- Synthesis of 1, 1′, 2, 2′, 3, 3′, 4, 4′ - Octadeutero-Sulforaphane
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Sulforaphane (SFN), a naturally occurring isothiocyanate present in broccoli, shows strong evidence of anti-carcinogenic activity. The mechanism of action, absorption, distribution, metabolism and excretion of the compound is however still poorly understood and requires a stable isotope labelled version of the compound for further studies. The paper describes an optimized synthesis of octadeutero-SFN.
- Kuhnert, Nikolai,Lu, Ye
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- Synthetic method of lomitapide-D8
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The invention provides a synthetic method of lomitapide-D8. The method comprises the following steps: 1) performing a halogenation reaction on a compound 2a and hydrobromic acid to obtain a compound 2; 2) carrying out a hydrogen abstraction reaction on a compound 1 and n-butyllithium, and then adding the compound 2 to carry out a substitution reaction to prepare a compound 3; 3) performing a condensation reaction on the compound 3 and a compound 4 to obtain a compound 5; 4) performing a condensation reaction on a compound 6 and a compound 7 to obtain a compound 8; 5) removing tert-butyloxycarbonyl protection from the compound 8 by utilizing trifluoroacetic acid to obtain a compound 9; and 6) subjecting the compound 5 and the compound 9 to a substitution reaction to obtain the lomitapide-D8. Through the method, deuterated tetrahydrofuran with relatively low price is used as a raw material to synthesize the deuterated 1,4-dibromobutane-D8 for the first time, the deuterated lomitapide-D8is successfully synthesized, and a conventional synthesis route is changed, so that deuterated atoms which are difficult to obtain reach the maximum atom economic effect.
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Paragraph 0013
(2020/06/09)
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- Diphenylamino pyrimidine compound for inhibiting kinase activity
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The invention provides a diphenylamino pyrimidine compound for inhibiting the kinase activity, and particularly provides a medicinal composition of a substituted diphenylamino pyrimidine compound andapplication thereof. The compound is a compound as shown in a formula (I) in the specification, or pharmaceutically acceptable salt, prodrug, hydrate thereof or solvent compound, crystal form, N-oxideand various diastereomers thereof. The compound can be used for treating diseases which can be treated with JAK2 kinase inhibitors.
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Paragraph 0202; 0203; 0204; 0205; 0208; 0209
(2019/02/04)
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- Structure-property correlations in model compounds of oligomer liquid crystals
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Structure-property correlations of the following model compounds for oligomer liquid crystals (LCs) have been investigated: monomers, C 6H5O(CH2)xCH3 (x = 4 and 5); dimers, C6H5O
- Sasanuma, Yuji,Ono, Tetsushi,Kuroda, Yoshihiko,Miyazaki, Emi,Hikino, Ken,Arou, Jun,Nakata, Kohji,Inaba, Hideaki,Tozaki, Ken-Ichi,Hayashi, Hideko,Yamaguchi, Kentaro
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p. 13163 - 13176
(2007/10/03)
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