37 results about "Nucleophilic aromatic substitution" patented technology

The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.

The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.

A method for forming a polyaryletherketone is described. More particularly, a reaction mixture is initially supplied to the reactor vessel that contains one or more precursor monomers. A heteroaryl compound is also added to the reaction mixture. The reaction can be carried out according to, e.g., an electrophilic aromatic substitution reaction or a nucleophilic aromatic substitution reaction. The heteroaryl compound can serve as a dispersant to the polymer as it is formed. This minimizes the likelihood of gelling of the product polymer within the reactor vessel and limits the impact of process disruptions on the production of the polyaryletherketone.

The disclosure herein provides methods for performing nucleophilic aromatic substitution reactions in ionic liquids and forming polymeric materials.

The invention discloses a method for preparing 2-(2-nitrophenyl) pyrrole and 2,5-bis(2-nitrophenyl) pyrrole compounds. In the method, a compound shown in a general formula V and a compound shown in a general formula VI undergo reaction similar to nucleophilic aromatic substitution reaction under the alkali condition to obtain a compound shown in a general formula VII in a mode of high efficiency and high regioselectivity. The reaction has high regioselectivity; even if an N-H pyrrole compound or a pyrrole compound with an N-H substituent group is used as a substrate, the aromatic substitutionreaction can still be performed at 2-position and 5-position of the pyrrole compound to obtain a C-arylation product in a mode of high regioselectivity; and no N-arylation product is generated. Thus,the characteristic ensures that the reaction can be used in the pyrrole compound which contains activated hydrogen, thereby expanding the application scope of the method.

The invention relates to a method for preparing 4-methylsulfonyltoluene, which comprises the following steps of: reacting anhydrous sodium sulphite and sodium bicarbonate with paratoluensulfonyl chloride to obtain a crude sodium 4-toluenesulfinate product; and mixing sodium 4-toluenesulfinate and a small amount of 4-methylsulfonyltoluene, heating for melting, adding imidazole quaternary ammonium salt ionic liquid serving as a catalyst, introducing chloromethane gas, and ensuring that chloromethane is dissolved in the 4-methylsulfonyltoluene and subjected to synthetic reaction with the sodium 4-toluenesulfinate to obtain the 4-methylsulfonyltoluene. In the method, methylation reaction is nucleophilic substitution, an organic phase is the chloromethane and the product 4-methylsulfonyltoluene, and the sodium 4-toluenesulfinate is taken as a nucleophilic reagent and carried by the ionic liquid serving as the catalyst into the organic phase to be subjected to nucleophilic substitution reaction with the chloromethane. Any other solvent except the product 4-methylsulfonyltoluene is not used, so that side reactions in the reaction are avoided, product yield is over 88 percent, purity is over 97 percent, and organic solvent recovery is reduced.

The invention belongs to the field of medicine, and discloses (1R,4R,7R)-7-amino-2-azabicyclo[2,2,1]heptane derivatives and preparation methods, including: (S1) compound I-1 and I-2 undergoes nucleophilic aromatic substitution reaction to obtain compound A-1; (S2) compound A-1 is deprotected with hydrochloric acid or trifluoroacetic acid to obtain compound A-2; (S3) compound A-2 and organic acid or acid chloride Coupling reaction, or reaction with amine and solid phosgene, or reaction with amine and carbonyldiimidazole to obtain (1R,4R,7R)-7-amino-2-azabicyclo[2,2,1]heptane derivative . The (1R,4R,7R)-7-amino-2-azabicyclo[2,2,1]heptane derivative developed by the present invention can avoid inhibiting JAK2, and selectively inhibit JAK1 or JAK1 / Tyk2, which has The treatment of autoimmune diseases is of great significance.