- Preparation method of 2-fluoro-5-formyl chloropyridine
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The invention relates to a preparation method of 2-fluoro-5-formyl chloropyridine, and belongs to the technical field of organic chemistry. The method comprises the following steps: 1) taking 2-fluoro-5-methylpyridine as a raw material, and reacting in the presence of potassium permanganate or sodium permanganate to obtain 2-fluoro-5-formic acid pyridine; and 2) carrying out reflux reaction on the2-fluoro-5-formic acid pyridine and thionyl chloride or oxalyl chloride in a chlorinated solvent, after the reaction is finished, carrying out reduced pressure distillation on the solvent, adding analkane solvent, freezing, filtering to obtain a 2-fluoro-5-formyl chloropyridine solution, and carrying out reduced pressure distillation to obtain the 2-fluoro-5-formyl chloropyridine. According to the invention, the method has the advantages that the conversion rate is high, the purity of the obtained product reaches 99.0% or above, the single impurity content is smaller than 0.5%, the production cost is low, and the method is suitable for industrial production.
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Page/Page column 4; 5
(2021/02/13)
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- Nickel-catalyzed carboxylation of aryl iodides with lithium formate through catalytic CO recycling
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A protocol for the Ni-catalyzed carboxylation of aryl iodides with formate has been developed with good functional group compatibility for the synthesis of a variety of aromatic carboxylic acids under mild conditions. The reaction tolerates other functionalities for cross-coupling, such as aryl bromide, aryl chloride, aryl tosylate, and aryl pinacol boronate. The reaction proceeds through a carbonylation process with in situ generated carbon monoxide in the presence of a catalytic amount of acetic anhydride and lithium formate, avoiding the use of gaseous CO. The strategy of CO recycling in catalytic amounts is critical for the success of the reaction.
- Fu, Ming-Chen,Fu, Yao,Shang, Rui,Wu, Ya-Nan
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supporting information
p. 4067 - 4069
(2020/04/20)
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- Green synthesis method of aromatic acid
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The invention discloses a green synthesis method of aromatic acid. Nickel-catalyzed carbonyl insertion is carried out on aryl iodine in the presence of formate, acid anhydride, a phosphine ligand andan organic solvent by using a nickel catalyst to obtain the aromatic acid. Efficient catalytic conversion is realized by utilizing the cheap nickel catalyst, the reaction conditions are mild, and theoperation is simple.
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Paragraph 0048-0122; 0256-0260; 0271-0272
(2020/05/01)
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- IMAGING AND RADIOTHERAPY METHODS FOR TUMOUR STEM CELLS
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The present invention relates to in vivo imaging and radiotherapeutic methods and agents which target the enzyme aldehyde dehydrogenase (ALDH) and that are suitable for the in vivo imaging of tumours and treatment of cancer.
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Page/Page column 28
(2013/04/13)
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- Rapid and efficient synthesis of [18F]fluoronicotinamides, [18F]fluoroisonicotinamides and [18F]fluorobenzamides as potential pet radiopharmaceuticals for melanoma imaging
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In an attempt to simplify nucleophilic radiofluorination reactions to be amenable for automation, a series of [18F]fluoronicotinamides, [ 18F]fluoroisonicotinamides and [18F]fluorobenzamides were synthesized using one-step
- Al Jammaz,Al-Otaibi,Okarvi,Amartey
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scheme or table
p. 312 - 317
(2012/06/04)
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- Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof
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The present invention is directed to substituted nicotinamides and analogs thereof, represented by Formula V: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Ar′ and Ar are independently optionally substituted aryl or optionally substituted heteroaryl, provided that the ring structure of said optionally substituted heteroaryl comprises not more than two nitrogen atoms; and R11 is hydrogen; or alkyl, cycloalkyl, aryl or heteroaryl, each of which is optionally substituted. The present invention also relates to the discovery that compounds having Formula V are activators of caspases and inducers of apoptosis. Therefore, the compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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- Bis-acyloxymethyl derivatives
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This invention relates to new pyridyl, quinoline and acridine bis-acyloxymethyl compounds; to compositions comprising these compounds; and to processes for their utility as fungicides, bactericides and as inhibitors of the growth of cancer in warm-blooded animals. In accordance with this invention, new bis-acyloxymethyl derivatives are provided of the formula: STR1 wherein B is selected from substituted and unsubstituted alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl and alkynyl; A is selected from hydrogen and B; or, A and B together comprise a pyrrolizine; L is selected from STR2 wherein Y is selected from hydrogen or STR3 each R and Z is independently selected from hydrogen or substituted and unsubstituted alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl, alkynyl, amine group, each Z' is independently selected from hydrogen and substituted or unsubstituted alkyl; M is Z or is selected from halogen, nitro, hydroxyl, nitrile and substituted or unsubstituted, carboxylic acid group, carboxylic acid ester group, carboxylic acid amide group, sulfonic acid group and sulfonic acid amide group; ether group, thioether group, acylated hydroxyl, sulfonylamide, sulfonylurea, sulfoxide group, sulfone group and mixtures thereof; each n is the same and is 0 or 1; q is from 0-4; and, X is the anion of an acid.
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- Synthesis, Chemistry, and Antineoplastic Activity of α-Halopyridinium Salts: Potential Pyridone Prodrugs of Acylated Vinylogous Carbinolamine Tumor Inhibitors
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A series of 4- and 5-methyl>-1H-pyrrolizin-5-yl>-2-halopyridinium iodides were synthesized.The rates of hydrolysis of the α-halopyridinium salts to the corresponding pyridones, and the reactivities of the carbamate moieties were studied as a function of pH, buffer composition, and ionic strength.The 4- and 5-pyrrolizinyl-2-halopyridinium iodides and the corresponding pyridones were evaluated against P388 lymphocytic leukemia in vivo.The α-fluoropyridinium compounds were active but the α-chloro compounds were not.This activity was correlated with the rates of hydrolysis of the α-halopyridinium compounds to the active pyridone.Compounds that were active in the P388 screen were evaluated in L1210 leukemia, M5076 carcinoma, and MX-1 mammary xenograft assays in mice.
- Anderson, Wayne K.,Dean, Dennis C.,Endo, Toshiyasu
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p. 1667 - 1675
(2007/10/02)
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