72784-42-0Relevant academic research and scientific papers
Microwave-Assisted Ruthenium- and Rhodium-Catalyzed Couplings of α-Amino Acid Ester-Derived Phosphinamides with Alkynes
Li, Xue-Hong,Gong, Jun-Fang,Song, Mao-Ping
supporting information, (2021/12/23)
Two different types of new phosphinamide α-amino ester derivatives have been prepared in moderate to high yields via ruthenium(II) and rhodium(III)-catalyzed ortho-C?H functionalization under microwave irradiation. Specifically, the ortho-alkenylated phosphinamides were produced through coupling of phosphinamides containing an α-substituted or α,α-disubstituted α-amino ester with internal alkynes under ruthenium catalysis. In contrast, Ru and the more effective Rh-catalyzed coupling of the α-unsubstituted glycine ester phosphinamide with alkynes resulted in formation of oxidative annulation products, phosphaisoquinolin-1-ones. The developed methods feature the use of easily accessible starting materials, short reaction time, exclusive E-stereoselectivity (for ortho-alkenylation) and good functional group tolerance. The alkenylation reaction was readily scaled up to gram scale. Furthermore, the obtained alkenylated phosphinamide could be transformed into P-containing dipeptides through hydrolysis of the ester group in the catalysis product and subsequent condensation with an α-amino ester.
Carboxamide derivatives, intermediate, preparation method, pharmaceutical composition and application
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Paragraph 0235; 0236; 0237, (2017/08/26)
The invention discloses a formamide derivative, an intermediate, a preparation method, a pharmaceutical composition and an application. The invention provides a formamide derivative shown in a formula 1 as well as pharmaceutically acceptable salt or solvates of the derivative. The formamide derivative disclosed by the invention is an inhibitor of 11 beta-hydroxysteroid dehydrogenase in a type I, can be used for preparing medicines for treating various diseases which are related to expression or activity of 11beta-HSD1, and has a good market development prospect.
INHIBITORS OF HEPATITIS C VIRUS POLYMERASE
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Paragraph 409; 410; 413, (2016/10/11)
The present invention provides, among other things, compounds represented by the general Formula I: (I) and pharmaceutically acceptable salts thereof, wherein L and A (and further substituents) are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
Synthesis of the First Representatives of Spiro-1λ6-isothiazolidine-1,1,4-triones
Dobrydnev, Alexey V.,Popova, Maria V.,Saffon-Merceron, Nathalie,Listunov, Dymytrii,Volovenko, Yulian M.
, p. 2523 - 2528 (2015/09/01)
A strategy for the construction of spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones through the sulfonylation of 1-aminocyclopropane- and 1-aminocyclobutanecarboxylates with methanesulfonyl chloride followed by alkylation with methyl iodide and subsequent cyclization in the presence of potassium tert-butoxide in N,N-dimethylformamide is reported. An efficient synthesis of starting 1-aminocyclopropane- and 1-aminocyclobutanecarboxylic acids was developed. The reaction of spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones with N,N-dimethylformamide dimethyl acetal (DMF-DMA) gives 5′-[(Z)-(dimethylamino)methylene]spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones, the structure of which was confirmed by X-ray diffraction study.
A COMPOUND FOR INHIBITING 11B-HYDROXY STEROID DEHYDROGENASE 1, AND A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 0349-0350, (2014/08/06)
Disclosed are a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the same for inhibiting human 11-β-hydroxy steroid dehydrogenase type 1 (11β-HSD1). The disclosed compound and the pharmaceutical composition including the same for inhibiting human 11-β-hydroxy steroid dehydrogenase type 1 (11β-HSD1) are excellent in activity and solubility, and is more efficient in formulation and transfer.
SUBSTITUTED SULFONAMIDE COMPOUNDS
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Page/Page column 113, (2014/04/17)
The invention is concerned with the compounds of formula (I), and salts thereof, wherein X, Y, Z, R1, R2, R3, R3, R4, R5 and R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of Formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
A COMPOUND FOR INHIBITING 11BETA-HYDROXY STEROID DEHYDROGENASE 1, AND A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 635-637, (2013/03/26)
Disclosed are a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the same for inhibiting human 11-beta-hydroxy steroid dehydrogenase type 1 (11beta-HSD1). The disclosed compound and the pharmaceutical composition including the same for inhibiting human 11-beta-hydroxy steroid dehydrogenase type 1 (11beta-HSD1) are excellent in activity and solubility, and is more efficient in formulation and transfer.
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious γ-secretase inhibitors (Part II)
Ye, Xiaocong M.,Konradi, Andrei W.,Smith, Jenifer,Aubele, Danielle L.,Garofalo, Albert W.,Marugg, Jennifer,Neitzel, Marty L.,Semko, Chris M.,Sham, Hing L.,Sun, Minghua,Truong, Anh P.,Wu, Jing,Zhang, Hongbin,Goldbach, Erich,Sauer, John-Michael,Brigham, Elizabeth F.,Bova, Michael,Basi, Guriqbal S.
scheme or table, p. 3502 - 3506 (2010/08/07)
Significant improvement in metabolic stability on the pyrazolopiperidine scaffold over the original series were achieved and this stability improvement translated in an improved in vivo efficacy.
CYCLYLAMINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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Page/Page column 13, (2009/10/31)
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted cyclylamine derivatives as shown in formulas (1).
NOVEL MICROBIOCIDES
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Page/Page column 29, (2009/12/02)
Compounds of formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.
