3430-27-1Relevant articles and documents
Preparation method of (S)-4- (C)-3-(S)-bromopyridine (bromopyridine) (by machine translation)
-
Paragraph 0017-0018; 0020-0021; 0023-0024, (2020/02/19)
The method disclosed by the invention has, the beneficial, effects :(1) that 4 - the reaction conditions are mild, the treatment is easy 4 - the method is easy to, operate, the, treatment, is easy . and the method is, easy to, operate 4 - and easy to ;(2) operate 4 - pH, 4 . (by machine translation)
Low-cost simple and convenient preparation method of 3-amino-4-methylpyridine
-
Paragraph 0063-0074, (2019/08/20)
The invention relates to a low-cost simple and convenient preparation method of 3-amino-4-methylpyridine. The method comprises the following steps: performing addition on halogenated crotonaldehyde asa raw material and nitromethane, performing methylenenation condensation, performing aminopyridine cyclization to obtain 4-methyl-3-nitropyridine, and performing reduction to prepare the 3-amino-4-methylpyridine. According to the preparation method provided by the invention, the raw materials used in the method are cheap and easy to obtain, the conditions are mild, the operation is simple, convenient and safe, the reaction selectivity is high, the product yield and purity are high, and the costs are low; and in the process, the atomic economy is high, and three waste (waste water, waste gas and solid waste) is less.
A 4 - methyl -3 - bromo pyridine preparation method
-
Paragraph 0014; 0017; 0018; 0020; 0021; 0023; 0024, (2019/06/05)
The invention belongs to the field of organic synthesis, in particular to a 4 - methyl - 3 - bromo pyridine method, comprises the following steps: (1) to 4 - methyl - 3 - nitro pyridine as raw materials, methanol as solvent, under the effects of catalyst hydrogenation reduction, filtered, the filtrate is concentrated, be 4 - methyl - 3 - aminopyridine; (2) the 4 - methyl - 3 - aminopyridine reacts with acid to form the salt cooling to - 10 °C - 0 °C, [...], [...] sodium nitrite aqueous solution, pH adjusting solution is dropped is alkaline, and then extracted, drying, concentration, a 4 - methyl - 3 - bromo pyridine. The beneficial effect of the invention is: mild reaction conditions, is easy to operate, after treatment is simple, and easy to enlarge production, is extremely suitable for industrial production; good catalytic effect, high yield; low prices of raw materials, the production cost is low.
Copper(ii)-catalyzed c-n coupling of aryl halides and n-nucleophiles promoted by quebrachitol or diethylene glycol
Chen, Guoliang,Chen, Yuanguang,Du, Fangyu,Fu, Yang,Wu, Ying,Zhou, Qifan
supporting information, p. 2161 - 2168 (2019/11/25)
Herein, we report the natural ligand quebrachitol (QCT) as a promoter for a Cu(II) catalyst, which is highly effective for N-Arylation of various amines and related aryl halides. A series of diarylamine derivatives were obtained in high yields by using diethylene glycol (DEG) as both ligand and solvent. The C-N coupling reactions proceed under mild conditions and exhibit good functional group tolerance.
A 3-amino-4-methylpyridine preparation method
-
Paragraph 0019-0020, (2017/04/27)
The invention belongs to the field of organic chemical synthesis and particularly relates to a synthesis method of 3-amino-4-methylpyridine which is an intermediate of an anti-AIDS drug nevirapine. According to the method, 4-methylpyridine-3-boronic acid is used as a raw material, an inorganic amide is used as an ammonia source and obtain3-amino-4-methylpyridine is prepared through one-step reaction in the presence of metal oxide as a catalyst. The preparation method is still simple and provides a new way for novel and efficient synthesis of 3-amino-4-methylpyridine and the disadvantages of long traditional route, low yield and severe reaction conditions are overcome.
Preparation method for nevirapine intermediate
-
Paragraph 0070-0072, (2017/05/27)
The invention relates to a preparation method for an intermediate, i.e., 2-chloro-3-amino-4-methylpyridine, of an anti-AIDs drug nevirapine. The intermediate has a chemical structural formula I as described in the specification. The preparation method is characterized in that 4-methylpyridine is subjected to halogenation, ammonia substitution and chlorination so as to prepare 2-chloro-3-amino-4-methylpyridine. The preparation reactions are as shown in the specifications, wherein X is bromine or chlorine; a halogenation condition is Br2/AlCl3/95-105 DEG C, Br2/AlCl3/MBr/110 to 130 DEG C (wherein M is Li, Na or K), Br2/Fe/135-145 DEG C, Cl2/AlCl3, Br2/FeCl3 or Br2/SnCl4; an ammonia substitution condition is NH3(g)/CuSO4/CH3OH/170-190 DEG C, NH3(aq)/CuSO4/170-190 DEG C, or NaNH2; and a chlorination reaction condition is Cl2/AlCl3 or HCl/H2O2/30-50 DEG C.
Synthesis of some fluorine-containing pyridinealdoximes of potential use for the treatment of organophosphorus nerve-agent poisoning
Timperley, Christopher M.,Banks, R. Eric,Young, Ian M.,Haszeldine, Robert N.
scheme or table, p. 541 - 547 (2011/09/15)
Fluoroheterocyclic aldoximes were screened as therapeutic agents for the treatment of anticholinesterase poisoning. 2-Fluoropyridine-3- and -6-aldoxime, and 3-fluoropyridine-2- and -4-aldoxime, were synthesised. Attempts to obtain 3,5,6-trifluoropyridine-2,4-bis(aldoxime) and -2-aldoxime, however, proved unsuccessful. Pentafluorobenzaldoxime was prepared by oximation of pentafluorobenzaldehyde. Acid dissociation constants (pKa) and second-order rate constants (kox-) of the fluorinated pyridinealdoximes towards sarin were measured. 2,3,5,6-Tetrafluoropyridine-4- aldoxime had the best profile: its kox- approached that of the therapeutic oxime P2S (310 vs. 120 l mol-1 min-1), but its higher pKa (9.1 vs. 7.8) fell short of the target figure of 8 required for reactivation of inhibited acetylcholinesterase in vivo. N-alkylation of the fluorinated pyridine-aldoximes may reduce their pK a nearer to 8 and enhance their therapeutic potential. Crown Copyright
Rapid reduction of heteroaromatic nitro groups using catalytic transfer hydrogenation with microwave heating
Quinn, John F.,Bryant, Cole E.,Golden, Kathryn C.,Gregg, Brian T.
experimental part, p. 786 - 789 (2010/03/24)
A method for the rapid, safe reduction of heteroaromatic and aromatic nitro groups to amines is described using catalytic transfer hydrogenation under microwave heating conditions. Commonly available Pd/C or Pt/C catalyst is extremely effective with 1,4-cyclohexadiene as the hydrogen transfer source. In the case of substrates containing potentially labile aromatic halogens, Pt/C is effective and results in little or no dehalogenation. In general, the reactions are complete within 5 min at 120 °C.
Reduction of 2-amino-3- and -5-nitropyridine derivatives with hydrazine hydrate
Smolyar,Yutilov
experimental part, p. 115 - 118 (2009/07/19)
The reactions of 2-amino-3-nitropyridine and 2-amino-5-nitropyridine with hydrazine hydrate resulted in elimination of the amino group and reduction of the nitro group with formation of 3-aminopyridine. A probable reaction mechanism involves addition of hydrazine hydrate at the N-C2 bond, followed by elimination of ammonia and reduction of the nitro group to amino. 2-Amino-4-methyl-3-nitropyridine and 2-amino-5-methyl-3-nitropyridine reacted with hydrazine hydrate in a similar way.
Heterocyclic substituted aminoazacycles useful as central nervous system agents
-
Page 42, (2010/02/07)
Heterocyclic substituted aminoazacyclic compounds of the formula (I):Z-R3, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
