- Preparation method of zucapsaicin and its intermediate
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The invention discloses a preparation method of zucapsaicin and its intermediate. The invention provides a preparation method of zucapsaicin I. The preparation method comprises that a zucapsaicin intermediate IV and a dialkylborane reducing agent in an organic solvent in the presence of a catalyst undergo a reduction reaction to produce zucapsaicin I. The preparation method is simple and safe in operation, the reaction is easy to monitor, the zucapsaicin I product has high purity, a total yield is high, a production cost is low and the preparation method is suitable for industrial production.
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Paragraph 0080-0090
(2019/01/08)
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- Vanilloids. 1. Analogs of Capsaicin with Antinociceptive and Antiinflammatory Activity
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As part of a program to establish structure-activity relationships for vanilloids, analogs of the pungent principle capsaicin, the alkyl chain portion the parent structure (and related compounds derived from homovanillic acid) was varied.In antinociceptive and antiinflammatory assays (rat and mouse hot plate and croton oil-inflamed mouse ear), compounds with widely varying alkyl chain structures were active.Short-chain compounds were active by systemic administration in the assays mentioned above but they retained the high pungency and acute toxicity characteristic of capsaicin.In contrast, the long chain cis-unsaturates, NE-19550 (vanillyloleamide) and NE-28345 (oleylhomovanillamide), were orally active, less pungent, and less acutely toxic than capsaicin.The potential of these compounds as antiinflammatory/analgesic agents is discussed in light of recent data on the mechanism of action of vanilloids on sensory nerve fibers.
- Janusz, John M.,Buckwalter, Brian L.,Young, Patricia A.,LaHann, Thomas R.,Farmer, Ralph W.,et al.
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p. 2595 - 2604
(2007/10/02)
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- The Capsaicinoids: Their Separation, Synthesis, and Mutagenicity
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Capsaicin (1b), the pungent ingredient in many varietes of Capsicums has recently been implicated as a possible carcinogen.When obtained from natural sources 1b is always accompanied by a number of related homologues.We have isolated seven of these homologues, characterized them, and synthesized them by a general and unique route developed in our laboratories.Also reported are mutagenicity data for 1b and an extract of red pepper as measured by the Ames assay and the V-79 mammalian cell assay.
- Gannett, Peter M.,Nagel, Donald L.,Reilly, Pam J.,Lawson, Terence,Sharpe, Jody,Toth, Bela
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p. 1064 - 1071
(2007/10/02)
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