651027-03-1

Upstream product

• 651027-02-0 1-triethylsilyl-2,6-difluorobenzene 
• 994-30-9 triethylsilyl chloride 
• 372-18-9 1,3-Difluorobenzene 
• 348-57-2 2,4-difluorobromobenzene 

Downstream Products

• 651027-04-2 (3,5-dibromo-2,6-difluorophenyl)triethylsilane 
• 651027-08-6 3-bromo-4,6-difluoro-5-(triethylsilyl)benzoic acid 
• 651027-10-0 (3-bromo-2,6-difluoro-5-iodophenyl)triethylsilane 
• 1200498-22-1 C₁₆H₂₃BrF₂OSi 
• 1200495-69-7 C₁₈H₁₈F₂N₄OS 
• 1200498-32-3 C₂₃H₂₆F₂N₄O₃S 
• 1200498-28-7 C₁₁H₁₁BrF₂N₂S 
• 1200498-24-3 C₁₀H₉BrF₂O 
• 1200498-30-1 (S)-tert-butyl 4-(5-bromo-2,4-difluorophenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-ylcarbamate 
• 651027-09-7 2-bromo-4,6-difluoro-5-(triethylsilyl)benzoic acid 
• 651027-12-2 2-bromo-3,5-difluoro-4-(triethylsilyl)benzoic acid 
• 651027-11-1 (3-bromo-2,6-difluoro-4-iodophenyl)triethylsilane 
• 651027-07-5 3,5-difluoro-4-(triethylsilyl)benzoic acid 

Relevant academic research and scientific papers

Discovery and Evaluation of Pyrazolo[3,4-d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor

The identification and lead optimization of a series of pyrazolo[3,4-d]pyridazinone derivatives are described as a novel class of potent irreversible BTK inhibitors, resulting in the discovery of compound 8. Compound 8 exhibited high potency against BTK kinase and acceptable PK profile. Furthermore, compound 8 demonstrated significant in vivo efficacy in a mouse-collagen-induced arthritis (CIA) model.

BTK INHIBITOR

Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).

SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ?-SECRETASE-INHIBITING ACTIVITY

The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid β protein, for example,. a compound represented by the formula (I): wherein ruing A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.

Exploring Structural Opportunities: The Regioflexible Substitution of 1,3-Difluorobenzene

To demonstrate the superiority of modern organometallic methods, the inexpensive starting material 1,3-difluorobenzene has been selectively converted into the three benzoic acids and all seven bromobenzoic acids containing the two fluorine atoms in homovicinal positions. The 2,6-difluorobenzoic acid (1) was prepared in a one-pot reaction consisting of direct metallation and carboxylation. The key step on the route to the bromobenzoic acid 4 was a deprotonation-triggered bromine migration from the 2- to the 4-position. All other products were attained through (2,6-difluorophenyl)triethylsilane (11). Consecutive deprotonation of the sites adjacent to the fluorine atoms, followed by appropriate electrophilic substitution, provided not only the acid 7 but also the dibromo and iodobromo derivatives 13 and 23. These in turn gave the isomers 14 and 24 upon base-mediated migration of the heaviest halogen, which made the acids 8 and 10 directly accessible. The regiocontrolled monodebromination of intermediate 14 afforded (4-bromo-2,6-difluoro)triethylsilane (15), which opened the route to the acids 3 and 5 (by carboxylation and protodesilylation) and to acid 9 (by carboxylation and bromodesilylation). Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.