- Vanillylamine type new compound as well as preparation method and medical appliance thereof
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The invention provides a novel compound of a treatment medicine or preventive medicine serving as an analgesic drug, and a medicinal composition containing the same. The invention relates to a vanillylamine type new compound or a pharmaceutically acceptab
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- Method for preparing characterized
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The invention provides a preparation method of gefarnate. The preparation method is characterized by comprising the following steps: conducting phosphorylation reaction on bromobutyric acid ethyl ester and triphenylphosphine to obtain phosphorus ylide solution, conducting whittig reaction to the phosphorus ylide solution and geranylacetone to obtain farnesyl ethyl acetate; adding the farnesyl ethyl acetate into sodium hydroxide and N,N-dimethylformamide so as to conduct acidification reaction to obtain farnesyl acetic acid; and adding geraniol, dimethylbenzene and a polymerization inhibitor into farnesyl acetic acid for conducting heating reflux and vacuum concentration, and collecting fraction at 186-200 DEG C to obtain gefarnate. According to the method, the technical problems that the gefarnate obtained in the prior art is long in synthetic route, low in yield, low in yield purity, complicated in after-treatment, and not applicable to industrial production can be solved.
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Paragraph 0071; 0073
(2017/01/09)
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- 2-(Acyloxy)ethylphosphonate analogues of prenyl pyrophosphates: synthesis and biological characterization
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2-(Acyloxy)ethylphosphonate analogues of geranyl, farnesyl, and geranylgeranyl pyrophosphate have been prepared. Horner-Wadsworth-Emmons condensation of different terpene aldehydes with an unsymmetrical bisphosphonate was the key step in syntheses of the phosphonates bearing α,β-unsaturated acyloxy groups. After preparation of the respective phosphonic acids through reaction with TMSBr, both acids and esters were tested for their effects on DNA synthesis in human-derived myeloid and lymphoid leukemia cell lines. The phosphonate esters varied substantially in their ability to impair proliferation of the different cell lines, but testing against one possible target, farnesyl protein transferase (FPTase), revealed little impact at concentrations ranging up to 10μM. Because the corresponding 2,3-dihydro compounds showed similar biological activity, conjugate addition would not appear to be involved in the toxicity. Copyright (C) 2000 Elsevier Science Ltd.
- Cermak, Diana M.,Wiemer, David F.,Lewis, Kriste,Hohl, Raymond J.
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p. 2729 - 2737
(2007/10/03)
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- SUPERACID CYCLIZATION OF ESTERS OF SOME BISHOMOISOPRENOID ACIDS
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It is shown that on the superacid cyclization of esters of bishomobicyclogeranylgeranic and E,E-bishomofarnesic acids fully cyclized hydroxyesters are formed in good yield, while on the interaction of esters of 6-hydroxy- and 6-acyloxy-15-bishomobicyclogeranylgeranic acids with a superacid no carbocyclization takes place.
- Ungur, N. D.,Tuen, Nguen Van,Popa, N. P.,Vlad, P. F.
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p. 561 - 568
(2007/10/02)
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- Process for preparing stereospecific nerolidol and ester thereof
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A process for obtaining a stereospecific nerolidol at the Δ6 -position thereof by rectifying a mixture of Δ6 -cis-nerolidol and Δ6 -trans-nerolidol in rectification column having from 10 to 100 theoretical plates with a reflux ratio of from 2 to 200 at a temperature below 230° C. under reduced pressure to separate each stereospecific nerolidol from said mixture.
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