欧盟法规
ECHA物质C&L通报上下游产品
diethyl 1-aminoethylphosphonate methyl magnesium iodide (diethoxyphosphoryl-ethylsulfanyl-methylene)-carbamic acid ethyl ester ethyl 2-diethoxyphosphorylpropionateN-Benzoyl-1-amino-ethyl-1-phosphonsaeure N-benzyloxycarbonyl-α-aminoethylphosphonic acid -phosphonic acidDL-1-(phthaloylamino)ethyl-phosphonic acid 1-R-1-[(N-benzyloxycarbonyl-L-alanyl)amino]ethanephosphonic acid 📜1-乙酰氨基乙基膦酸置于水体系中,用 重水 作为反应溶剂,化学反应 8.0H,以23.457%的收率获得产物
参考文献:1-(N-酰基氨基)烷基膦酸--水溶液中的脱酰
标题:1-(N-酰基氨基)烷基膦酸--水溶液中的脱酰
摘要:图形摘要摘要 1-(N-酰基氨基)烷基膦酸(Ac)-Aap属于令人感兴趣且具有潜在药理学重要性的1-氨基烷基膦酸衍生物组.由于 (Ac)-Aap 对水解脱酰的敏感性可以形成影响其生物活性的重要因素,我们在水性介质中对这些化合物进行了脱酰研究.在本文中,我们介绍了各种类型的 1-(N-酰氨基) 烷基膦酸 (Ac)-Aap 脱酰的结果,包括 1-(N-乙酰氨基) 烷基-膦酸 Ac-Aap,1-(N-氯乙酰氨基))烷基膦酸 Mca-Aap,1-(n-三氟乙酰氨基)烷基膦酸 Tfa-Aap 和 1-(n-苯甲酰氨基)-烷基膦酸 Bz-Aap,衍生自代表性 1-氨基烷基膦酸 Aap(glyp,Alap,Valp,Pglp,
DOI:10.1080/10426507.2017.1286494
专利信息
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-5981691-A
优先权日:1997-04-23
标题 :Imide-free and mixed amide/imide thermal synthesis of polyaspartate
发明人:SIKES C STEVEN
权利人:UNIV SOUTH ALABAMA
摘要:Thermal polymerization of a salt of aspartic acid affords polyaspartate directly without hydrolyzing polysuccinimide. Copolymerization of a salt of aspartic acid with aspartic acid itself affords a copolymer of succinimide and aspartate which may be readily derivatized to produce a sulfonated, phosphonated or hydrophobized polymer.
专利号:US-8431745-B2
优先权日:2006-03-29
标题 :Process for preparation of HIV protease inhibitors
发明人:CRAWFORD KENNETH R; DOWDY ERIC D; GUTIERREZ ARNOLD; POLNIASZEK RICHARD P; YU RICHARD HUNG CHIU
权利人:CRAWFORD KENNETH R; DOWDY ERIC D; GUTIERREZ ARNOLD; POLNIASZEK RICHARD P; YU RICHARD HUNG CHIU; GILEAD SCIENCES INC
摘要:A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.
专利号:US-7511113-B2
优先权日:2002-04-26
标题:Oligomeric hydroxy arylether phthalonitiles and synthesis thereof
发明人:KELLER TEDDY M; DOMINGUEZ DAWN D
权利人:US NAVY
摘要:An aromatic ether oligomer or polyaromatic ether comprising the formula:n n O—Ar n ;n nwherein Ar is an independently selected divalent aromatic radical; formed by reacting a dihydroxyaromatic with a dihaloaromatic; and wherein the reaction is performed in the presence of a copper compound and cesium carbonate. The polyaromatic ether is formed when neither the dihydroxyaromatic nor the dihaloaromatic is present in an excess amount. The aromatic ether oligomer is formed by using an excess of either dihydroxyaromatic or dihaloaromatic. A phthalonitrile monomer comprising the formula:n n nformed by reacting a 3- or 4-nitrophthalonitrile with a hydroxy-terminated aromatic ether oligomer. A thermoset formed by curing the phthalonitrile monomer. Processes for forming all the above.
专利号:US-7078406-B2
优先权日:2001-10-09
标 题 :Substituted diphenyloxazoles, the synthesis thereof, and the use thereof as fluorescence probes
发明人:CARVER JR THEODORE E; RINKER JAMES M
权利人:JOHNSON & JOHNSON PHARM RES
摘要:The present invention is directed to a compound of Formula I: n nwherein A, R 1 , and R 2 are defined herein. The present invention is also directed to compositions comprising compounds of Formula I, methods of using compounds of Formula I, and methods of making compounds of Formula I.
专利号:EP-0980404-A1
优先权日:1997-04-23
标题:Imide-free and mixed amide/imide thermal synthesis of polyaspartate