1016644-38-4

Usage

Uses

Used in Pharmaceutical Industry:
2-Oxo-2,3-dihydrobenzo[d]oxazol-6-yl-boronic acid is used as a potential pharmaceutical agent for drug discovery and development. Its ability to form reversible covalent complexes with biological molecules makes it a candidate for targeting specific biological pathways or interactions in the design of new drugs.
Used in Drug Discovery:
In the field of drug discovery, 2-Oxo-2,3-dihydrobenzo[d]oxazol-6-yl-boronic acid is utilized as a chemical probe to explore and understand the interactions between biological molecules and potential drug candidates. This can aid in the identification of novel therapeutic targets and the optimization of drug candidates for enhanced efficacy and selectivity.

Upstream product

• 19932-85-5 6-bromobenzo[d]oxazol-2(3H)-one 
• 13675-18-8 tetrahydroxydiboron 
• 22876-17-1 6-amino-1,3-benzoxazol-2-(3H)-one 
• 14733-73-4 5-bromo-1,3-benzoxazol-2(3H)-one 

Downstream Products

• 1076188-10-7 6-[6-(2-chlorophenyl)-2-oxo-1,2-dihydropyrimidin-4-yl]-1,3-benzoxazol-2(3H)-one 

Relevant academic research and scientific papers

Pd- And Ni-Based Systems for the Catalytic Borylation of Aryl (Pseudo)halides with B2(OH)4

Despite recent advancements in metal-catalyzed borylations of aryl (pseudo)halides, there is a continuing need to develop robust methods to access both early-stage and late-stage organoboron intermediates amendable for further functionalization. In particular, the development of general catalytic systems that operate under mild reaction conditions across a broad range of electrophilic partners remains elusive. Herein, we report the development and application of three catalytic systems (two Pd-based and one Ni-based) for the direct borylation of aryl (pseudo)halides using tetrahydroxydiboron (B2(OH)4). For the Pd-based catalyst systems, we have identified general reaction conditions that allow for the sequestration of halide ions through simple precipitation that results in catalyst loadings as low as 0.01 mol % (100 ppm) and reaction temperatures as low as room temperature. We also describe a complementary Ni-based catalyst system that employs simple unligated Ni(II) salts as an inexpensive alternative to the Pd-based systems for the borylation of aryl (pseudo)halides. Extrapolation of all three systems to a one-pot tandem borylation/Suzuki-Miyaura cross-coupling is also demonstrated on advanced intermediates and drug substances.

Sequential one-pot access to molecular diversity through aniline aqueous borylation

On the basis of our recently reported aniline aqueous borylation, molecular diversity was achieved in a one-pot process by combining other reactions such as esterification, Suzuki-Miyaura coupling, hydrogenolysis, or Petasis borono-Mannich.

6-PHENYLPYRIMIDINONES AS PIM MODULATORS

A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.