Background and overview of application examples of 4-carboxy-2-fluorophenylboronic acid
4-Carboxy-2-fluorophenylboronic acid is a pharmaceutical intermediate that can be used for Suzuki and other metal coupling reactions. There are reports in the literature that it can be used as an intermediate to prepare WDR5 protein-protein interaction inhibitors and BTK inhibitors.
Application examples of 4-carboxy-2-fluorophenylboronic acid
Application examples of 4-carboxy-2-fluorophenylboronic acid Application 1,
4-Carboxy-2-fluorophenylboronic acid can be used to prepare a WDR5 protein-protein interaction inhibitor with the following structure. This type of compound can inhibit the level and downstream of histone methyltransferase at the cellular level. The expression of hematopoietic genes can inhibit the growth of transplanted tumors in nude mice at the animal level. It can be used in the treatment of drugs for indications related to MLL enzyme function, and can be used to treat acute leukemia and other diseases.
Application examples of 4-carboxy-2-fluorophenylboronic acid Application 2.
4-Carboxy-2-fluorophenylboronic acid can also be used to prepare BTK inhibitors with the following structure. Bruton’s tyrosine kinase (Btk), a sodium perborate monohydrate and pyridine dihydrochloride member of the Tec family of non-receptor tyrosine kinases, is a member of the Tec family of non-receptor tyrosine kinases in addition to T lymphocytes and natural killer cells. A key signaling enzyme expressed in all hematopoietic cell types. Btk plays a critical role in the B cell signaling pathway that connects cell surface B cell receptor (BCR) stimulation to downstream intracellular responses.
References
[1] [Invented in China] CN201910139980.6 Aniline WDR5 protein-protein interaction inhibitor and its preparation method and use
[2] From PCT Int. Appl., 2020052628, 19 Mar 2020
