- Preparation method of 4-aminopyridine compound
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The invention discloses a preparation method of a 4-aminopyridine compound. The preparation method comprises the following steps: adding a 4-amino- 3-chloropyridine compound or a 4-amino-3, 5-dichloropyridine compound, potassium phosphate and a catalyst into a solvent, and reacting at 0-10 MPa and 0-100 DEG C for 4-12 hours. According to the preparation method of the 4-aminopyridine compound, therelated raw materials are easy to obtain or self-make, the cost is low, the preparation method is simple, the reaction efficiency is high, the raw material cost is low, and byproducts have economic value; meanwhile, the reaction involved in the invention has good universality and tolerance to functional groups.
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- Medicament intermediate and preparation method of fluroxypyr 1-methylheptyl ester
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The invention discloses a medicament intermediate and a preparation method of fluroxypyr 1-methylheptyl ester, and relates to the field of organic synthesis. The preparation method of the medicament intermediate has the advantages that a molecular sieve is added, a fluoridation reaction and next amination reaction of pentachloropyridine can be realized through one-pot reaction, complex separation steps are saved, product loss caused by the separation process is avoided, and the key medicament intermediate for preparing herbicide can be prepared at high yield. The preparation method is easy to operate, is low in equipment demand, contributes to lowering production cost, and is suitable for large-scale industrial production. The preparation method is characterized in that low-cost and readily-available pentachloropyridine is taken as an initial raw material, the fluoridation reaction and next amination reaction are implemented by adopting the one-pot method to obtain key medicament intermediate; on the basis of the medicament intermediate, a hydroxylation reaction and a condensation reaction are implemented to obtain efficient high-yield fluroxypyr 1-methylheptyl ester. The preparation method is reasonable in route design, is simple in steps, is convenient to operate, is low in cost, is low in pollution, and is suitable for industrial large-scale production.
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- Three nitrogen heterocycle containing 1, 2, 3 - thiadiazole - 5 - a amidine compounds and synthesis
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The invention discloses an N-trisubstituted-1,2,3-thiadiazole-5-formamidine compound with three aromatic rings of general formula TDCA and a synthesis method of N-trisubstituted-1,2,3-thiadiazole-5-formamidine compound. The target compound of general formula TDCA is obtained by reacting a compound of general formula B and a compound of general formula A, wherein references of X and Y in the general formula A are the same as those in the general formula TDCA.
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Paragraph 0077; 0078
(2017/08/25)
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- Method for preparing fluroxypyr
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The invention discloses a method for preparing fluroxypyr, and belongs to the technical field of fine chemical engineering. The method comprises the steps of carrying out fluorination, carrying out amination, carrying out hydroxylation, carrying out stock solution extraction, carrying out condensation, carrying out hydrolysis and carrying out byproduct conversion. Byproducts and unreacted raw materials in a reaction process are used again through the steps of carrying out stock solution extraction and carrying out byproduct conversion, so that the utilization ratio of the raw materials is increased, the production cost and environmental treatment cost are reduced, and thus the method is applicable to large-scale production.
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- Selective mono-and diamination of polyfluorinated benzenes and pyridines with liquid ammonia
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Amination of pentafluoropyridine, 2,3,5,6-tetrafluoropyridine, 4-chlorotetrafluoropyridine, 3,5-dichlorotrifluoropyridine, octafluorotoluene, α,α,α,2,3,5,6-heptafluorotoluene, decafluoro-m-xylene, decafluorobiphenyl, hexafluorobenzene, and pentafluorobenzene with liquid ammonia was investigated. Bis-aminodefluorination temperatures for the majority of substrates were shown to exceed significantly the corresponding temperatures of monoaminodefluorination. The optimal conditions for selective preparation of mono-and diaminopolyfluoro(het)arenes were elucidated. An efficient method for isolation of particular polyfluorophenylenediamines from product mixtures formed in nonselective reactions of pentafluorobenzene and hexafluorobenzene with aqueous ammonia based on complexation with a crown ether is proposed.
- Vaganova,Kusov,Rodionov,Shundrina,Malykhin
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p. 2239 - 2246
(2008/09/20)
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- Novel nucleosides and related processes, pharmaceutical compositions and methods
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The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and antibacterial applications. Preferred embodiments of the instant invention include novel 2 halogen-substituted, 3 halogen-substituted, and 2′,3′dihalogen-substituted analogues of 3-deazaadenosine, and novel 3 halogen-substituted analogues of 3-deazaguanosine. Compounds of the instant invention, including 4-Amino-6-fluoro-1-(β-D-ribofuranosyl)imidazo[4,5-c]pyridine and 6-Amino-7-bromo-1,5-dihydro-1-β-D-ribofuranosylimidazo[4,5-c]pyridin-4-one, have exhibited potent antiviral and anticancer activity in vitro. The compounds are also useful in the concomitant treatment of bacterial infections associated with viral infections such as AIDS.
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Page/Page column 11; Figure 1
(2010/02/07)
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- Selective hydrodechlorination of fluorinated arylamines
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Chlorine-containing polyfluorinated anilines and meta-phenylenediamines undergo selective hydrodechlorination easily upon reduction by zinc in aqueous ammonia. A new approach is thus provided to synthetically valuable, partially fluorinated arylamines based on utilizing polyfluorochloroarenes, which are available as intermediates of perfluoroarene production from perchloroarenes. When chlorine atoms are present in positions both ortho and para to the amino group, para chlorine is initially eliminated. Based on this reaction, a one-pot synthesis of partially fluorinated 4-aminopyridines from 3,5-dichlorotrifluoro- and 3-chlorotetrafluoropyridine has been realized.
- Selivanova, Galina A.,Gurskaya, Larisa Yu.,Pokrovskii, Leonid M.,Kollegov, Vitaliy F.,Shteingarts, Vitaliy D.
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p. 1829 - 1834
(2007/10/03)
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- Synthesis of halogen-substituted 3-deazaadenosine and 3-deazaguanosine analogues as potential antitumor/antiviral agents
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Various 2-halogen-substituted analogues (38, 39, 43 and 44), 3-halogensubstituted analogues (51 and 52), and 2′,3′ -dihalogen- substituted analogues (57-60) of 3-deazaadenosine and 3-halogen-substituted analogues (61 and 62) of 3-deazaguanosine have been synthesized as potential anticancer and/or antiviral agents. Among these compounds, 3-deaza-3-bromoguanosine (62) showed significant cytotoxicity against L1210, P388, CCRF-CEM and B16F10 cell lines in vitro, producing IC50 values of 3, 7, 9 and 7μM, respectively. Several 3-deazaadenosine analogues (38, 51, 57 and 59) showed moderate to weak activity against hepatitis B virus.
- Liu,Luo,Mozdziesz,Lin,Dutschman,Gullen,Cheng,Sartorelli
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p. 1975 - 2000
(2007/10/03)
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