- Preparation method of Nicodil
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The invention discloses a preparation method of Nicorandil, the preparation method comprises the following steps: directly synthesizing N-(2-ethoxyl) nicotinamide by taking nicotinamide as an initial raw material through a transamidation method, and nitrifying by using a mixture of non-fuming nitric acid, acetic anhydride and concentrated sulfuric acid to obtain Nicorandil. The method simplifies the existing synthesis process, is easy and convenient to operate and is more suitable for large-scale production; meanwhile, the yield of products obtained in each step of reaction is increased, the types and the dosage of reaction reagents are greatly reduced, and the production cost is lower. The technical problems of more reaction steps, high reagent consumption, low production efficiency, serious environmental pollution, poor quality of the prepared product and low yield of the existing preparation process are solved.
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Paragraph 0045; 0067; 0068; 0069; 0070
(2021/10/16)
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- Nicorandil preparation method
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The invention discloses a nicorandil preparation method, which comprises the following steps: synthesis of 3-pyridyloxazolidine: under stirring, adding aminoethanol and a solid bromination reagent into an alcoholic solution of 3-pyridylaldehyde, stirring at room temperature until the 3-pyridylaldehyde is completely consumed, quenching the reaction system with a saturated sodium thiosulfate solution, extracting with ethyl acetate, and concentrating the organic phase to obtain a crude product 3-pyridyloxazolidine; and synthesis of nicorandil: dissolving the 3-pyridyloxazolidine in a solvent, adding nitrite, heating, introducing an oxygen-containing gas, stirring until the 3-pyridyloxazolidine is completely consumed, quenching with a saturated sodium sulfate solution, extracting with ethyl acetate, concentrating, adding the crude product into a 30% ethyl acetate n-hexane solution until dissloving, cooling to 10 DEG C, precipitating a solid, and filtering to obtain the nicorandil.
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Paragraph 0043; 0044
(2020/04/06)
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- Practical catalytic nitration directly with commercial nitric acid for the preparation of aliphatic nitroesters
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To pursue a sustainable and efficient approach for aliphatic nitroester preparation from alcohol, europium-triflate-catalyzed nitration, which directly uses commercial nitric acid, has been successfully developed. Gram scalability with operational ease showed its practicability.
- An, Jichao,He, Pan,Li, Wenhao,Liu, Peipei,Si, Mengyuan,Yang, Bo,Yang, Guanyu
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supporting information
p. 6612 - 6616
(2020/09/21)
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- Preparation method of nicorandil
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The invention discloses a preparation method of nicorandil. According to the method, N-(2-hydroxyethyl)niacinamide is used as a raw material and is subjected to nitrifying under the actions of dilutenitric acid, propionic acid and propionic anhydride to obtain nicorandil. The method has the advantages of mild conditions, simple operation, stable process, cheap and easily available raw materials,high product yield, easy treatment of three wastes, small environmental pollution, and suitability for industrial large-scale production.
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Paragraph 0056-0059
(2020/03/09)
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- Highly efficient synthesis of β-nitrate ester carboxamides through the ring-opening of 2-oxazolines
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A novel method for the synthesis of β-nitrate ester carboxamides using non-corrosive tert-butyl nitrite (TBN) as the nitro source and easily available oxygen as the oxidant has been developed. Variously substituted 2-oxazolines were efficiently ring-opened to deliver the corresponding products in excellent yields. Notably, this reaction provides fast access to pharmaceuticals such as nicorandil.
- Qiao, Kai,Yuan, Xin,Wan, Li,Zheng, Ming-Wei,Zhang, Dong,Fan, Bing-Bing,Di, Zhe-Chen,Fang, Zheng,Guo, Kai
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p. 5789 - 5793
(2017/12/26)
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- Synthesis, antinociceptive activity and pharmacokinetic profiles of nicorandil and its isomers
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Nicorandil (N-(2-hydroxyethyl)nicotinamide nitrate) is an antianginal drug, which activates guanylyl cyclase and opens the ATP-dependent K+ channels, actions that have been suggested to mediate its vasodilator activity. We synthesized nicorandil and its two isomers, which vary in the positions of the side chain containing the nitric oxide (NO) donor, and also their corresponding denitrated metabolites. The activities of these compounds were evaluated in an experimental model of pain in mice. Pharmacokinetic parameters of nicorandil and its isomers, as well as the plasma concentrations of the corresponding denitrated metabolites and also nicotinamide and nitrite were determined. Nicorandil exhibited the highest antinociceptive activity, while the ortho-isomer was the least active. Nicorandil and para-nicorandil, which induced higher plasma concentrations of nitrite, exhibited higher antinociceptive activity, which suggests that the release of NO may mediate this activity.
- Cesar, Isabela C.,Godin, Adriana M.,Araujo, Debora P.,Oliveira, Francinely C.,Menezes, Raquel R.,Santos, Julliana R.A.,Almeida, Mariana O.,Dutra, Marcela M.G.B.,Santos, Daniel A.,MacHado, Renes R.,Pianetti, Gerson A.,Coelho, Marcio M.,De Fatima, Angelo
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p. 2783 - 2790
(2014/05/06)
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- Electronic device
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PROBLEM TO BE SOLVED: To avoid breakage and display failure of a display panel when strong pressure is applied to an exterior member by releasing the charge adhering to the display panel to the ground level. SOLUTION: This electronic device includes the display panel 6 arranged between a conductive chassis 10 and exterior members 1 and 2, frames 5 and 8 that are made of conductive material and hold the display panel 6, and a reinforcement member 9 that is arranged along the outer periphery of the frames and abuts on the exterior member on the exterior member side of the display panel and frames. The frames have an extending section 8a gripped between the chassis and the reinforcement member. The chassis has a projection 10b, and the reinforcement member and the projection have engaging mechanisms 9a and 10a. The reinforcement member is arranged along the outer periphery of the frames in an elastically deformed state, and holds the engagement of the engaging mechanisms with a force caused by the elastic deformation. An elastic member 4 for pressing the frames onto the chassis is arranged between the exterior member and the frames. COPYRIGHT: (C)2010,JPOandINPIT
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- PROCESS FOR THE MANUFACTURE OF NICORANDIL
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Disclosed is a process for the synthesis of Nicorandil (1), 2-(nicotinamide)ethyl nitrate, starting from N-(2-hydroxyethyl)nicotinamide (15), using nitration with nitric acid in the presence of acetic anhydride Said synthesis method is particularly advantageous because it solves the safety problems involved in the use of nitric acid as nitrating agent, and allows a product with excellent yields and quality to be isolated.
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Page/Page column 9-10
(2012/07/14)
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- N'-NITROXYALKYLNICOTINAMIDES FOR THE TREATMENT OF CARDIOVASCULAR DISEASES
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The invention relates to the novel N′-nitroxyalkylnicotinamide derivatives represented by the general formula I wherein R1 is C1-C4 alkyl; R2 is hydrogen. C1-C4 alkyl, CH2OH or CH2ONO2; R3 is ONO2, CH2ONO2 or OH; provided that when R3 is OH, R2 is CH2ONO2; and X? is an organic or inorganic anion; as well as pharmaceutical compositions thereof and their use as a medicament, in particular, in the treatment of diseases of the cardiovascular system.
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Page/Page column 4
(2011/04/24)
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- N'-NITROXYALKYLNICOTINAMIDES FOR THE TREATMENT OF CARDIOVASCULAR DISEASES
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The invention relates to the novel N'-nitroxyalkylnicotinamide derivatives represented by the general formula (I) wherein R1 is C1C4 alkyl; R2 is hydrogen, C1-C4 alkyl, CH2OH or CH2ONO2; R3 is ONO2, CH2ONO2 or OH; provided that when R3 is OH, R2 is CH2ONO2; and X- is an organic or inorganic anion; as well as pharmaceutical compositions thereof and their use as a medicament, in particular, in the treatment of diseases of the cardiovascular system.
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Page/Page column 11-12
(2010/04/03)
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- Use of a combination of active substances containing bioquinones for the production of cosmetic or dermatological preparations
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The invention relates to the use of a compound or several compounds from the group of bioquinones a) in combination with a compound or several compounds from the group of potassium channel openers and/or b) in combination with a compound or several compounds from the group of 5-alpha-reductase inhibitors, for the production of cosmetic or dermatological preparations for treatment of the scalp and for hair in order to prolong the anagenic phase and/or for the treatment and prophylaxis of seborrhoeic symptoms, optionally by additionally using one or several compounds from the group formed from carnitine, arginine, succinic acid, folic acid, conjugated fatty acids and respectively the derivatives thereof, in addition to antioxidants.
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