- Method for synthesizing nifedipine intermediate by using combined catalyst
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The invention provides a method for synthesizing a nifedipine intermediate by using a combined catalyst, and belongs to the technical field of organic medicine synthesis. The synthesis method of the nifedipine intermediate comprises the following step: un
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Paragraph 0043; 0047; 0053; 0056-0057; 0060
(2020/06/22)
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- Synthesis of Functionalized Quinolines from 4-(o-Nitroaryl)-Substituted 3-Acyl-4,5-Dihydrofurans: Reductive Cyclization and C=C Bond Cleavage
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A new synthetic approach to functionalized quinolines was developed based on the application of Zn–AcOH system as a simple and efficient reductive agent towards 4-(o-nitroaryl)-3-acyl-substituted 4,5-dihydrofurans. Reduction of 3-carbonyl-substituted dihy
- Zaytsev, Sergey V.,Villemson, Elena V.,Ivanov, Konstantin L.,Budynina, Ekaterina M.,Melnikov, Mikhail Ya.
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p. 2814 - 2823
(2017/05/29)
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- Design and synthesis of 4-alkyl-2-amino(acetamino)-6-aryl-1,3-thiazine derivatives as influenza neuraminidase inhibitors
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With a convenient and economical method, two series of 1,3-thiazine derivatives 1 and 2 were synthesized, and their neuraminidase (NA) inhibitory activities were evaluated. The pharmacological results showed that most of the compounds have potent NA inhibitory activity. Especially, 1g exhibited the best activity against influenza virus A (H1N1) NA (IC50 = 29.06 μg/mL), and its crystal structure was determined by single-crystal X-ray diffraction. The preliminary biological assay indicated that 1,3-thiazine could be used as a core structure to design novel influenza NA inhibitors. Two series of novel 1,3-thiazine analogs were synthesized and their neuraminidase (NA) inhibitory activities were evaluated. Most of the compounds have potent NA inhibitory activity. Compound 1g exhibited the best activity against influenza virus A (H1N1) NA with an IC50 of 29.06 μg/mL, and its crystal structure was determined by single-crystal X-ray diffraction.
- Li, Wan,Xia, Lin,Hu, Aixi,Liu, Ailin,Peng, Junmei,Tan, Weiqing
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p. 635 - 644
(2013/09/24)
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- Facile and efficient aromatization of 1,4-dihydropyridines with M(NO 3)2·XH2O, TNCB, TBAP and HMTAI and preparation of deuterium labeled dehydronifedipine from nifedipine-d3
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The easy and efficient aromatization of various 1,4-dihydropyridines was investigated using various metal nitrates, trinitratocerium(IV) bromate (TNCB), and tetrabutyl ammonium periodate (TBAP) as oxidant in acetic acid at 100 °C, as well as hexamethylenetetramine-iodine (HMTAI) reflux in methanol. The efficient conversion of nifedipine-d3 to dehydronifedipine-d 3 as an internal standard can be used in the measurement of nifedipine concentration in a body.
- Shaikh, Ajam C.,Chen, Chinpiao
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supporting information; experimental part
p. 3664 - 3668
(2010/09/04)
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- Electrochemical Behaviour of an Unsymmetrical 4-(o-Nitrophenyl)-1,4-Dihydropyridine in Protic Medium.
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The electrochemical behaviour of 3-cyano-5-methoxycarbonyl-2,6-dimethyl-4(o-nitrophenyl)-1,4-dihydropyridine and the corresponding N-methyl derivative have been investigated in hydroalcoolic medium.The 4 electron reduction leads to an amino-benzonaphtyrid
- David, J. Y.,Hurvois, J. P.,Tallec, A.,Toupet, L.
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p. 3181 - 3196
(2007/10/02)
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- Novel 2-amino-1,4-dihydropyridine calcium antagonists. II. Synthesis and antihypertensive effects of 2-amino-1,4-dihydropyridine derivatives having N,N-dialkylaminoalkoxycarbonyl groups at 3- and/or 5-positions
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Novel 2-amino-1,4-dihydropyridine derivatives I, which contain N,N-dialkylaminoalkoxycarbonyl groups at the 3- and/or 5-position, were synthesized and their antihypertensive effects were evaluated in spontaneously hypertensive rats. Remarkably prolonged duration of antihypertensive action was observed when a tertiary amino group was introduced into either the 3- or 5-ester side-chain of the 1,4-dihydropyridine ring. In particular, the compounds containing cyclic amino moieties at the 3-position showed greater potency than those with acyclic amino moieties. Chemical modification studies indicated that the two ester side-chains of 1,4-dihydropyridine at the 3- and 5-position might function in a different manner in relation to the antihypertensive activities. 3-(1-Benzhydrylazetidin-3-yl) 5-isopropyl 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridine-dicarboxyl ate, I-43 (CS-905), exhibited potent and long-lasting antihypertensive effects with gradual onset of action, and is a promising candidate as an antihypertensive drug.
- Kobayashi,Inoue,Nishino,Fujihara,Oizumi,Kimura
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p. 797 - 817
(2007/10/02)
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- Process for the preparation of 1,4-dihydropyridinedicarboxylic esters
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In the preparation of a 1,4-dihydropyridine of the formula STR1 in which R is a phenyl radical which is optionally substituted once or twice by nitro and/or chlorine, R1 is a C1 -C4 -alkyl radical which is optionally substituted by a C1 -C4 -alkoxy group, and R2 is a C1 -C12 -alkyl radical which is optionally substituted by a C1 -C4 -alkoxy group, a trifluoromethyl group or the radical (C6 H5 CH2) (CH3)N, by preparing an ylidene compound of the formula STR2 and reacting such ylidene compound with an enamine compound of the formula STR3 the improvement which comprises preparing the ylidene compound by reaction of a ketocarboxylic ester of the formula STR4 with an aldehyde of the formula RCHO, in a solvent in the presence of a catalytic amount of any acetate salt of an amine, at a temperature from about -10° C. up to 100° C. The products symmetrical or unsymmetrical, are produced in high yield and purity.
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