Category: pyridine-derivatives

Gulevskaya, Anna V. published the artcileC-N bond formation by the oxidative alkylamination of azines: comparison of AgPy2MnO4 versus KMnO4 as oxidant, Formula: C9H11N3O3, the main research area is pyridine quinazoline amine oxidative alkylamination permanganate; aminopyridine preparation; aminoquinazoline preparation; permanganate oxidative alkylamination oxidant.

Reports on the successful oxidative alkylamination of azines by the SN-reaction, with the use of alkylamines other than methylamine, are very scarce. Hitherto, the exptl. limitation to extend oxidative amination of azines with NH3/KMnO4 to oxidative alkylamination is solely ascribed to the low solubility of KMnO4 in alkylamines and the increased sensitivity of alkylamines towards oxidation in comparison with ammonia. The exptl. data proved that there is also a substrate dependence in this type of reaction. 2-Alkylamino-5-nitropyridines and 4-alkylaminoquinazolines were smoothly obtained by the treatment of 3-nitropyridine and quinazoline, resp., with alkylamine/AgPy2MnO4. Although KMnO4 still gives moderate to good results with 3-nitropyridine, it is completely useless for reactions with quinazoline with the same alkylamines. The use of AgPy2MnO4 was found to give equal or superior results to those of KMnO4 depending on the alkylamine and the substrate used and therefore seems to be a promising general oxidant for successful oxidative alkylaminations.

European Journal of Organic Chemistry published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Formula: C9H11N3O3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jiang, Ling published the artcileApplication of Enzymatic Promiscuity in Pharmaceutical Synthesis: Papain-catalyzed One-pot Synthesis of 1,4-Dihydropyridine Calcium Channel Antagonists and Derivatives, Computed Properties of 72509-76-3, the main research area is aryl aldehyde acetoacetate aminocrotonate papain catalyst three component reaction; phenyl dihydropyridine dicarboxylate preparation green chem.

A new method for the synthesis of 1,4-dihydropyridine(1,4-DHP) calcium channel antagonists felodipine, nitrendipine and their derivatives via papain-catalyzed three-component reactions of aldehyde, Me acetoacetate and Et 3-aminocrotonate was developed. Operational simplicity, mild reaction conditions and eco-friendliness are the key features of this protocol.

Chemical Research in Chinese Universities published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Computed Properties of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sakai, Hiroki published the artcileSecond basic pKa: An overlooked parameter in predicting phospholipidosis-inducing potential of diamines, Quality Control of 149489-32-7, the main research area is phospholipidosis pos diamine second basic pKa PLIP; Diamine; Phospholipidosis; Second basic pKa.

In this paper, we present the phospholipidosis-inducing potential (PLIP) of forty fragment-sized diamines derived from N-benzyl-4-(methylamino)piperidine and discuss the relationship between their PLIP and the physicochem. properties. Our results demonstrate that the previously reported methods are not suitable for predicting the PLIP of fragment-sized diamines; the second basic pKa can distinguish PLIP-pos. diamines from PLIP-neg. diamines more accurately than ClogP or most basic pKa. To the best of our knowledge, this is the first report describing the relationship between PLIP and second basic pKa.

Bioorganic & Medicinal Chemistry Letters published new progress about Chemical potential (phospholipidosis-inducing potential (PLIP)). 149489-32-7 belongs to class pyridine-derivatives, name is 2-(Chloromethyl)-3-fluoropyridine, and the molecular formula is C6H5ClFN, Quality Control of 149489-32-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yang, Chu-Ting published the artcilePd-Catalyzed Vinylation of Aryl Halides with Inexpensive Organosilicon Reagents Under Mild Conditions, Application In Synthesis of 21190-89-6, the main research area is aryl chloride bromide organosilicon reagent vinylation palladium catalyst; Am/Cm separation; cross-coupling; palladium; silicon; substituent effects.

Pd-catalyzed Hiyama vinylation reaction of non-activated aryl chlorides and bromides under mild conditions was developed. The use of efficient vinyl donors and electron-rich sterically hindered phosphine ligands was critical for the success of the reaction. The products of this transformation can be used for Am/Cm separation, an important challenge in nuclear fuel reprocessing. The substituent effect on Am/Cm separating selectivity was also achieved, which could contribute to the development of new chromatog. materials for the separation of Am and Cm.

Chemistry – A European Journal published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 21190-89-6 belongs to class pyridine-derivatives, name is Ethyl 6-chloropicolinate, and the molecular formula is C8H8ClNO2, Application In Synthesis of 21190-89-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Zhengyong published the artcileUltrasonic extraction and nebulization in real-time coupled with carbon fiber ionization mass spectrometry for rapid screening of the synthetic drugs adulterated into herbal products, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is ultrasonic extraction nebulization direct analysis carbon fiber ionization; screening drug adulterated herbal product; Carbon fiber ionization; Direct analysis; Herbal products; Rapid screening; Synthetic drugs; Ultrasonic extraction and nebulization in real-time.

Ultrasonic extraction and nebulization in real-time/carbon fiber ionization mass spectrometry (UEN/CFI-MS) was developed to screen the synthetic drugs adulterated into herbal products such as antidiabetic drug, antihypertensive drug, and hypolipidemic drug. Recently, ambient ionization MS techniques have achieved great advance for rapid anal. of sample surface. However, direct anal. of the analytes inside samples remains a challenge due to a lack of effective online sample extraction procedures. Owing to disappointing desorption efficiency, analytes inside the sample suffer from low detecting sensitivity when applying ambient ionization MS techniques. In this study, online ultrasonic extraction combined with carbon fiber ionization was used for real-time extraction, nebulization and detection of the analytes inside samples. The ultrasonic atomizer could produce a high-frequency vibration to realize online extraction and nebulization of sample. Then, the produced sample droplets could be immediately ionized by the carbon fiber ionization mass spectrometry. UEN/CFI-MS has shown great compatibility to solvents and compounds with a wide range of polarity and has few limitations for the shape of sample. UEN/CFI-MS was successfully applied for the rapid screening of synthetic drugs adulterated into herbal products. Among 37 batches of herbal products, 1 batch of Chinese patent medicine and 6 batches of dietary supplements were detected to be adulterated with the synthetic chems. without labeling.

Analytica Chimica Acta published new progress about Carbon fibers Role: NUU (Other Use, Unclassified), USES (Uses). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Guo, Xuelei published the artcileNickel-Catalyzed Suzuki-Miyaura Cross-Coupling Facilitated by a Weak Amine Base with Water as a Cosolvent, Quality Control of 321438-86-2, the main research area is nickel catalyst preparation Suzuki coupling reaction amine water cosolvent; aryl chloride Suzuki coupling aryl boronic acid water cosolvent; pharmaceutical substrate nickel catalyzed Suzuki cross coupling.

The development of a Ni-catalyzed Suzuki-Miyaura cross-coupling that uses a weak amine base and performs optimally with H2O as a cosolvent is reported. The aqueous amine base facilitates an equilibrium between the Ni oxidative addition complex and Ni μ-hydroxo dimers, enabling productive catalysis at low metal loadings (typically 1 mol %). A practical catalytic system is enabled using a com. available Ni oxidative addition complex as a precatalyst. The mild conditions allow high functional group tolerance and application to complex pharmaceutical substrates, one of which was demonstrated on a 50 g scale with a catalyst loading of 0.5 mol %.

Organometallics published new progress about Amines Role: RGT (Reagent), RACT (Reactant or Reagent) (weak). 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, Quality Control of 321438-86-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Steib, Andreas K. published the artcileChemoselective Chromium(II)-Catalyzed Cross-Coupling Reactions of Dichlorinated Heteroaromatics with Functionalized Aryl Grignard Reagents, Product Details of C6H5Cl2N, the main research area is dichloropyridine quinoline grignard reagent chemoselective regioselective cross coupling chromium; chromium; cross-coupling; magnesium; nitrogen heterocycles.

Chromium(II) chloride catalyzes the chemoselective cross-coupling reaction of dichloropyridines with a range of functionalized (hetero)aromatic Grignard reagents at room temperature Functional groups, such as esters and acetals, are well tolerated in this transformation. Previously challenging substrates, quinolines and isoquinolines, participate in the selective Cr-catalyzed cross-coupling in cyclopentyl Me ether (CPME) as the solvent. The effective purging of Cr salts is demonstrated by using various solid supports.

Chemistry – A European Journal published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Product Details of C6H5Cl2N.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kuroboshi, Manabu published the artcileElectroreductive generation of recyclable organic reductant from N,N’-dioctyl-4,4′-bipyridinium and Pd-catalyzed reductive coupling of aryl halides, Computed Properties of 36437-30-6, the main research area is electroreductive generation recyclable organic reductant dioctylbipyridinium electroreduction; palladium catalyzed reductive coupling aryl halide electroreductive generation reductant.

Electroreduction of N,N’-dioctyl-4,4′-bipyridinium bis(triflimide) [C8V2+][Tf2N-]2 in THF gave a dark blue solution of the corresponding quinoid C8V0, which worked as an efficient organic reductant for Pd-catalyzed reductive coupling of aryl bromides to give the corresponding biphenyl derivatives in good yields. After usual workup, [C8V2+][Tf2N-]2 was recovered and reused for generation of the organic reductant C8V0.

Synlett published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, Computed Properties of 36437-30-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jiang, Ling published the artcileMechanochemical enzymatic synthesis of 1,4-dihydropyridine calcium antagonists and derivatives, Application In Synthesis of 72509-76-3, the main research area is Lipozyme ball milling dihydropyridine calcium antagonists.

BACKGROUND : Enzyme promiscuity has attracted significant attention from chemists and biochemists in recent years. However, long reaction time and use of toxic organic solvents limit its applications for industrial processes. 1,4-Dihydropyridine (1,4-DHP) calcium antagonists are recommended for the first line treatment of hypertension. Although some chem. protocols for the preparation of 1,4-DHP calcium antagonists have been developed, enzymic synthesis of these compounds still remains uncovered. RESULTS : Solvent-free quick synthesis of 1,4-DHP calcium antagonists felodipine, nitrendipine, nifedipine and nemadipine B and their derivatives was achieved by Lipozyme RM IM (triacylglycerol acylhydrolase, EC3.1.1.3)-catalyzed multicomponent reactions of aromatic aldehyde, alkyl acetoacetate and alkyl 3-aminocrotonate under ball-milling conditions. The products were obtained in moderate yields (up to 86.8%) and the influence of reaction conditions including catalyst loading, grinding auxiliary and grinding frequency was investigated. CONCLUSION : The protocol successfully overcame some longstanding problems in the field of enzymic promiscuity research, such as long reaction time and use of harmful organic solvents, and demonstrated the potential application value of promiscuous enzyme-catalyzed reactions under ball-milling conditions for pharmaceutical synthesis. © 2019 Society of Chem. Industry.

Journal of Chemical Technology and Biotechnology published new progress about Pharmaceutical natural products (1,4-Dihydropyridine calcium). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application In Synthesis of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Youcan published the artcileCopper-catalyzed carbonylative synthesis of pyrrolidine-containing amides from γ,δ-unsaturated aromatic oxime esters, Related Products of pyridine-derivatives, the main research area is pyrrolidine containing amide preparation regioselective copper catalyst; unsaturated aromatic oxime ester amine carbonylative cyclization.

A new method of low-cost copper-catalyzed carbonylative cyclization for preparing pyrrolidine-containing amides I (R = H, R’ = t-Bu, Ph, 2-Py, etc; R1 = Me, Et, Ph, R2 =Me, Allyl, CHC6H5; Ar = Ph, 3-MeC6H4, 2-thiophenenyl, 2-Naph, etc.; R3, R4 = H, Me;) from γ,δ-unsaturated aromatic oxime esters II and amines has been described. A range of readily available amines were examined, including primary, secondary, and heterocycle amines, giving over 60 examples of targeted N-heterocycle substituted amides with broad functional group tolerance, good chem. selectivity and moderate to excellent yields.

Organic Chemistry Frontiers published new progress about Amides Role: SPN (Synthetic Preparation), PREP (Preparation). 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem