348-91-4

Upstream product

• 7693-46-1 4-Nitrophenyl chloroformate 
• 320-51-4 4-chloro-3-trifluoromethyl-aniline 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 75-44-5 phosgene 

Downstream Products

• 1129683-83-5 4-[ ({[4-chloro-3-(trifluoromethyl)phenyl]amino}carbonyl)amino]phenol 
• 755037-03-7 regorafenib 
• 284461-73-0 sorafenib 

Relevant academic research and scientific papers

Preparation method of regorafenib

The invention relates to a preparation method of regorafenib. The method comprises the following steps: adding 4-chloro-3-trifluoromethylaniline and an alkaline reagent into an organic solvent of triphosgene, and stirring for reaction to obtain a compound 2; and then adding N-methyl-4-(4-amino-3-fluoro) phenoxy pyridine-2-formamide and an alkaline reagent into the organic solvent of the compound 2, and reacting to obtain the regorafenib. The method provided by the invention is short in reaction time, easy for large-scale preparation, easy to operate, good in stability, high in purity and yield, free of intermediate separation and suitable for industrial production.

"Close-to-Release": Spontaneous Bioorthogonal Uncaging Resulting from Ring-Closing Metathesis

Bioorthogonal uncaging reactions offer versatile tools in chemical biology. In recent years, reactions have been developed to proceed efficiently under physiological conditions. We present herein an uncaging reaction that results from ring-closing metathesis (RCM). A caged molecule, tethered to a diolefinic substrate, is released via spontaneous 1,4-elimination following RCM. Using this strategy, which we term "close-to-release", we show that drugs and fluorescent probes are uncaged with fast rates, including in the presence of mammalian cells or in the periplasm of Escherichia coli. We envision that this tool may find applications in chemical biology, bioengineering and medicine.

Preparation method for medicine for treating tumors and application of medicine

The invention discloses a preparation method for a medicine for treating tumors and an application of the medicine. A structural formula of the medicine for treating the tumors is shown in the description. The preparation method disclosed by the invention greatly simplifies the operation steps, has a short reaction route, a stable reaction system, very good controllability, mild reaction conditions, low costs, and a higher total yield; the obtained product has higher purity; the medicine disclosed by the invention can inhibit growth of tumor cells, facilitate prolonging life span of patients,and improve quality of life of the patients; and the medicine has a very good therapeutic effect on human lung cancers, human melanoma and human fibrosarcoma.

SEMICARBAZIDE DERIVATIVES AS KINASE INHIBITORS

The present invention relates to semicarbazide derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.