专利号:WO-2021260722-A1 优先权日:2020-06-21 标 题:Design, synthesis of novel oxyindole inhibitors of denv rna dependent rna polymerase 发明人:GUNDLA RAMBABU; ASTHANA SHAILENDRA; BHATTACHARYYA SANKAR; MADDIPATI VENKATANARAYANA CHOWDARY; MITTAL LOVIKA; KAUR JASKARAN; RAWAT YOGITA 权利人:TRANSLATIONAL HEALTH SCIENCE AND TECH INSTITUTE; GANDHI INSTITUTE OF TECH AND MANAGEMENT 摘要:The present invention is drawn to novel compounds of formula I, II and III, including any conformational isomeric form, salts and solvates for inhibition of DENV RNA dependent and RNA polymerase. The present invention also discloses a process of synthesis of the compounds, compositions comprising the said compounds and use of the compounds and treatment comprising the compounds of the present invention.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-8722852-B2 优先权日:2006-04-28 标 题 :Cosmetic composition for stimulating the synthesis of proteins of the basement membrane 发明人:ZIEGLER HUGO; IMFELD DOMINIK; STOCKLI MARTIN; HEIDL MARC 权利人:ZIEGLER HUGO; IMFELD DOMINIK; STOCKLI MARTIN; HEIDL MARC; DSM IP ASSETS BV 摘要:Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which R 1 is H, C 1 -C 20 -alkyl, cycloalkyl or aryl-C 1 -C 4 -alkyl, n is 1-4, X is —O—, —NH— or —NR 2 — and R 2 H or C 1 -C 20 -alkyl; and at least one compound corresponding to the above formula (I) but in which XR 1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is —NR 2 — and both R 1 and R 2 are different from H, and the compounds corresponding to formula (I) but in which XR 1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid, as such.
专利号:US-8076479-B2 优先权日:2006-08-28 标题 :Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates 发明人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI 权利人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI; SCHERING CORP 摘要:Disclosed is a process for the synthesis of compounds of Formula I n nby sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1,n n nwherein R 1 is a linear, branched, or cyclic alkyloxy functional group of the structure (—R 2a —OH), R 2a is a linear, branched or cyclic alkyl group, R 2 is a linear, branched or cyclic alkyl group, and R 3 is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1,n n nwith a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.
专利号:US-5783698-A 优先权日:1996-01-23 标题:Chemical synthesis of 1,3-disubstituted quinazolinediones 发明人:SMITH ADRIAN LEONARD 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to a method for the synthesis of 1,3-disubstituted quinazolinedione derivatives which comprises: n (a) reacting a haloformate functionalized polystyrene resin with a substituted anthranilic acid derivative under conditions effective to form a urethane-linkage; n (b) reacting the product of step (a) with a primary amine under conditions effective to form an anthranilamide derivative; n (c) heating the anthranilamide to effect intramolecular cyclization thereby liberating the 1,3-disubstituted quinazolinedione derivative from the resin into solution; and n (d) isolating the 1,3-disubstituted quinazolinedione by filtration and solvent removal.
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合成参考文献
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 247. 摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 22. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2018) 2, 98. 摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 20. 摘要:Harris, P. A., Science of Synthesis Knowledge Updates, (2021) 3, 125.