422 results about "Picoline" patented technology

Compounds of formula 1 are modulators of P2X3 useful for the treatment of pain and genitourinary, gastrointestinal, and respiratory disorders:whereinR1 is —C(═S)CH3, pyridyl, pyrimidinyl, pyrazinyl, thiazolyl, furyl, furylcarbonyl, acetyl, or carbamoyl; R2a and R2b are independently H, methyl, or ethyl; R3 is H or methyl; Y is a bond, —(CR4R5)n— or —CR4═CR5—; wherein R4 and R5 are each independently H or methyl and n is 1 or 2; X is N or CH; A is phenyl, 5-membered heterocyclyl, or 6-membered heterocyclyl; R6, R7 and R8 are each independently H, halo, lower alkyl, cycloalkyl, alkylthio, alkylthio-lower alkyl, alkylsulfonyl-lower alkyl, di(lower alkyl)amino-lower alkyl, morpholinyl-lower alkyl, 4-methyl-piperazinyl-methyl, trifluoromethyl, pyridyl, tetrazolyl, thiophenyl, phenyl, biphenyl, or benzyl (where thiophenyl, phenyl and benzyl are substituted with 0-3 lower alkyl, halo, sulfonamido, trifluoromethyl, lower alkoxy or lower alkylthio) or R6 and R7 together form a 5-membered or 6-membered carbocyclic or heterocyclic ring substituted with 0-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, oxo, halo, thiophenyl-lower alkyl, phenyl, benzyl (where phenyl and benzyl are substituted with 0-3 lower alkyl, halo, sulfonamido, trifluoro-methyl, lower alkoxy, lower alkylthio, amino-lower alkyl, lower alkylamino-lower alkyl, or di(lower alkyl)amino-lower alkyl); and pharmaceutically acceptable salts thereof; wherein when R1 is pyrimidin-2-yl, X is N, Y is a bond and A is oxazol-5-yl the carbon atom at position 4 in said oxazol-5-yl is not substituted by propyl when the carbon atom at position 2 in said oxazol-5-yl is substituted by substituted phenyl and the carbon atom at position 4 in said oxazol-5-yl is not substituted by phenyl when the carbon atom at position 2 is substituted by unsubstituted or substituted phenyl.

The invention relates to a pharmaceutical composition containing esomeprazole sodium, and a preparation method thereof. Among the active components of the pharmaceutical composition provided by the invention, the amount of 5-(-)-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfonyl]-1H-benzimidazole sodium is lower than 0.3%. The invention also provides a method for producing a target product through a salt forming reaction and recrystallization of esomeprazole. With the controlling over reaction conditions and reaction solvents, advantages such as simple process, low cost, high yield, and suitability for industrialized productions are realized, and the esomeprazole sodium provided by the invention can be obtained. The invention also provides prescriptions and a preparation method of the pharmaceutical composition.

The invention relates to a preparation method of pyridine and 3-picoline by loading ZSM-5 zeolite with metallic oxides selected form cobalt, lead or its mixture as catalyst, reacting the mixture of formaldehyde and acetaldehyde with ammonia in gaseous phase, thus obtaining high yield of pyridine and 3-methyl pyridine.

The invention discloses a preparation method of artificially synthesized (R, S)-nicotine salt. The method comprises: S1, taking 4-methylamino-1-(3-pyridine)-butanone hydrochloride and an alkaline substance, and carrying out a reaction at a temperature of -5-5 DEG C; S2, concentrating a reactant in the step S1, and adding a first refining solvent for refining, so as to obtain 1-methyl-2-(3-pyridine)-2-pyrrolidinol; S3, taking 1-methyl-2-(3-pyridine)-2-pyrrolidinol, adding a reducing agent, and carrying out a reaction at the temperature of 15-35 DEG C; and S4, concentrating the reactant in the step S3, adding a second refining solvent for refining, and then adding acid for reaction to obtain the artificially synthesized (R, S)-nicotine salt. The invention innovatively provides a two-step method for synthesizing the (R, S)-nicotine salt, and the prepared (R, S)-nicotine salt does not contain any other harmful tobacco compounds, has the advantages of simple process and high purity, and is suitable for industrial large-scale production.

The invention discloses a preparation method of an agricultural bactericide. The method includes following steps: carrying out a reaction between 3-isochromanone, which is used for a starting raw material, and an acetol of a formamide compound, performing hydrolysis to obtain 4-([alpha]-hydroxyl)-methylene-2-H-benzopyrane-3-(4H)-one, performing methylation to obtain 4-(methoxylmethylene)-3-isobenzopyrone, preparing (E)-2-(2-halomethyl)-3-methoxylmethyl acrylate from the 4-(methoxylmethylene)-3-isobenzopyrone in methanol, a third inert solvent and a halogenation reagent, and performing a reaction between the (E)-2-(2-halomethyl)-3-methoxylmethyl acrylate and 2-hydroxyl-6-trifluoromethylpyridine or 6-trifluoromethyl-2-pyridine alkoxide to obtain picoxystrobin. The method is short in reaction processes, is mild in conditions, is simple and convenient in post treatment, is less in waste gas, waste water and waste solid, is high in yield and is suitable for industrial production. Appearance of the agricultural bactericide is good and an external standard content of the agricultural bactericide is more than 98%.

The invention discloses a method for synthesizing high-efficiency green agriculture bactericide. The method comprises the following steps: preparing 4-(alpha-hydroxyl) methylene-2-H-benzopyran-3-(4H)-ketone by taking 3-isodihydrocoumarin as an initial raw material, performing methylation to obtain 4-(methoxy-methylene)-3-isobenzopyrone, reacting 4-(methoxy-methylene)-3-isobenzopyrone with a halogenations reagent and methanol to obtain (E)-2-(2-halogen methyl phenyl)-3-methoxy-methyl acrylate, and reacting (E)-2-(2-halogen methyl phenyl)-3-methoxy-methyl acrylate with 2-hydroxyl-6-trifluoromethyl picoline or 6-trifluoromethyl-2-pyridine alcoholate, thereby obtaining picoxystrobin. The method is short in reaction step, gentle in condition, simple, convenient and feasible in aftertreatment, less in waste water, waste gas and waste residue, low in cost, high in yield, applicable to industrialization production and good in product appearance, and the external standard content is greater than 98%.