专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-5763587-A 优先权日:1987-11-27 标题:Process for the synthesis of amikacin 发明人:MANGIA ALBERTO 权利人:GIST BROCADES ITALY SPA 摘要:In the synthesis of amikacin, having the formula: (I) by acylation of a diprotected derivative of kanamycin A with a reactive derivative of L-(-)-4-amino-2-hydroxybutyric acid, the selection of the reaction solvent and of the pH conditions permit the industrial economically and the synthesis yield to be improved.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-2024197774-A1 优先权日:2021-04-16 标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles 发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO 权利人:UNIV TEXAS 摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.
专利号:US-4902790-A 优先权日:1985-10-10 标 题 :Novel process for the synthesis of amikacin 发明人:MANGIA ALBERTO; GIOBBIO VICENZO; ORNATO GIORGIO 权利人:PIERREL SPA 摘要:A novel process for the synthesis of amikacin starting from kanamycin A protected at the positions 3 and 6' is described comprising the reaction of kanamycin A with a salt of a bivalent metal cation selected from zinc, nickel, iron, cobalt, manganese, copper and cadmium in the presence of water as the solvent or co-solvent followed by the in situ reaction of the resulting complex with a reactive derivative of L-amino-2-hydroxy-butyric acid, removal of the metal cation of the protecting groups and purification of the thus obtained raw product. The acylation under these conditions is extremely selective.
专利号:US-2011087037-A1 优先权日:2007-10-31 标题:Synthesis of ring b abeo-sterols as novel inhibitors of mycobacterium tuberculosis 发明人:RODRIGUEZ-PIERLUISSI ABIMAEL D; WEI XIAOMEI 权利人:INTELLECTUAL PROPERTY AND TECHNOLOGY VIC OFF OF 摘要:Novel 3β-hydroxy-Δ 5 -steroid analogs possessing a contracted cyclopentane B-ring provide good inhibitory activity against Mycobacterium tuberculosis . The 5(6→7)abeo-sterol nucleus present in compounds of the invention represents a novel scaffold for the development of new antitubercular agents.
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合成参考文献
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