- Synthesis method of 3-amino methyl isonicotinate
-
The invention discloses a synthesis method of 3-amino methyl isonicotinate, wherein the synthesis method comprises the steps: by taking 4-trifluoromethyl nicotinic acid as an initial raw material, sequentially carrying out acylation condensation series connection, Hofmann degradation, hydrolysis and esterification reaction to obtain the 3-amino methyl isonicotinate. The synthesis method has the advantages of mild reaction conditions, high yield, low cost, easily available raw materials, and realization of industrial production, the thionyl chloride reaction liquid can be repeatedly used, the utilization rate of the raw materials is improved, the resource waste is reduced, the pollution is reduced, the production cost of the whole process is furthest reduced, and the application value is extremely high.
- -
-
-
- High-yield synthesis method of methyl 3-aminoisonicotinate
-
The invention belongs to the field of chemical pharmacy, and particularly discloses a high-yield synthesis method of methyl 3-aminoisonicotinate. According to the high-yield synthesis method, 4-picolinic acid is used as a raw material and subjected to brominating, ammonifying and esterifying to obtain methyl 3-aminoisonicotinate. The high-yield synthesis method of methyl 3-aminoisonicotinate has the advantages of mild reaction conditions, high total yield, realization of repeated use of a 3-bromo-4-picolinic acid reaction waste filtrate, improvement of the utilization rate of the raw material,reduction of resource waste, maximum reduction of the production cost of the whole process, and extremely high application value.
- -
-
-
- Method for rapidly and efficiently synthesizing 3-aminoisonicotinic acid methyl ester (by machine translation)
-
Of the method for rapidly and efficiently synthesizing 3 - aminoisonicotinic acid methyl ester, through nitration, reduction, to obtain the 3 -aminoisonicotinic acid methyl ester, disclosed by the invention can be repeatedly utilized 3 - to improve the utilization rate, of the raw material and reduce the resource waste, to the maximum reduction . of the whole process . The method comprises the following steps: synthesizing,aminoisonicotinic acid methyl ester in a high, total yield; and reducing resource waste. (by machine translation)
- -
-
-
- Azaindole synthesis through dual activation catalysis with N-heterocyclic carbenes
-
A convergent, transition-metal-free synthesis of 2-aryl-azaindoles has been developed. The interception of a reactive aza-ortho-azaquinone methide intermediate by an acyl anion equivalent generated through carbene catalysis provides high yields, a wide substrate scope, and the synthesis of previously inaccessible azaindoles.
- Sharma, Hayden A.,Todd Hovey,Scheidt, Karl A.
-
supporting information
p. 9283 - 9286
(2016/07/25)
-
- Hofmann-type rearrangement of imides by in situ generation of imide-hypervalent iodines(III) from iodoarenes
-
The Hofmann-type rearrangement of aromatic and aliphatic imides using a hypervalent iodine(III) reagent generated in situ from PhI, m-CPBA, and TsOH·H2O proceeded in the presence of a base in alcohol to provide anthranilic acid derivatives and amino acid derivatives in high yields, respectively. This reaction proceeds through a tandem reaction via alcoholysis followed by a Hofmann rearrangement promoted by the formation of an imide-λ3-iodane intermediate.
- Moriyama, Katsuhiko,Ishida, Kazuma,Togo, Hideo
-
supporting information; experimental part
p. 946 - 949
(2012/05/05)
-
- Synthesis of novel 1,7-naphthyridines by Friedlaender condensation of pyridine substrates
-
The general ability of appropriate pyridyl compounds (aldehyde or ketone) to undergo Friedlaender condensation to give different 1,7-naphthyridines has been demonstrated. 2,4-Disubstituted 1,7-naphthyridine 8 was prepared from 3-amino-4-acetylpyridine (6) and ketone 4 (82%). The Friedlaender self-condensation of pyridyl substrate 6 is reported, as well. The dimer product, 2-(3-aminopyridin-4-yl)-4-methyl-1,7-naphthyridine (7), was obtained in 97% yield. 2-Aryl-and 2,3-diaryl-1,7-naphthyridines (16-18) were prepared from 3-aminoisonicotinaldehyde (13) and arylketones 4, 14, and 15 (28-71%). The key substrates 6 and 13 are readily available via the improved pyridine nitration method. Copyright
- Stockmann, Vegar,Fiksdahl, Anne
-
p. 1383 - 1387
(2012/01/05)
-
- Iminooxazolidine Derivatives and Their Use
-
The present application relates to novel iminooxazolidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.
- -
-
Page/Page column 18
(2010/02/16)
-
- HETEROCYCLIC HYDRAZIDE COMPOUND AND PESTICIDAL USE OF THE SAME
-
A hydrazide compound represented by the formula (I), an N-oxide thereof or suitable salt thereof: has excellent pesticidal activity.
- -
-
-
- BICYCLIC PYRIMIDIN-4-(3H)-ONES AND ANALOGUES AND DERIVATIVES THEREOF WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1)
-
Compounds of formula (I); which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
- -
-
Page/Page column 38
(2010/02/12)
-
- ANTITHROMBOTIC AROMATIC ETHERS
-
This application relates to a compound of formula (I) (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.
- -
-
Page/Page column 70
(2008/06/13)
-
- Aryl tetrahydropyridine inhibitors of farnesyltransferase: Glycine, phenylalanine and histidine derivatives
-
Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered a series of aryl tetrahydropyridines that incorporate substituted glycine, phenylalanine and histidine residues. The design, synthesis, SAR and biological properties of these compounds will be discussed.
- Gwaltney II, Stephen L.,O'Connor, Stephen J.,Nelson, Lissa T. J.,Sullivan, Gerard M.,Imade, Hovis,Wang, Weibo,Hasvold, Lisa,Li, Qun,Cohen, Jerome,Gu, Wen-Zhen,Tahir, Stephen K.,Bauch, Joy,Marsh, Kennan,Ng, Shi-Chung,Frost, David J.,Zhang, Haiying,Muchmore, Steve,Jakob, Clarissa G.,Stoll, Vincent,Hutchins, Charles,Rosenberg, Saul H.,Sham, Hing L.
-
p. 1359 - 1362
(2007/10/03)
-
- Inhibitors of protein isoprenyl transferases
-
The present invention relates to novel compounds of Formula I which are useful in inhibiting protein isoprenyl transferases and the farnesylation or geranylgeranylation of the oncogene protein Ras and other related small g-proteins, and compositions containing such compounds and methods of using such compounds.
- -
-
-
- Preparation of 4-substituted 3-amino-2-chloropyridines, synthesis of a nevirapine analogue
-
A new method for preparing 3-amino-2-chloropyridines with a substituent (methyl, phenyl, carboxamide, methoxycarbonyl, acetyl, benzoyl and cyano) at the 4-position has been developed. An isoquinoline analogue of the reverse transcriptase inhibitor Nevirapine has been synthesized from the 4-amino-3-chloroisoquinoline.
- Bakke,Riha
-
-