84198-76-5

Upstream product

• 349-75-7 3-(trifluoromethyl)benzyl alcohol 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 75-44-5 phosgene 

Downstream Products

• 1400654-59-2 C₁₈H₂₁F₃N₂O₅ 

Relevant academic research and scientific papers

Novel biphenyl tetrazole derivative and preparation method thereof

The invention relates to a novel biphenyl tetrazole derivative. A chemical general molecular formula of the novel biphenyl tetrazole derivative is shown as the accompanying drawing. The invention also relates to a preparation method of the novel biphenyl tetrazole derivative. A synthesis path is shown as the accompanying drawing, wherein n is selected from 0, 1, 2, 3, 4 and 5; Y is selected from -Br, -Cl, -NO2 and a substance shown as the accompanying drawing; R1, R2 and R3 are selected from -H, mono-substituted or poly-substituted -F, -(CH2)mCH3, -(CH2)mCF3, -O(CH2)mCH3, -O(CH2)mCF3 and -NO2 groups; m is selected from 0, 1, 2, 3, 4 and 5. The method comprises the operation steps that a compound II and 1,4-diazido dicyclic [2.2.2] octane are dissolved into a mixed reaction solution of a first organic solvent and carbon disulfide; filtering is performed to obtain yellow solids; after washing drying, the materials are dissolved into a second organic solvent; triphosgene or diphosgene is added; or phosgene reaction is performed; filtering is performed; filter liquid is collected; concentration is performed to obtain a crude product; the crude product is dissolved into a third organic solvent; ammonia water is added; concentration is performed to obtain yellow solid crude products; the solid crude products are dissolved into a four organic solvent; then, NaN3, I2 and organic amine NHpR are sequentially added into the organic solvent; basic water solution is added for quenching reaction; a fifth organic solvent is used for extracting the organic layer; concentration and purification are performed; a compound III is obtained.

SAR development of lysine-based irreversible inhibitors of transglutaminase 2 for huntington's disease

We report a series of irreversible transglutaminase 2 inhibitors starting from a known lysine dipeptide bearing an acrylamide warhead. We established new SARs resulting in compounds demonstrating improved potency and better physical and calculated properties. Transglutaminase selectivity profiling and in vitro ADME properties of selected compounds are also reported.