected from the group consisting of halogen, C1-C20 alkyl, C1-C20 alkoxy and halo C1-C20 alkyl, respectively. |
