📜对羟基联苯置于tris(Triphenylphosphine)Ruthenium(II) Chloride,四氯化钛体系中,用 二氯甲烷,乙酸乙酯,苯 作为反应溶剂,化学反应 3.5H,反应生成 苯基-P-苯醌 参考文献:Ruthenium-Catalyzed Oxidation Of Phenols With Alkyl Hydroperoxides. A Novel,Facile Route To 2-Substituted Quinones 标题:Ruthenium-Catalyzed Oxidation Of Phenols With Alkyl Hydroperoxides. A Novel,Facile Route To 2-Substituted Quinones 摘要: DOI:10.1021/ja954009Q
专利号:EP-2465936-A1 优先权日:2010-12-20 标题 :Enzymatic synthesis of statins and intermediates thereof 权利人:LEK PHARMACEUTICALS 摘要:The present invention discloses a process for preparing an active pharmaceutical ingredient (API) or intermediates thereof, notably particular step in the synthesis of an intermdiate useful for example in the preparation of statins, by using an enzyme capable of catalyzing oxidation or dehydrogenation. The invention further provides an expression system effectively translating said enzyme. In addition, the invention relates to a specific use of such enzyme for preparing API or intermediate thereof, and in particular for preparing statin or interemediate thereof.
专利号:US-5094782-A 优先权日:1990-12-24 标 题:Synthesis of capsacin derivatives and their use as an analgesic drug and vessel dilation drug 发明人:CHEN ING-JUN; YEH JWU-LAI 权利人:NAT SCIENCE COUNCIL REPUBLIC CHINA 摘要:Nonanoyl vanillylamide succinate was synthesized from synthetic capsaicin (nonanoyl vanillylamide) and succinic anhydride. The antinociceptive and cardiovascular effects of nonanoyl vanillylamide and its derivatives were investigated. We found that nonanoyl vanillylamide and nonanoyl vanillylamide succinate strongly inhibited the writhing response, led to the vascular smooth muscle relaxation, produces bradycardia and a fall of blood pressure. The potency of nonanoyl vanillylamide succinate was found to be slight greater than that of nonanoyl vanillylamide, when compared with the same molar dose/kg of their administrations.
专利号:US-5098531-A 优先权日:1988-03-24 标题 :Electrochemical synthesis of 2-aryl-hydroquinones 发明人:GATTI NORBERTO; FOA MARCO 权利人:DONEGANI GUIDO IST 摘要:Preparation of 2-aryl-hydroquinones of formula (I) by oxidizing by an electrochemical route a compound of formula (II): ##STR1## wherein A represents an aryl group optionally substituted with groups compatible with the reaction conditions in an acidic aqueous reaction medium, at temperatures within the range of from 10° to 100° C., and with anodes of graphite or PbO 2 . The products are used in photography and in the field of liquid-crystal polymers.
专利号:US-4895954-A 优先权日:1986-07-26 标题 :Precursors for synthesis of triphendioxazine dyestuffs 发明人:SCHWAIGER GUENTHER; SPRINGER HARTMUT; HELMLING WALTER 权利人:HOECHST AG 摘要:Water-soluble triphendioxazine compounds which have fiber-reactive properties as dyestuffs, which afford deep and fast dyeings on fiber materials, such as wool and, in particular, cellulose, and which correspond to the formula (1) ##STR1## in which: n is the number 0 or 1; n Y is the vinyl group or an ethyl group containing, in β-position, a substituent which can be eliminated by means of an alkali; n Q 1 and Q 2 both represent a benzotriazole radical which can also be additionally substituted in the benzene nucleus by alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halogen, carboxy or sulfo; n B is --O--, --S--, --NH-- or --N(R')-- wherein R' is optionally substituted alkyl having 1 to 6 carbon atoms; n W 1 and W 2 both represent a divalent, optionally substituted aliphatic, cycloaliphatic, aliphatic-cycloaliphatic, araliphatic or aromatic-carbocyclic radical, it being possible for the aliphatic radicals to be interrupted by hetero groups --O--, --S--, --SO 2 --, --CO--, 1,4-piperidino, --NH-- and/or --N(R o )-- in which R o is optionally substituted alkyl having 1 to 6 carbon atoms or alkanoyl having 2 to 5 carbon atoms, and/or for aliphatic and aryl radicals to be attached to one another through such a hetero group; n R is hydrogen, alkyl having 1 to 6 carbon atoms, alkoxy having 1 to 6 carbon atoms, halogen, carboxyl or sulfo; n E is hydrogen, sulfo, carboxyl, a group --SO 2 --Y as defined above or an optionally substituted sulfonamide group; and n X 1 and X 2 are both hydrogen or halogen, cycloalkyl, alkoxy, aryloxy, aryl or another substituent; n and at least one carboxy, sulfo or sulfato group is present in the molecule (1), n and pre-products of those triphendioxazine compounds, of the general formula ##STR2## in which K is an amino or nitro group, Y' is β-hydroxyethyl or defined as for Y, W has one of the meanings of W 1 , and E' is hydrogen, sulfo, carboxy or a group of the formula --SO 2 --Y' defined above, or an optionally substituted sulfonamide group, and R, B and R* have the above meanings.
专利号:US-3935314-A 优先权日:1971-11-24 标题 :Anti-hypertensive compositions of benzimidazole derivatives 发明人:WATTS ERIC ALFRED 权利人:BEECHAM GROUP LTD 摘要:Antihypertensive pharmaceutical compositions comprising a compound of the formula (II) ##SPC1## n or pharmaceutically acceptable salts or solvates thereof wherein R 1 is nitrile or amidino; R 2 is hydrogen or lower hydrocarbon; R 3 , R 4 , R 5 and R 6 which may be the same or different, are each selected from hydrogen, halogen, nitro, trifluoromethyl, lower alkyl, lower acyl, hydroxyl, lower etherified hydroxyl or lower acylated hydroxyl; together with a pharmaceutically acceptable carrier. The compounds of formula (II) are also useful as intermediates in the synthesis of the corresponding 2-aminoimidazoline compounds.
专利号:US-4089855-A 优先权日:1976-04-23 标题:Process for the stereoselective reduction of 6- and 8-keto morphine and morphinan derivatives with formamidinesulfinic acid and compounds obtained thereby 发明人:CHATTERJIE NITHIANANDA; INTURRISI CHARLES E 权利人:CORNELL RES FOUNDATION INC 摘要:Process for the stereoselective synthesis of 6β-and 8β- hydroxy epimers by the chemical reduction of 6- and 8-keto derivatives in the morphine and morphinan series utilizing alkaline formamidinesulficic acid. The 6β- and 8β-hydroxy derivatives obtained according to the invention evidence narcotic antagonist and/or agonist activity and are also useful in the chemical and pharmacological standardization of various morphine and codeine derivatives and metabolites.
1: Pinho-Ribeiro FA, Hohmann MS, Borghi SM, Zarpelon AC, Guazelli CF, Manchope MF, Casagrande R, Verri WA Jr. Protective effects of the flavonoid hesperidin methyl chalcone in inflammation and pain in mice: role of TRPV1, oxidative stress, cytokines and NF-κB. Chem Biol Interact. 2015 Feb 25;228:88-99. doi: 10.1016/j.cbi.2015.01.011. Epub 2015 Jan 21.
合成参考文献
摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2018) 4, 154. 摘要:Liu, G.; Chen, P., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 12. 摘要:Arzneimittel-Forschung. Drug Research., 20(1751), 1970 [] 摘要:Wang, P.-S.; Sayed, M.; Gong, L.-Z., Science of Synthesis: Knowledge Updates, (2023) 1, 204. 摘要:Escudero, J.; Besset, T., Science of Synthesis: Cross-Dehydrogenative Coupling, (2023) nan, 71.