40results about How to "Easy and green post-processing" patented technology

The invention discloses a preparation method of an N-(2-pyridyl/pyrimidyl)indole derivative. The preparation method of the N-(2-pyridyl/pyrimidyl)indole derivative comprises the following steps: mixing a 2-substituted phenylaminopyridine/pyrimidine derivative, an alkenyl azide compound, a catalyst, an oxidizing agent, alkali and an organic solvent uniformly, heating to 60 to 80 DEG C under nitrogen or air, performing a cyclization reaction for 18 to 24 hours, cooling to room temperature after the reaction, and performing concentration and column chromatographic purification to obtain the N-(2-pyridyl/pyrimidyl)indole derivative. By the preparation method, the N-(2-pyridyl/pyrimidyl)indole derivative with various substituent groups which cannot be synthesized according to other methods canbe synthesized; furthermore, the used raw materials are easily available, the yield is high, the reaction condition is mild, the reaction time is short, the substrate range is wide, the reaction specificity is high and aftertreatment is simple, convenient and green.

The invention discloses a synthetic method for a 2(1H)-quinoxalinone C-3 site phosphate compound. The synthetic method includes the following steps: (1) dissolving 2(1H)-quinoxalinone derivatives, a phosphatized reagent and potassium persulfate in an organic solvent, and reacting for 7.7-8.3 h at the temperature of 99-102 DEG C in the air conditions; (2) cooling the reaction product obtained in the step (1) to room temperature, and performing separation and purification, so as to obtain the 2(1H)-quinoxalinone C-3 site phosphate compound. According to the synthetic method, raw materials are easy to obtain, the reaction condition is gentle, the addition of an additive, namely a metal catalyst is not needed, and the yield is high (up to 92%); besides, the range of substrates is wide, the reaction specificity is high, and aftertreatment is simple, convenient and green.

The invention discloses a preparation method of a trans-trisubstituted alkene derivative. The preparation method comprises following steps: 1, an alkali, an alkyne, a palladium catalyst, a ligand, a halogenated aromatic hydrocarbon, a precursor compound, and an organic solvent are introduced into a reaction container, nitrogen gas is adopted for repeat filling, and reaction is carried out for 12 to 36h at 60 to 140 DEG C; 2, a product obtained in step 1 is diluted with Ethyl Acetate, is washed with water, and is separated so as to obtain an organic phase; and 3, the organic phase obtained in step 2 is subjected to drying, filtering, concentrating, and column chromatography or thin-layer chromatography processing so as to obtain the trans-trisubstituted alkene derivative. According to the preparation method, construction of one carbon boron bond is realized in construction of the trans-tri aromatic hydrocarbon-substituted alkenes, excellent zone selectivity is achieved, and the trans-trisubstituted alkene derivative which is not easily synthesized using other methods is synthesized.

The invention discloses a preparation method of a cis-N-styryl amide derivative, which comprises the following steps of: (1) mixing an N-phenylethynyl amide derivative, p-methylbenzenesulfonyl hydrazide, alkali and an organic solvent, and reacting at 80-90 DEG C for 12-24 hours; (2) diluting the material obtained in the step (1) with ethyl acetate, washing with water, and separating to obtain an organic phase; and (3) carrying out drying, filtering, concentration and column chromatography or thin-layer chromatography on the organic phase obtained in the step (2) to obtain the cis-N-styryl amide derivative. The prepared cis-N-styryl amide derivative has good chemical selectivity, and when a carbon-carbon triple bond participates in the reaction, a cis-configuration product is preferentially generated in the reduction process.