81879-64-3Relevant academic research and scientific papers
Preparation method of levo-demethyl benzene ring nonyl ester hydrochloride
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Paragraph 0067; 0072; 0073, (2020/09/09)
The invention belongs to the technical field of medicine preparation, and discloses a preparation method of levo-demethylated benzene ring nonyl ester hydrochloride, the molecular formula of the levo-demethylated benzene ring nonyl ester hydrochloride is shown as (1), the method comprises the following steps: (1) preparing (R)-alpha-phenyl-alpha-cyclopentyl-alpha-methyl glycolate; (2) preparing anintermediate, wherein the intermediate is N-benzyl-3-azabicyclo-[3.3. 1]-non-9 [alpha]-alcohol; and (3) carrying out transesterification on the (R)-alpha-phenyl-alpha-cyclopentyl-alpha-methyl glycolate and N-benzyl-3-azabicyclo-[3.3. 1]-non-9 alpha-ol, removing benzyl on N through catalytic hydrogenation to obtain a crude product of L-demethyl benzene ring nonyl ester, salifying, and recrystallizing to obtain the L-hydrochloric acid demethyl benzene ring nonyl ester. The method is environmentally friendly and suitable for large-scale production.
Preparation method of demethyl levophencynonate hydrochloride
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Paragraph 0014, (2019/06/08)
The invention belongs to the field of preparation of chemical intermediates, and specifically relates to a preparation method of demethyl levophencynonate hydrochloride. The preparation method is characterized in that benzylamine as a raw material is prepared into N,N-diethoxy methyl benzylamine; the N,N-diethoxy methyl benzylamine reacts with cyclohexanone and is selectively reduced, and reacts with (R)-alpha-phenyl-alpha-cyclopentyl-alpha-methyl glycolate; and a target product, namely the demethyl levophencynonate hydrochloride, is obtained through hydrogenation and salifying. The yield is improved; the cost is reduced; and operation is simple.
5,6-Membered CNN palladium pincer complexes of 3-benzyl-8-dimethylamino -3-azabicyclo[3.2.1]octane and 3-benzyl-9-dimethylamino-3-azabicyclo[3.3.1]nonane
Bulygina, Ludmila A.,Khrushcheva, Natalya S.,Lyssenko, Konstantin A.,Peregudov, Aleksander S.
, p. 64 - 70 (2019/03/14)
The unsymmetrical CNN pincer ligand precursors 4 and 7b based on the structures of bicyclo[3.2.l]octane and bicyclo[3.3.l]nonane have been synthesized. The corresponding palladium pincer 5,6-membered complexes 5 and 9 were prepared by direct cyclopalladat
THERAPEUTICALLY ACTIVE BICYCLIC-SULPHONAMIDES AND PHARMACEUTICAL COMPOSITIONS
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Paragraph 0104, (2019/05/18)
Pharmaceutical compounds have a bicyclic-sulphonamide structure and pharmaceutical compositions including the compounds may be used in therapy as brain-cell-death protectants and may be used, for example, in the treatment of chronic neurodegenerative diseases. The compounds are active as inhibitors of N-acylethanolamine-hydrolysing acid amidase (NAAA) and may be used for the therapeutic treatment and prevention of pain and inflammatory disorders and other disorders which benefit from the modulation of fatty acid ethanolamides, particularly palmitoylethanolamide (PEA).
FXR RECEPTOR MODULATOR, PREPARATION METHOD THEREFOR, AND USES THEREOF
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Paragraph 0165; 0166, (2018/11/27)
The present disclosure disclosed a modulator of FXR receptor and preparation and use thereof, which relates to the technical filed of medicinal chemistry. The present disclosure provides a modulator of FXR receptor having a structural formula I or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, which can combine with FXR receptor (that is NR1H4) and be acted as a FXR agonist or a partial agonist for preventing and treating the disease mediated by FXR, such as chronic intrahepatic or extrahepatic cholestasis, hepatic fibrosis caused by chronic cholestasis or acute intrahepatic cholestasis, chronic hepatitis B, gallstone, hepatic carcinoma, colon cancer or intestinal inflammatory disease, etc. Specifically, for some chemical compounds, their EC50 for FXR agonist activity reach below 100nM, which show an excellent FXR agonist activity and an excellent prospect to provide a new pharmaceutical selection in clinical treatment for the disease mediated by FXR.
Cyclopalladate complex of 3-benzyl-7-methyl-3,7-diazabicyclo[3.3.1]nonane
Bulygina,Khrushcheva,Peregudov,Sokolov
, p. 2479 - 2484 (2017/05/09)
A new (C,N,N)-pincer cyclopalladate unsymmetrical complex of 3-benzyl-7-methyl-3,7-diazabicyclo[3.3.1]nonane (3-benzyl-7-methylbispidine) was synthesized and characterized. Catalytic performance of this complex was examined in the Heck and Suzuki reactions and in the norbornene hydroarylation.
An approach to azabicyclo[ n.3.1]alkanes by double mannich reaction
Mityuk, Andrey P.,Denisenko, Aleksandr V.,Dacenko, Oleksandr P.,Grygorenko, Oleksandr O.,Mykhailiuk, Pavel K.,Volochnyuk, Dmitriy M.,Shishkin, Oleg V.,Tolmachev, Andrey A.
experimental part, p. 493 - 497 (2010/04/26)
Chlorotrimethylsilane-promoted double Mannich annulation of ketones using N,N-bis(methoxymethyl)benzylamine has been explored. It has been shown that the structure of the substrate drastically influenced the outcome of the reaction. The method allows azabicyclo[n.3.1]alkane derivatives (n=2-5) to be obtained in good yields. Georg Thieme Verlag Stuttgart New York.
Dihydropyridine derivatives as bradykinin antagonist
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, (2008/06/13)
Compound of formula (1) and their pharmaceutically acceptable salts wherein A1,A2,R1, R2,R3,R4,X are as defined in the specification have excellent bradykinin antagonistic activity. STR1
QUINUCLIDINE DERIVATIVES
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, (2008/06/13)
Quinuclidine derivatives of the formula STR1 and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R 1, R. sup.2 and R 3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.
