- Synthesis method and applications of polysubstituted 2-aminopyridine derivative
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The invention belongs to the field of organic synthetic chemistry, and relates to a synthetic method and applications of a polysubstituted 2-aminopyridine derivative. According to the method, a 1,2,3-triazine compound and a cyanomethyl compound are used as substrates and are subjected to a one-step cycloaddition reaction under an alkaline condition to obtain a polysubstituted 2-aminopyridine derivative, wherein the reaction does not involve in danger and control reagents and medicines, and a simple, safe, efficient and environment-friendly strategy is provided for synthesizing the polysubstituted 2-aminopyridine derivative. According to the present invention, the obtained product is subjected to further derivatization, such that the active molecule or the drug molecule containing the 2-aminopyridine structure can be synthesized, such as active molecule SC-53606, drug molecule apatinib and nevirapine.
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Paragraph 0051-0053; 0054; 0055
(2020/04/22)
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- Preparation method of 2-hydroxyl-3-trifluoromethylpyridine
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The invention relates to the technical field of chemical synthesis, and particularly discloses a preparation method of 2-hydroxyl-3-trifluoromethylpyridine. According to the preparation method disclosed by the invention, by using the 2-chloro-3-trifluoromethylpyridine as a starting raw material, fluorination is carried out under a certain condition so that 2-fluro-3-trifluoromethylpyridine is prepared; ammonolysis reaction is carried out on the 2-fluro-3-trifluoromethylpyridine so as to prepare 2-amino-3-trifluoromethylpyridine; then diazotization reaction is carried out to obtain the 2-hydroxyl-3-trifluoromethylpyridine. The preparation method disclosed by the invention is reliable in process, raw materials are sufficient and easy to get in the market, the production cost is low, an operation is simple, the yield is high, and scale production is facilitated; at present, a preparation method of the same or other components is never seen at home and abroad.
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- PROCESS FOR THE CATALYTIC DIRECTED CLEAVAGE OF AMIDE-CONTAINING COMPOUNDS
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The present invention relates to a catalytic method for the conversion of amide-containing compouds by means of a build-in directing group and upon the action of a heteronucleophilic compound (in se an amine (RNH2 or RNHR') or an alcohol (ROH) or a thiol (RSH)) in the presence of a metal catalyst to respectively esters, thioesters, carbonates, thiocarbonates and to what is defined as amide-containing compounds (such as carboxamides, urea, carbamates, thiocarbamates). The present invention also relates to these amide-containing compounds having a build-in directing group (DG), as well as the use of such directing groups in the catalytic directed cleavage of N-DG amides with the use of heteronucleophiles (in se an amine (RNH2 or RNHR') or an alcohol (ROH) or thiol (RSH)).
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Page/Page column 51; 53
(2017/04/11)
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- Novel compounds as metabotropic glutamate receptor antagonists
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The present invention relates to compounds of formula (I) wherein A, E G, J, L, M, R1, R2, and R3 are as defined in the specification and claims. The invention also relates to pharmaceutical compositions containing such compounds and methods for preparing the compounds and compositions. The compounds are metabotropic glutamate receptor antagonists and are useful for the treatment of a variety of CNS disorders.
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Page/Page column 18
(2008/06/13)
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- NOVEL SUBSTITUTED IMIDAZOLE DERIVATIVES
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The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1', R2, R2', R3, R3', R4, and R4', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.
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Page/Page column 54
(2010/11/27)
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- Nucleophilic displacement in 2-chloro(trifluoromethyl)pyridines with amines and ammonia
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The activating effect of trifluoromethyl groups in 2-chloro(trifluoromethyl)pyridines was investigated by comparing reactions of these compounds and of 2-chloropyridine with secondary cyclic amines. The ammonolysis of 2-chloro-3-trifluoromethylpyridine and 2-chloro-4-trifluoromethylpyridine is also reported and shown to proceed, in contrast to the reported behaviour of 2-chloro-5-trifluoromethylpyridine, without hydrolysis of the trifluoromethyl function. Both 2-amino-3-trifluoromethylpyridine and 2-amino-4-trifluoromethylpyridine were converted (via the corresponding pyridones) to 3-trifluoromethylpyridin-2(1H)-thione and 4-trifluoromethylpyridin-2(1H)-thione, and a number of S-alkyl derivatives of the latter compounds were prepared.
- Dunn
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p. 153 - 157
(2007/10/03)
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- Synthesis of 1H- and 5H-1,3-diazepines from azido- and tetrazolo-pyridines
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Stable 1H-1,3-diazepines 7-9, 10, 13, 14, 17 and 19 are obtained, often in high yields, by photolysis of trifluoromethyl-substituted azido- or tetrazolo-pyridines in the presence of alcohols or amines; in some cases, 5H-1,3-diazepines are also formed (11, 21 and 23).
- Reisinger, Ales,Wentrup, Curt
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p. 813 - 814
(2007/10/03)
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