- A model target anti-tumor medicament and its preparation method and application (by machine translation)
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This invention relates to the targeting of antineoplastic eEF2K of a small molecule inhibitor, its formula (I), formula (II) the structure of the formula (III): Formula (I), formula (II) compound of the formula (III) structure and its pharmaceutically acceptable salt thereof can kill cancer cells, the healthy organism cells are not affected, to various tumor is markedly inhibited, in particular breast cancer, glioma, stomach cancer, liver cancer cells is markedly inhibited. (by machine translation)
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Paragraph 0051-0053
(2016/10/10)
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- A method for preparing optically active 3-amino-1-phenylpropanol derivatives as an intermediate and a method for preparing optically active pharmaceutical products using the same
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The present invention relates to a method for preparing a 3-amino-1-phenylpropanol derivative having (R) or (S) optical activity with 80% or more of an enantiomeric excess (ee), which includes a step of performing an asymmetric reduction reaction in the presence of a spiroborate ester catalyst and a hydrogen donor. The invention also relates to a method for preparing an optically active pharmaceutical product, which includes a step of preparing a (R)- or (S)-3-amino-1-phenylpropanol derivative, that is an intermediate, by using the catalyst.(AA) 3-amino-1-phenylpropanol(BB) Tomoxetine(CC) Nisoxetine(DD) FluoxetineCOPYRIGHT KIPO 2016
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Paragraph 0117-0120
(2016/11/09)
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- ZnCl2-promoted asymmetric hydrogenation of β-secondary-amino ketones catalyzed by a P-chiral rh-bisphosphine complex
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A new catalytic system has been developed for the asymmetric hydrogenation of β-secondary-amino ketones using a highly efficient P-chiral bisphosphine-rhodium complex in combination with ZnCl2 as the activator of the catalyst. The chiral γ-secondary-amino alcohols were obtained in 90-94% yields, 90-99% enantioselectivities, and with high turnover numbers (up to 2000 S/C; S/C = substrate/catalyst ratio). A mechanism for the promoting effect of ZnCl2 on the catalytic system has been proposed on the basis of NMR spectroscopy and HRMS studies. This method was successfully applied to the asymmetric syntheses of three important drugs, (S)-duloxetine, (R)-fluoxetine, and (R)-atomoxetine, in high yields and with excellent enantioselectivities.
- Hu, Qiupeng,Zhang, Zhenfeng,Liu, Yangang,Imamoto, Tsuneo,Zhang, Wanbin
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supporting information
p. 2260 - 2264
(2015/02/19)
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- Practical synthesis of enantiopure γ-amino alcohols by rhodium-catalyzed asymmetric hydrogenation of β-secondary-amino ketones
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(Chemical Equation Presented) Another way to antidepressants: A series of β-secondary-amino ketone hydrochlorides (e.g. 1) were hydrogenated with remarkably high enantioselectivities by using a Rh complex containing P-chiral bisphospholane 2. These results establish a short and practical means for the synthesis of enantiopure N-monosubstituted γ-amino alcohols (e.g. 3), which are key intermediates in the synthesis of important antidepressants. (nbd = norbornadiene; TON = turnover number).
- Liu, Duan,Gao, Wenzhong,Wang, Chunjiang,Zhang, Xumu
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p. 1687 - 1689
(2007/10/03)
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- PROCESS FOR THE PREPARATION OF N-MONOSUBSTITUTED β-AMINO ALCOHOLS
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The invention relates to a process for the synthesis of N-monosubstituted β-amino alcohols of formula (I) and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each being optionally further substituted with alkyl, alkoxy and/or halogen via direct preparation of N-monosubstituted β-amino ketones of formula and its addition salts of proton acids, wherein R1and R2 are as defined above.
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- Synthesis and Reactions of 3,6-Diaryl-3,4-dihydro-1,3,2-oxazaphosphorin-2-oxides
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Aryl β-arylaminoethyl ketones (1), when reacted with phosphorus oxychloride followed by treatment with triethylamine, afford 3,6-diaryl-2-chloro-3,4-dihydro-1,3,2-oxazaphosphorin-2-oxides (3a-u), a hitherto unreported ring system.The oxazaphosphorin (3q), viz. 2-chloro-3-m-anisyl-6-phenyl-3,4-dihydro-1,3,2-oxazaphosphorin, is converted into 7-methoxy-4-phenylquinoline on keeping.This transformation is specific to 3q since other oxazaphosphorins fail to give the quinoline derivative.
- Tilak, B. D.,Gogte, V.N.,Modak, A.S.
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p. 414 - 415
(2007/10/02)
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