203056-27-3Relevant articles and documents
Synthesis method of 5-methyl-5-hydroxy-1-azabicyclo[4.4.0] decane-2-one
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Paragraph 0038-0042, (2020/10/04)
The invention discloses a synthetic method of 5-methyl-5-hydroxy-1-azabicyclo[4.4.0]decane-2-one, and belongs to the technical field of organic synthesis. The method comprises the following steps: reacting (S)-1-(tert-butyloxycarbonyl)-2-piperidine carboxylic acid adopted as an initial raw material with N,O-dimethyl hydroxylamine hydrochloride to obtain a carbamoyl piperidine intermediate, then carrying out a Grignard reaction to obtain an acetyl piperidine intermediate, then carrying out a Grignard reaction, Boc protection removal and acylation to obtain a diene ring closed precursor, and finally carrying out an olefin metathesis reaction and a hydrogenation reaction to obtain a target product. Two diastereoisomers in the product are split by the preparative liquid chromatography, and thesequence of removing Boc protecting groups is different, so that the dominant spatial configuration control of the diastereoisomers is realized, and the method provides a powerful technical support for the total synthesis of related natural products.
Compound, preparation method thereof, pharmaceutical composition and application of compound
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Paragraph 0315-0318, (2020/01/03)
The invention discloses a compound, a preparation method thereof, a pharmaceutical composition and application of the compound. The compound I, and a stereoisomer or a pharmacologically acceptable salt thereof can serve as a CDK7 kinase inhibitor, are high in inhibition activity, and can be used for treatment of various malignant tumors.
COMPOUNDS, COMPOSITIONS AND METHODS FOR SYNTHESIS
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Paragraph 00679; 00680; 00681; 00682, (2019/01/10)
The present disclosure, among other things, provides technologies for synthesis, including reagents and methods for stereoselective synthesis. In some embodiments, the present disclosure provides compounds useful as chiral auxiliaries. In some embodiments, the present disclosure provides reagents and methods for oligonucleotide synthesis. In some embodiments, the present disclosure provides reagents and methods for chirally controlled preparation of oligonucleotides. In some embodiments, technologies of the present disclosure are particularly useful for constructing challenging internucleotidic linkages, providing high yields and stereoselectivity.
Pyrazolo[1,5-A]pyrimidines as antiviral agents
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Page/Page column 213, (2016/04/20)
The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
COMPOUNDS AND USE FOR TREATING CANCER
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, (2016/08/17)
The present invention relates to certain 2,4-disubstituted quinoline derivatives, to their therapy, as well as to pharmaceutical compositions comprising said compounds. More specifically the invention relates to certain 2,4-disubstituted quinoline derivatives or pharmaceutical compositions comprising said compounds for the treatment of cancers characterized by overactive Ras and/or Rac or signalling pathway.
Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines
Moas-Héloire, Valeria,Renault, Nicolas,Batalha, Vania,Arias, Angela Rincon,Marchivie, Mathieu,Yous, Said,Deguine, Noémie,Buée, Luc,Chavatte, Philippe,Blum, David,Lopes, Luisa,Melnyk, Patricia,Agouridas, Laurence
, p. 15 - 25 (2015/11/23)
In the aim of identifying new privileged structures, we describe the 5-steps synthesis of cyclic guanidine compounds "tetrahydroisoquinoline-iminoimidazolinesg" derived from tetrahydroisoquinoline-hydantoin core. In order to evaluate this new minimal structure and the impact of replacing a carbonyle by a guanidine moiety, their affinity towards adenosine receptor A2A was evaluated and compared to those of tetrahydroisoquinoline-hydantoin compounds.
PHACETOPERANE FOR THE TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER
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Paragraph 0098, (2015/02/19)
The invention relates to the treatment of an attention deficit hyperactivity disorder (ADHD) with alpha-phenyl(piperidin-2-yl)methanol, or the pharmaceutically acceptable salts and esters thereof, in particular the acetate derivative, more particularly de
COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT
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Paragraph 0417-0420, (2013/10/22)
Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections
PYRAZOLO[1,5-A]PYRIMIDINES AS ANTIVIRAL AGENTS
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Paragraph 0367; 0368; 0369; 0370; 0371; 0372, (2013/07/05)
The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
PYRAZOLO [1, 5 -A] PYRIMIDINES AS ANTIVIRAL AGENTS
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Page/Page column 151-152, (2012/01/14)
The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
