- Preparation method of 1-(3-cyanopyridin-2-yl)-2-phenyl-4-methylpiperazine oxalate
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The invention discloses a preparation method of 1-(3-cyanopyridin-2-yl)-2-phenyl-4-methylpiperazine oxalate. The preparation method comprises the following steps: (1) adding 2-chloronicotinonitrile, potassium fluoride and 1-methyl-3-phenylpiperazine into DMSO (dimethylsulfoxide), carrying out nitrogen displacement, and conducting heating for a reaction; (2) pressurizing and distilling the reactionproduct, adding ethyl acetate into the rest residues, and conducting filtering; and (3) adding methanol and oxalic acid into the filtrate, conducting stirring for crystallization, and conducting filtering to obtain the product. DMSO is used as the reaction solvent, and the reaction temperature and the ratio of the raw material usage amount are optimized, so that the reaction time for preparationof 1-(3-cyanopyridin-2-yl)-2-phenyl-4-methylpiperazine is greatly shortened, and the production period is effectively shortened; the yield of 1-(3-cyanopyridin-2-yl)-2-phenyl-4-methylpiperazine is greatly improved and the quality is controllable; and the post-treatment mode of the method is simple, the whole synthesis process is simple to operate, and the cost is low.
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Paragraph 0020; 0023; 0024; 0025; 0026; 0027; 0028-0053
(2019/08/12)
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- Microwave-induced by-products in the synthesis of 2-(4-methyl-2-phenylpiperazinyl)pyridine-3-carbonitrile
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The Letter describes the investigation of an industrial reaction of N-methylphenylpiperazine and chloronicotinonitrile, under microwave heating. Besides the formation of the expected 2-(4-methyl-2-phenylpiperazinyl)pyridine-3-carbonitrile (4), extension o
- Lamazzi, Christelle,Dreau, Armelle,Bufferne, Christel,Flouzat, Christine,Carlier, Patrick,ter Halle, Rob,Besson, Thierry
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scheme or table
p. 4502 - 4505
(2009/11/30)
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- METHOD FOR PRODUCING 2-(4-METHYL-2-PHENYLPIPERAZINE-1-YL)-3-CYANOPIRIDINE
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The present invention provides a process for producing 2-(4-methyl-2-phenylpiperazin-1-yl)-3-cyanopyridine which comprises reacting 1-methyl-3-phenylpiperazine with 2-chloro-3-cyanopyridine in the presence of an organic base and in the absence of alkali metal halide in an polar aprotic organic solvent.
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Page/Page column 4
(2010/11/27)
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- Novel method for the preparation of piperazine and its derivatives
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A novel method for the synthesis of piperazine and its derivatives of formula 1, 1wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; R1 is selected from hydrogen, a methyl group, a phenyl group optionally substituted with an alkyl group having 1 to 6 carbon atoms, or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; and R2 is selected from hydrogen, or a methyl group, or a fluoromethyl group; 2comprising the steps: a. reacting an ester of formula 11 with substituted or unsubstituted ethylenediamine of formula 7 to give 3,4-dehydropiperazine-2-one and its derivatives of formula 12, wherein R, R1, R2 are as defined above and R6 is a C1 to C4 linear or branched alkyl group; and b. reacting the 3,4-dehydro-piperazine-2-one and its derivatives of formula 12 with a reducing agent to yield the piperazine and its derivatives of formula 1.
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- Synthesis of piperazine ring
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A novel process for preparing a compound of the formula I: whereinR1 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy; R2 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy, arylalkoxy, tosyl, formyl, acetyl or amine; and R3 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy is disclosed. These compounds are useful in the synthesis of the antidepressant mirtazapine and other tetracyclic compounds.
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Page column 4
(2008/06/13)
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- Process for preparing piperazine derivatives
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A process for preparing a piperazine derivative represented by the formula (V): comprising reacting 1-methyl-3-phenylpiperazine with 2-chloro-3-cyanopyridine in an aprotic polar organic solvent in the presence of a base and an alkali metal halide. The piperazine derivative and its oxalate are compounds useful as preparation intermediates of mirtazapine.
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- Tetracyclic compounds
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The invention relates to compounds of the general formula I: STR1 or a salt thereof, in which A represents a pyridine ring or a halogen substituted pyridine ring, R1 represents hydrogen, alkyl (1-6 C), alkoxy (1-6 C), alkylthio (1-6 C), halogen, OH, SH or CF3 R2 represents hydrogen or a lower alkyl or aralkyl group and n and m may each be 1, 2 or 3 with the proviso that the sum of m and n must be 2, 3 or 4, having CNS activity, a pronounced antihistamine activity and little or no antiserotonin activity.
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