专利号:US-6339131-B1 优先权日:1999-12-06 标题 :Synthesis of poly (arylene ether)-poly(organosiloxane) copolymers 发明人:CELLA JAMES A; LISKA JURAJ; ULERY VICTORIA L; YEAGER GARY W; NYE SUSAN ADAMS; GUO HUA; SINGH NAVJOT 权利人:GEN ELECTRIC 摘要:A method comprising n (a) synthesis of a poly(arylene ether) having the structure (1) n wherein m is an integer having an average value in the range from about 3 to about 300; n (b) solution functionalization of polymer (1) to form functionalized poly(arylene ether) having the structure (2) n wherein X is a reactive functional group selected from the group consisting of anhydride, hydroxyl, epoxy, carboxyl, —R 1 OH, R 1 CO 2 R 2 , —R 1 CH 2 â•?CH 2 , or vinyl, wherein R 1 is a primary or secondary divalent alkyl or haloalky group having from 1 to 20 carbons, or an aryl group and R 2 is a primary or secondary alkyl group having from 1 to 10 carbons; and Q 4 is hydrogen, X, or a mixture thereof; n (c) reaction of functionalized poly(arylene ether) (2) with a poly(organosiloxane) having structure (3): n wherein x is zero or one and Y is a functional group reactive with X, selected from the group consisting of —OH, —CH 2 â•?CH 2 , epoxy, amino, carboxy, —C(O)CH 2 OH, or hydrogen, to form a poly(arylene ether)-poly(siloxane) copolymer, wherein the functionalization is in solution, and copolymer synthesis and isolation are effected by first solution nd then melt copolymerization.
专利号:US-8101804-B2 优先权日:2006-07-28 标 题 :Process for the synthesis of (E)-stilbene derivatives which makes it possible to obtain resveratrol and piceatannol 发明人:SCHOUTEETEN ALAIN; JUS SEBASTIEN; VALLEJOS JEAN-CLAUDE 权利人:SCHOUTEETEN ALAIN; JUS SEBASTIEN; VALLEJOS JEAN-CLAUDE; CLARIANT SPECIALTY FINE CHEM F 摘要:A subject-matter of the present invention is a novel process for the synthesis of (E)-stilbene derivatives targeted at obtaining in particular resveratrol and piceatannol.
专利号:EP-2676962-A1 优先权日:2012-06-21 标 题 :Derivatives of 1-aminoalkylphosphonate diaryl esters, method of 1-aminoalkylphosphonate diaryl ester derivatives preparation and their application 发明人:SIENCZYK MARCIN; GRZYWA RENATA; PIETRUSEWICZ EWA; OLEKSYSZYN JOZEF; WINIARSKI LUKASZ; BURSTER TIMO; BOEHM OTTO 权利人:UNIV ULM; WROCLAW UNIVERSITY OF TECHNOLOGY 摘要:The subject of the invention relates to 1-aminoalkylphosphonate diaryl esters of formula I, in which Bt represents biotin, W is a hydrocarbon linker chain of 5 to 10 carbon atoms, Y is the amino acid residues in an amount of 0 to 4, R is a substituent corresponding to the side chain of valine, alanine, leucine, phenylalanine, 4-guanidinephenylglycine, or 2-aminobutyric acid (Abu), X is the hydrogen or a compound selected from the group consisting of mercaptomethyl (S-methyl), methoxy (O-methyl), or carboxymethyl, and their use as inhibitors of serine proteases, and the low molecular weight molecular probes to detect the catalytically active forms of the enzymes. n A process for preparing 1-aminoalkylphosphonate diaryl esters of formula I, in which Bt represents biotin, W is a hydrocarbon linker chain of 5 to 10 carbon atoms, Y is the amino acid residues in an amount of 0 to 4, R is a substituent corresponding to the side chain of valine, alanine, leucine, phenylalanine, 4-guanidinephenylglycine, or 2-aminobutyric acid (Abu), X is the hydrogen or a compound selected from the group consisting of mercaptomethyl (S-methyl), methoxy (O-methyl), or carboxymethyl relies on application of triaryl phosphite, obtained from the phenol substituted at para position phosphorus (III) chloride in refluxing acetonitrile and is subjected to amidoalkylation reaction with benzyl carbamate and an aldehyde such as acetaldehyde, propionic aldehyde, iso -butyric aldehyde, phenylacetic aldehyde, p-nitrobenzoic aldehyde and isovaleric aldehyde, followed by the synthesis of hydrobromide salts of 1-aminoalkylphosphonate diaryl esters, in which the benzyloxycarbonyl (Cbz) protective group is removed, and in the next step is reacted with an amino acid containing protected α-amino group in the presence of a coupling reagent. The resulting phosphonic dipeptide containing tert-butoxycarbonyl (t-Boc) protective group is subjected to deprotection of α-amino group and obtained dipeptidyl 1-aminoalkylphosphonate diaryl ester is coupled with another amino acid with protected α-amino group, biotin or a derivative thereof in a manner analogous to that described above.
专利号:US-2025188022-A1 优先权日:2022-02-07 标 题 :Process for the preparation of nafamostat, camostat and their derivatives 发明人:AHMED RIYAZ; KUMAR GULSHAN; MAHAJAN SHEENA; Verma Praveen Kumar; CHAM PANKAJ SINGH; KUMAR AMIT; AHMED QAZI NAVEED; REDDY DUMBALA SRINIVASA; SHANKAR RAVI; SINGH PARVINDER PAL 权利人:COUNCIL SCIENT IND RES 摘要:The invention provides a novel, economical and practical route for the synthesis of an ester from acid and alcoholic functionalities using Trihalotriazine as coupling agent. Specifically, the invention provides a novel, economical and practical route for the preparation of Nafamostat and Camostat. Synthesis of p-guanidinobenzoic acid (Al) was also achieved from thiourea and p-aminobenzoic acid by using trihalotriazine as coupling reagent.
专利号:US-2006115880-A1 优先权日:2002-12-03 标 题 :Enzymatic production of acyl flavonoid derivatives 发明人:GHOUL MOHAMED; ENGASSER JEAN-MARC; MOUSSOU PHILIPPE; PAULY GILLES; ARDHAOUI MELIKA; FALCIMAIGNE AUDE 权利人:COGNIS FRANCE SA 摘要:Disclosed is a method for enzymatic synthesis of esters of flavonoid and flavonoid derivatives, according to which a reaction medium containing an organic solvent, a glycosylated flavonoid or aglycon flavonoid, an acyl group donor, and an enzymatic catalyst is produced, b) additional quantities of flavonoid and/or acyl donor are optionally added during the reaction, and c) the obtained esters are separated from the enzymatic particles and the solvent. The inventive method is characterized by maintaining the concentration of water and/or alcohol which are formed during the reaction to below 150 mM. Advantageously, the molar ratio of flavonoid to acyl donor in the reaction medium is maintained in the range from 0.01 to 20.00 during the reaction.
专利号:US-5639785-A 优先权日:1995-06-07 标 题 :Methods for the treatment of baldness and gray hair using isoflavonoid derivatives 发明人:KUNG PATRICK C 权利人:GLOBAL PHARMA LTD 摘要:The present invention relates to novel pharmaceutical compositions of isoflavanoid derivatives useful for the treatment of male pattern baldness and alopecia areata, and their use in promoting the conversion of gray hair to the original pigment in hair follicles. Also described herein are methods for the synthesis of isoflavanoid derivatives.
1: Zhao H, Jiang Z, Chang X, Xue H, Yahefu W, Zhang X. 4-Hydroxyphenylacetic Acid Prevents Acute APAP-Induced Liver Injury by Increasing Phase II and Antioxidant Enzymes in Mice. Front Pharmacol. 2018 Jun 19;9:653. doi: 10.3389/fphar.2018.00653. 2: Liu Z, Xi R, Zhang Z, Li W, Liu Y, Jin F, Wang X. 4-hydroxyphenylacetic acid attenuated inflammation and edema via suppressing HIF-1α in seawater aspiration- induced lung injury in rats. Int J Mol Sci. 2014 Jul 21;15(7):12861-84. doi: 10.3390/ijms150712861. 3: Shen YP, Pan Y, Niu FX, Liao YL, Huang M, Liu JZ. Biosensor-assisted evolution for high-level production of 4-hydroxyphenylacetic acid in Escherichia coli. Metab Eng. 2022 Mar;70:1-11. doi: 10.1016/j.ymben.2021.12.008. Epub 2021 Dec 26.
合成参考文献
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