专利号:WO-2016005407-A1 优先权日:2014-07-07 标 题:One-pot synthesis of squaramides 发明人:MÃ?RQUEZ LÓPEZ MARÃ?A EUGENIA; ALEGRE REQUENA JUAN VICENTE; PÉREZ HERRERA RAQUEL 权利人:UNIV ZARAGOZA; CONSEJO SUPERIOR INVESTIGACION 摘要:The present invention refers to the first one-pot synthesis of squaramides. The one-pot synthesis of squaramides described herein is an easy and straightforward procedure to obtain squaramide derivatives which saves energy, avoids time consuming purification steps, reduces costs and provides better yields as compared with those squaramides obtained through the traditional 'stop-and-go' approach. Moreover, the authors of the present invention herein demonstrate the efficiency of this one-pot process with the synthesis of three biologically active structures, improving in most of the cases the results of the previous stepwise syntheses.
专利号:US-6909010-B2 优先权日:2001-04-11 标题:Facile synthesis of symmetric esters of alkylenebisphosphonic acids 发明人:HERLINGER ALBERT W; STEPINSKI DOMINIQUE C 权利人:UNIV LOYOLA CHICAGO 摘要:A facile synthesis of symmetric esters of C 1 -C 10 alkylenebisphopsphonic acids is disclosed in which a C 1 -C 10 alkylenebis(phosphonic dichloride) is reacted with an alcohol in the presence of a catalytic amount of 1H-tetrazole and a base in an aprotic solvent to form a first reaction mixture. The first reaction mixture is maintained for a time period sufficient to form a C 1 -C 10 alkylenebis(chloro ester phosphonate) that is reacted under basic conditions with an excess of a hydroxylated compound to form a second reaction mixture that is itself maintained for a time period sufficient to form a C 1 -C 10 alkylenebis(ester phosphonate) partial ester, homoleptic tetraester or mixed tetraester. The material so formed can be recovered or used as is.
专利号:US-9416113-B2 优先权日:2011-02-10 标 题:Formation of N-protected bis-3,6-(4-aminoalkyl)-2,5,diketopiperazine 发明人:FREEMAN JOHN J; STAMPER ADRIENNE; HEITMANN MELISSA 权利人:MANNKIND CORP; MANNKIND CORP 摘要:The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.
专利号:WO-2013117440-A1 优先权日:2012-02-09 标 题 :Synthesis of water-soluble phosphine oxides by pd/c-catalyzed p-c coupling in water 发明人:RANOCCHIARI MARCO; RUMMELT STEPHAN; VAN BOKHOVEN JEROEN A 权利人:SCHERRER INST PAUL 摘要:Cross-coupling between diphenylphosphine oxide and halogenated benzoic acids catalyzed by Pd/C in water is a green, simple and fast protocol to obtain water-soluble tertiary phosphine oxides without the addition of ligands and additives. Low reaction times, microwave irradiation, and high substrate scope make this method general and excellent for lab- and large-scale synthesis without the need to use organic solvents for neither reaction nor workup.
专利号:US-10899878-B2 优先权日:2017-04-06 标 题:Phosphorus-containing caprolactone monomers for synthesis of flame retardant polycaprolactones 发明人:CAMPBELL ERIC J; CZAPLEWSKI SARAH K; KOBILKA BRANDON M; WERTZ JASON T 权利人:IBM 摘要:A process of forming a flame retardant monomer includes forming a hydroxyl-functionalized caprolactone molecule, and reacting the hydroxyl-functionalized with a phosphorus-containing flame retardant molecule to form a flame retardant-functionalized caprolactone monomer. A flame retardant monomer includes at least one moiety derived from a hydroxyl-functionalized caprolactone molecule and at least one phosphorus-containing flame retardant moiety. A flame retardant polymer includes at least two flame retardant monomer repeat units, each flame retardant monomer repeat unit including at least one moiety derived from a hydroxyl-functionalized caprolactone molecule and at least one phosphorus-containing flame retardant moiety.
专利号:WO-2025010390-A1 优先权日:2023-07-05 标题 :Synthesis of pyruvate kinase activators 发明人:FANDRICK DANIEL; LEUNG CHUN YUEN; CRANE SHELDON; LACHANCE NICOLAS; LE ROUX ANTOINE; PATEL JIGNESH; VALAMALE ASHALATHA 权利人:AGIOS PHARMACEUTICALS INC 摘要:Provided herein are methods for preparing activators of Pyruvate Kinase (PK) or a salt or a hydrate thereof.