- Preparation process of amantadine nitrate derivative
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The invention discloses a preparation process of an amantadine nitrate derivative, and the amantadine nitrate derivative is prepared from substituted or unsubstituted adamantane as a raw material by the following steps: (1) synthesizing of adamantanol; (2) carboxylation of the adamantanol; (3) amidation of adamantane acid; (4) reduction; (5) hydrolysis of acylamino adamantanol and boc protection of amino; (6) crystallization of Boc-protected amantadine alcohol; (7) nitric acid esterification of Boc-protected amantadine alcohol; (8) refining of a nitric acid esterification product; (9) amino deprotection and salt formation; and (10) refinement of amantadine nitrate. The amantadine amine nitrate derivative is as shown in the specification, wherein R1 and R2 are same or different, and are respectively hydrogen, a linear or branched alkyl group, a substituted or unsubstituted aryl group and a hetero aryl group. The preparation process is efficient, economic, green, safe and reliable and issuitable for industrial production.
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Paragraph 0069-0077
(2019/01/24)
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- Liquid-phase oxidation of alkanes with molecular oxygen catalyzed by high valent iron-based perovskite
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Hexagonal BaFeO3-δ containing high valent iron species acted as an efficient heterogeneous catalyst for the aerobic oxidation of alkanes without the need for additives. The activity of BaFeO3-δ was much higher than that of typical Fe3+/Fe2+-containing iron oxide-based catalysts, and the recovered catalyst could be reused without significant loss of catalytic performance.
- Shibata, Satomi,Sugahara, Kosei,Kamata, Keigo,Hara, Michikazu
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supporting information
p. 6772 - 6775
(2018/06/26)
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- One-pot synthesis of cage alcohols
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An efficient one-pot procedure has been developed for the synthesis of cage alcohols with hydroxy groups in the bridgehead positions. The procedure includes initial nitroxylation with nitric acid or a mixture of nitric acid with acetic acid and subsequent hydrolysis in the presence of urea.
- Klimochkin, Yu. N.,Yudashkin,Zhilkina,Ivleva,Moiseev,Oshis, Ya. F.
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p. 971 - 976
(2017/09/07)
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- Synthesis and biological evaluation of memantine nitrates as a potential treatment for neurodegenerative diseases
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A series of memantine nitrate derivatives, as dual functional compounds with neuroprotective and vasodilatory activity for neurodegenerative diseases, was designed and synthesized. These compounds combined the memantine skeleton and a nitrate moiety, and thus inhibited the N-methyl-d-aspartic acid receptor and released NO in the central nervous system. The biological evaluation results revealed that the new memantine nitrates were effective in protecting neurons against glutamate-induced injury in vitro. Moreover, memantine nitrates dilated aortic rings against phenylephrine-induced contraction. The structure-activity relationships of neuroprotection and vasodilation were both analyzed. In further studies, compound MN-05 significantly protected cortical neurons by inhibiting Ca2+ influx, reducing free radical production and maintaining the mitochondrial membrane potential. Further research on MN-05 is warranted.
- Liu, Zheng,Yang, Si,Jin, Xiaoyong,Zhang, Gaoxiao,Guo, Baojian,Chen, Haiyun,Yu, Pei,Sun, Yewei,Zhang, Zaijun,Wang, Yuqiang
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supporting information
p. 135 - 147
(2017/02/05)
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- Synthesis of hydroxy derivatives from adamantanecarboxylic acids in the system MnO2–H2SO4
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A convenient procedure has been developed for the synthesis of mono- and dihydric cage alcohols from adamantanecarboxylic acids and their esters using the MnO2–H2SO4system. The reaction at elevated temperature involved both decarboxylation and decarbonylation of the initial acid or ester.
- Ivleva,Gavrilova,Klimochkin, Yu. N.
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p. 785 - 790
(2016/07/30)
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- Formation of adamantan-1-ols by the reactions of adamantanes with 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ) in trifluoromethanesulfonic acid
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Adamantanes were treated with DDQ in trifluoromethanesulfonic acid followed by hydrolysis to give adamantan-1-ols in good yields.
- Tanemura,Suzuki,Nishida,Satsumabayashi,Horaguchi
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p. 3230 - 3231
(2007/10/03)
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- Synthese en serie adamantane : preparation d'adamantanes trisubstitues-1,2,3 et -1,2,5 et de protoadamantanones -4 substituees en position -6 ou -8
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A regio and diastereospecific synthetic approach to 1,3-dialkyl (and 1,3-diphenyl) adamantanes bearing a functional group in position-2 (7) and to 1,5-dialkyl (and 1,5-diphenyl) 2-adamantanols (syn 8) is described.This has been accomplished through an addition-isomerisation process on two new classes of 4-protoadamantanones bearing a substituent in position 8 or 6 (3 and 4).These have been prepared via an intramolecular base catalysed cyclisation of iodoketones (11), obtained by thermolysis of hypo-iodites (10).
- Drivas, Ioannis,Mison, Pierre
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p. 252 - 264
(2007/10/02)
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