38923-57-8Relevant articles and documents
Process for the alkylation of active methylene compounds
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Paragraph 0157-0162, (2017/02/24)
The invention discloses an alkylation method of an active methylene compound. The method comprises the following steps: A, adding the active methylene compound to an inorganic alkali-first polar organic solvent mixing system to form a to-be-reacted mixture; B, adding an alkylating agent to the to-be-reacted mixture, filtering after reacting to obtain filtrate, and removing a solvent in the filtrate to obtain the alkylated active methylene compound. According to the method, the inorganic alkali is adopted as a proton abstraction reagent of the active methylene compound, so that the removal effect on alpha-hydrogen in the active methylene compound can be ensured, the alkylation reaction of the active methylene compound can be carried out under a mild condition, and the reaction safety is improved. Meanwhile, the inorganic alkali is low in price, so that the production cost of the alkylation reaction is reduced.
PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES
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Page/Page column 177-178, (2012/10/07)
Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
Titanium silicates as efficient catalyst for alkylation and acylation of silyl enol ethers under liquid-phase conditions
Sasidharan, Manickam,Bhaumik, Asim
experimental part, p. 87 - 93 (2011/10/12)
The activity of titanium- and tin-silicate samples such as TS-1, TS-2, Ti-β and Sn-MFI has been investigated for acylation and alkylation of silyl enol ethers under mild liquid-phase conditions. Silyl enol ethers successfully react with acetyl chloride and tert-butyl chloride under dry conditions in the presence of above catalysts to produce the corresponding acylated and alkylated products, respectively. In the case of acetylation reaction, two different nucleophiles with carbon-center (C-atom) and oxygen-center (O-atom) in silyloxy group of silyl enol ether reacts with acetyl chloride to give 1,3-diketone and ketene-ester, respectively. The selectivity for alkylation is always ca. 100% and no side products are formed. Among the various solvents investigated, anhydrous THF was found to be the suitable solvent for alkylation; whereas dichloromethane exhibited high selectivity for diketones for acylation. The formation of nucleophiles from silyl enol ethers appears to be the key step for successful acetylation and tert-butylation by nucleophilic reaction mechanism. Sn-MFI showed less activity than that observed over the titanosilicates. The observed catalytic activity is explained on the basis of "oxophilic Lewis acidity" of titanium silicate molecular sieves in the absence of H 2O under dry reaction conditions.