专利号:US-2003180804-A1 优先权日:2001-10-29 标题:Solid phase synthesis of chemical libraries 发明人:PRYOR KENT E; LEWIS RONALD D; BROWN JASON W 权利人:CORVAS INT INC 摘要:The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.
专利号:US-2018312463-A1 优先权日:2015-10-22 标题:Synthesis of Cyclohexane Carboxamide Derivatives Useful as Sensates in Consumer Products 发明人:YELM KENNETH EDWARD; WOS JOHN AUGUST; BUNKE GREGORY MARK; FREDERICK HEATH; HAUGHT JOHN CHRISTIAN; HOKE STEVEN HAMILTON; SREEKRISHNA KOTI TATACHAR; LIN YAKANG 权利人:PROCTER & GAMBLE 摘要:Synthesis methods to produce a series of carboxamides built off of an (S)-2-amino acid backbone or an (R)-2-amino acid backbone, depending upon the desired diastereomer of the end product.
专利号:US-2022288005-A1 优先权日:2019-07-26 标题:Synthesis of pro-resolving analogs and compositions therefor 发明人:VAN DYKE THOMAS E; SERHAN CHARLES N 权利人:NOCENDRA INC 摘要:This disclosure relates to methods of synthesizing certain lipoxin analogs (e.g., lipoxin mimetics, etc.) and pharmaceutical compositions comprising these pro-resolving compounds. Methods of administering the lipoxin mimetics (e.g., lipoxin A4 mimetics, lipoxin B4 mimetics, etc.) to patients in need thereof are also provided.
专利号:US-2019276389-A1 优先权日:2015-12-18 标题:Synthesis of aryl cyclohexane ester derivatives useful as sensates in consumer products 发明人:WOS JOHN AUGUST; YELM KENNETH EDWARD; BUNKE GREGORY MARK; FREDERICK HEATH ALAN; REILLY MICHAEL; HAUGHT JOHN CHRISTIAN; SREEKRISHNA KOTI TATACHAR; LIN YAKANG 权利人:PROCTER & GAMBLE 摘要:Personal care compositions, such as oral care and skin care compositions containing a flavor/perfume system comprising one or more coolants. The pleasant cool sensation provided by a coolant is enhanced in terms of quicker onset, greater intensity, impact or longer duration, which improves appeal and acceptability of the compositions to consumers.
专利号:US-8754259-B2 优先权日:2008-08-15 标 题 :Synthesis of cyclohexane derivatives useful as sensates in consumer products 发明人:YELM KENNETH EDWARD; BUNKE GREGORY MARK; HAUGHT JOHN CHRISTIAN 权利人:PROCTER & GAMBLE; PROCTER & GAMBLE 摘要:The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect. Preparation schemes for neoisomers of other menthyl derivatives which are useful as coolants, including esters, ethers, carboxy esters and other N-substituted carboxamides are also provided.
专利号:US-8354530-B2 优先权日:2005-07-28 标 题:Process for the synthesis of rosuvastatin calcium 发明人:ZLICAR MARKO 权利人:LEK PHARMACEUTICALS; ZLICAR MARKO 摘要:Present invention represents process for the preparation of HMG-CoA reductase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain.
[参考文献]: Tokuoka Y, Et Al. Enhancement In Skin Permeation Of 5-Aminolevulinic Acid Using L-Menthol And Its Derivatives.Drug Dev Ind Pharm. 2008 Jun;34(6):595-601.
合成参考文献
摘要:Bertau, M.; Jeromin, G. E., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 164. 摘要:Vicens, L.; Borrell, M.; Costas, M., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 125. 摘要:Koike, T.; Akita, M., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 571. 摘要:S13 | EUCOSMETICS | Combined Inventory of Ingredients Employed in Cosmetic Products (2000) and Revised Inventory (2006) | DOI:10.5281/zenodo.2624118 参考文献:10.1021/ol049675n 摘要:Hata S, Iguchi M, Iwasawa T, Yamada K, Tomioka K. Lithium amide assisted asymmetric Mannich-type reactions of menthyl acetate with PMP-aldimines. Org Lett. 2004 May 27;6(11):1721–3. doi: 10.1021/ol049675n.