54089-04-2Relevant academic research and scientific papers
Radiation-induced Alkylation, Hydroxyalkylation, and Reduction of Pyridinecarboxamides in Acidic Alcoholic Solutions
Sugimori, Akira,Nishijima, Masayuki,Itoh, Hiroshi
, p. 3055 - 3056 (1982)
The γ-irradiation of pyridinecarboxamides in acidic methanol or ethanol brings about substitution of the ring hydrogen by alkyl or hydroxyalkyl groups derived from the solvent alcohols in relatively high G-values.In 2-propanol, little alkylation and hydroxyalkylation occur and reduction of CONH2 to CH2OH occurs in low G-values.
Transition-metal-free synthesis of primary to tertiary carboxamides: A quick access to prodrug-pyrazinecarboxamide
Mete, Trimbak B.,Singh, Ankit,Bhat, Ramakrishna G.
supporting information, p. 4709 - 4712 (2017/11/21)
One-pot expedient and direct carbamoylation of heterocyclics is described. The transformation is realized via direct dehydrogenative aminocarbonylation of heterocyclic compounds under transition-metal-free conditions. This method is regioselective and the protocol is proved to be scalable on a gram scale. Further, the therapeutically useful antitubercular agent pyrazinecarboxamide is successfully synthesized by employing this protocol.
Acid-Free Silver-Catalyzed Cross-Dehydrogenative Carbamoylation of Pyridines with Formamides
Han, Wei,Jin, Fengli,Zhao, Qian,Du, Hongyan,Yao, Lifang
supporting information, p. 1854 - 1859 (2016/07/16)
Primary pyridylcarboxamides are prevalent parent structures in bioactive molecules and have the apparent advantages over N-protected derivatives as synthetic building blocks. However, no practical methods have been developed for direct synthesis of this compound class from unfunctionalized pyridines. We herein present a general, safe, concise, acid-free, and highly selective method for the C2-carbamoylation of pyridines with unprotected formamide and N-methyl formamide through the cleavage of two C-H bonds.
Method for synthesizing pyridine primary amides by direct catalytic oxidation process
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Paragraph 0032; 0033; 0034, (2016/10/17)
The invention discloses a method for synthesizing pyridine primary amides by a direct catalytic oxidation process. The method comprises the following steps: under the action of acid or alkali, adding an accelerator water and an oxidizer into formamide which is used as a carbonyl source and nitrogen source, and catalytically oxidizing double C-H bonds of pyridine or derivatives thereof under the action of a silver and/or iron catalyst to directly prepare the pyridine primary amides. By activating the double C-H bonds, the method disclosed by the invention has the advantages of ideal atomic economy, less generated waste, wide and stable substrate sources, and low price. Under the optimized reaction conditions, the separation yield of the target products is up to 98%.
Synthesis of primary amides by aminocarbonylation of aryl/hetero halides using non-gaseous NH3 and CO sources
Suresh,Baburajan, Poongavanam,Ahmed, Mansur
supporting information, p. 4864 - 4867 (2015/07/28)
Abstract A practically simple method for the synthesis of primary amides via the palladium-catalysed aminocarbonylation of aromatic halides by using solid sources of gaseous ammonia and carbon monoxide is described. The system tolerated a wide variety of hindered and functionalized aryl/hetero halides and afforded good to excellent yields (69-94%) of the amide. Pharmacologically active Exalamide and Pyrazinecarboxamide were synthesised in high yields to demonstrate the effectiveness of this method.
Oxidative ammonolysis of 2,4,6-collidine at vanadium-titanium oxide catalyst
Kagarlitsky,Krichevsky
, p. 315 - 317 (2007/10/03)
4-Cyanopyridine was synthesized from the readily obtainable 2,4,6-collidine by oxidative ammonolysis in the presence of vanadium-titanium oxide catalyst. Conditions under which the yield of the product amounted to 73% on the amount of the trimethylpyridin
Photochemical Alkylation, Hydroxyalkylation, and Alkoxylation of Pyridinecarboxamides in Alcohol
Sugimori, Akira,Itoh, Hiroshi,Kanai, Mitsuharu,Itoh, Nobuko,Sugiyama, Toru
, p. 2837 - 2846 (2007/10/02)
The UV-irradiation of 2- and 4-pyridinecarboxamides in alcohol brings about alkylation and/or hydroxyalkylation in the pyridine ring.In the irradiation of 3-pyridinecarboxamide in the presence of sulfuric acid, ionic reaction (alkoxylation at the 2- and 6-position) and radical reaction (alkylation at the 4- and 6-position) occur in parallel.The effects of quenchers indicate that two alkylation products originate from one excited triplet state which is quenched by energy-transfer mechanism and that two alkoxylation products originate from the excited singlet state.
11a-Methano-TXA compounds
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, (2008/06/13)
The present invention provides novel 11a-methano-TXA compounds and intermediates and processs for their preparation. Further provided are methods for using these novel TXA analogs as inhibitors of thromboxane synthetase, rendering these analogs useful for a variety of pharmacological purposes. These pharmacological uses include anti-inflammatory, anti-thromobitc, and anti-asthma indications.
