32933-03-2Relevant academic research and scientific papers
Having a spiro ring substituent of aryl morpholine compound, its preparation and use
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Paragraph 0143-0145, (2017/08/02)
The invention discloses arylmorpholine compounds with spiro substituents. The arylmorpholine compounds are compounds having the following general formula (I), wherein X is N or CH; R1 is hydrogen, hydroxyl, alkoxy, halogen, amino, amido, acylamino, sulfam
AMINO ESTER DERIVATIVES, SALTS THEREOF AND METHODS OF USE
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Paragraph 0368, (2016/08/17)
The present invention provides amino ester compounds, salts, and pharmaceutical formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
Hydroxypurine compound and use thereof
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Paragraph 0099; 0100; 0101; 0102, (2016/10/08)
The invention discloses a hydroxypurine compound and a use of the hydroxypurine compound as a PDE2 or TNFa inhibitor and concretely discloses a compound shown in the formula (I) and its tautomer or pharmaceutically acceptable salt.
Preparation method for efficiently synthesizing Sitafloxacin midbody (7S)-5-azaspiro[2.4] heptanes-7-phenylbutane
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Paragraph 0048; 0049, (2017/02/17)
The invention discloses a preparation method for efficiently synthesizing Sitafloxacin midbody (7S)-5-azaspiro[2.4] heptanes-7-phenylbutane. The method comprises the following steps that a first material shown as the accompanying drawing takes a reaction to obtain a second material shown as the accompanying drawing; the second material takes a reaction to obtain a third material shown as the accompanying drawing; the third material takes a reaction to obtain a fourth material shown as the accompanying drawing; the fourth material takes a reaction to obtain a fifth material shown as the accompanying drawing. The preparation method has the advantages that the single compound with a high ee value can be obtained; the unnecessary waste of materials is avoided; the yield is obviously improved; the operation is simple; the industrial application is easy; the production cost is reduced.
An efficient method for the synthesis of 2′,3′-nonsubstituted cycloalkane-1,3-dione-2-spirocyclopropanes using (2-bromoethyl)-diphenylsulfonium trifluoromethanesulfonate
Nambu, Hisanori,Ono, Naoki,Hirota, Wataru,Fukumoto, Masahiro,Yakura, Takayuki
, p. 1763 - 1768 (2016/12/09)
An efficient and practical synthesis of 2′,3′-nonsubstituted cyclohexane-1,3-dione-2-spirocyclopropanes using a sulfonium salt was achieved. The reaction of 1,3-cyclohexanediones and (2-bromoethyl)diphenylsulfonium trifluoromethanesulfonate with powdered K2CO3 in EtOAc at room temperature (r.t.) provided the corresponding spirocyclopropanes in high yields. The synthetic method was also applied to 1,3-cyclopentanedione, 1,3-cycloheptanedione, 1,3-indanedione, acyclic 1,3-diones, ethyl acetoacetate, and Meldrum's acid.
COMBINATIONS OF HEPATITIS C VIRUS INHIBITORS
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Page/Page column 638, (2015/02/02)
The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
Synthesis of (S)-7-amino-5-azaspiro[2.4]heptane via highly enantioselective hydrogenation of protected ethyl 1-(2-aminoaceto)cyclopropanecarboxylates
Yao, Ying,Fan, Weizheng,Li, Wanfang,Ma, Xin,Zhu, Lvfeng,Xie, Xiaomin,Zhang, Zhaoguo
experimental part, p. 2807 - 2813 (2011/06/19)
Highly effective asymmetric hydrogenation of protected ethyl 1-(2-aminoaceto)cyclopropane carboxylates in the presence of [RuCl(benzene)(S)-SunPhos]Cl was realized, and high enantioselectivities (up to 98.7% ee) were obtained. This asymmetric hydrogenation provides a key intermediate for the enantioselective synthesis of (S)-7-amino-5-azaspiro[2.4] heptane moiety of quinolone antibacterial agents.
Synthesis of enantiomerically enriched α,α-disubstituted β,γ-epoxy esters using hydrolytic kinetic resolution catalyzed by salenCo(III)
Viera, Ignacio,Manta, Eduardo,Gonzalez, Lucia,Mahler, Graciela
experimental part, p. 631 - 635 (2010/08/03)
Novel α,α-disubstituted epoxy esters were prepared in enantiopure form by hydrolytic kinetic resolution (HKR) of the corresponding racemic mixtures using chiral salenCo(III) as catalyst. The methodology provides a convenient route to enantioenriched β,γ-epoxy esters 2a, 2c and 2d.
AMINO ESTER DERIVATIVES, SAILTS THEREOF AND METHODS OF USE
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, (2010/10/03)
The present invention provides amino ester compounds, salts, and pharmaceutical formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
COMPOUNDS AND METHODS OF USE
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Page/Page column 88, (2010/04/30)
The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
