4-硝基-L-苯丙氨酸置于氯化亚砜体系中,用 甲醇 用作溶剂,以76 %的收率获得(S)-4-硝基苯基丙氨酸甲酯盐酸盐 参考文献:Cargo Encapsulation In Photochromic Supramolecular Hydrogels Depends On Specific Guest‐gelator Supramolecular Interactions 标题:Cargo Encapsulation In Photochromic Supramolecular Hydrogels Depends On Specific Guest‐gelator Supramolecular Interactions 摘要:摘要光致变色超分子水凝胶是光触发药物释放和仿生技术的前景材料.在此,我们利用先进的核磁共振技术,对多肽衍生的光致变色超分子水凝胶进行了结构分析.这些结果有助于详细,正确地了解加载过程,并有助于正确设计用于光诱导给药的药理学相关系统. Doi:10.1002/ejoc.202300227
专利号:US-2009162290-A1 优先权日:2005-09-09 标 题 :Method for the synthesis of penta-pendant enantiomer-pure chelators and process for therapeutically active bioconjugates preparation by a covalent binding thereof 发明人:BENES IVAN; CIHELNIK SIMON; DROZ LADISLAV; SRAMEK MARTIN 权利人:THERAPHARM GMBH 摘要:The present invention provides a method for synthesis and binding methods of pentapendant enantiomer-pure chelators of formula (VII) wherein R 1 , R 2 , R 3 , R 4 are groups forming an adequate enantiomer of the chelator; and X 1 -X 5 , Y 1 -Y 5 , Z 1 -Z 5 each individually forming pendant chelating groups.
专利号:US-5135737-A 优先权日:1986-11-10 标 题:Amplifier molecules for enhancement of diagnosis and therapy 发明人:KEANA JOHN F W 权利人:OREGON STATE 摘要:Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
专利号:WO-9403593-A1 优先权日:1992-08-04 标题 :Amplifier molecules for enhancement of diagnosis and therapy 发明人:KEANA JOHN F W 权利人:OREGON STATE 摘要:Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
专利号:US-6303791-B1 优先权日:1995-08-07 标题 :One pot synthesis of 2-oxazolidinone derivatives 发明人:PATEL RAJNIKANT 权利人:ZENECA LTD 摘要:The invention provides an improved process for preparing compounds of formula (I
专利号:US-6909005-B1 优先权日:1995-08-07 标题 :One post synthesis of 2-oxazolidinone derivatives 发明人:PATEL RAJNIKANT 权利人:ASTRAZENECA UK LTD 摘要:The present invention provides an improved (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone product which is prepared by a method which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VII) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.
专利号:US-6160123-A 优先权日:1995-08-07 标 题:One pot synthesis of 2-oxazolidinone derivatives 发明人:PATEL RAJNIKANT 权利人:ZENECA LTD 摘要:The present invention provides an improved process for preparing (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VIl) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.