1256345-60-4

Usage

Uses

Used in Pharmaceutical Industry:
2-Fluoro-6-hydroxyphenylboronic acid is used as a synthetic reagent for the preparation of alkylene-bridged derivatives, which have potential applications as HIV integrase inhibitors. These derivatives, such as [(3,4-dihydro-2H-benzo[b][1,4]oxazinyl) or (piperidinyl)(biphenyl-3-yl)pyrazolo[1,5-a]pyrimidinyl](tert-butoxy)acetic acid, are being developed for the treatment of HIV infection. The compound plays a crucial role in the synthesis of these potential therapeutic agents, contributing to the development of new treatments for HIV.

Upstream product

• 150-46-9 triethyl borate 
• 456-49-5 1-fluoro-3-methoxybenzene 
• 372-20-3 3-fluorophenol 
• 185913-28-4 2-(3-fluorophenoxy)tetrahydro-2H-pyran 
• 78495-63-3 (2-fluoro-6-methoxyphenyl)boronic acid 

Downstream Products

• 1534369-41-9 3-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenol 
• 372-20-3 3-fluorophenol 

Relevant academic research and scientific papers

Rh/Pd catalysis with chiral and achiral ligands: Domino synthesis of aza-dihydrodibenzoxepines

A game of dominoes: A synthetic route to aza-dihydrodibenzoxepines is described, through the combination of a Rh-catalyzed arylation and a Pd-catalyzed C-O coupling in a single pot. For the first time, the ability to incorporate a chiral and an achiral ligand in a two-component, two-metal transformation is achieved, giving the products in moderate to good yields, with excellent enantioselectivities. Copyright

IMPROVED SYNTHESIS OF KRAS G12C INHIBITOR COMPOUND

The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2,2',2"-(1,3,5,2,4,6-trioxatriborinane-2,4,6-triyl)tris(3-fluorophenol), useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

IMPROVED SYNTHESIS OF KEY INTERMEDIATE OF KRAS G12C INHIBITOR COMPOUND

The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure (I), useful for the synthesis of compounds that target KRAS G12C mutations, such as (II).

COMBINATION THERAPY INCLUDING A KRASG12C INHIBITOR AND ONE OR MORE ADDITIONAL PHARMACEUTICALLY ACTIVE AGENTS FOR THE TREATMENT OF CANCERS

The present invention provides combination therapy that includes an KRASG12C inhibitor, such as (see Formula), or a pharmaceutically acceptable salt thereof, and one or more additional pharmaceutically active agents, particularly for the treatment of cancers. The invention also relates to pharmaceutical compositions that contain an KRASG12C inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers.

Method for synthesizing 2-fluoro-6-hydroxyphenylboronic acid

The invention belongs to the field of synthesis of pharmaceutical compounds, and provides a method for synthesizing 2-fluoro-6-hydroxyphenylboronic acid. The method comprises the following two steps:1) synthesizing an intermediate: reacting 3-fluorophenol

MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE

The present disclosure relates to bifunctional compounds, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure.