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.
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.
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.