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-6063919-A 优先权日:1998-08-14 标题:Process for the synthesis of exochelins 发明人:GAUDIOSO LARRY A; WEGLARZ MICHAEL A 权利人:KEYSTONE BIOMEDICAL INC 摘要:A process for the synthesis of an Exochelin comprising the steps of generating L-N-[(2-benzyloxy-(benzoyl)] serine or L-N-[2-benzyloxy (benzoyl)] threonine, creating L-N-t-Boc- epsilon -hydroxynorleucine and reacting same to produce L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester, providing a dicarboxylic acid and forming an O-benzyl methyl hydroxamate from the dicarboxylic acid, coupling the O-benzyl methyl hydroxamate with the L-N-Boc- epsilon -bromonorleucine trimethylsilylethyl ester to give an L-N2-Boc-N6-methyl,N6-(benzyloxy) lysine 2-trimethylsilylethyl ester which incorporates the dicarboxylic acid as modified above, removing the N-tert-butoxycarbonyl protecting group from the L-N2-Boc-N6-methyl, N6-(benzyloxy) lysine 2-trimethylsilylethyl ester to yield a substituted lysine, and coupling the same with the L-N-[2-benzyloxy (benzoyl) serine or -threonine to yield a 2-trimethyl silylethyl ester of dibenzyl Exochelic acid, transforming the 2-trimethyl silylethyl ester of dibenzyl Exochelic acid to dibenzyl Exochelic acid, preparing benzyl epi-cobactin, forming an ester bond between the dibenzyl Exochelic acid and benzyl epi-cobactin to form an intermediate, and, hydrogenolytically removing three benzyl groups from said intermediate, resulting in the synthesized Exochelin. More particularly, a synthesis for Exochelin 786SM (R) is disclosed wherein the dicarboxylic acid is suberic acid and the serine form is utilized.
专利号:US-2024082435-A1 优先权日:2021-02-26 标 题 :Solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates and their use as precursors for therapeutic and/or diagnostic agents 发明人:PINTO ARTUR; BONTEMPS ALEXIS; LEMAIRE LUCAS 权利人:TELIX INT INNOVATIONS PTY LTD 摘要:The disclosure provides methods for the solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates. The disclosure also relates to key intermediates of this process and methods for their preparation such as a method of preparing a compound of formula (V). Also disclosed are use of the conjugates as precursors for therapeutic and/or diagnostic agents, including treating and diagnosing prostate cancer.
专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:WO-2023150820-A1 优先权日:2022-02-10 标题 :Process for the synthesis of radiolabelled biological polymers 发明人:WICHMANN CHRISTIAN WERNER; RUDD STACEY ERIN; SCOTT ANDREW MARK; DONNELLY PAUL STEPHEN 权利人:UNIV MELBOURNE; OLIVIA NEWTON JOHN CANCER RES INSTITUTE 摘要:Processes for the synthesis of zirconium-89 radiolabelled biological polymer-chelate agent conjugates are provided. Radiolabelling is performed in the presence of a polycarboxylate buffer resulting in improved reaction kinetics and short process times. The processes provide a high degree of reproducibility, excellent radiochemical yields and may be automated.
专利号:US-5367113-A 优先权日:1991-10-30 标题 :Method for synthesis of desferrioxamine B, analogs and homologs thereof 发明人:BERGERON JR RAYMOND J 权利人:UNIV FLORIDA 摘要:Synthesis of desferrioxamine B and analogs and homologs thereof beginning with O-protected, N-protected hydroxylamine, which is N-alkylated to produce a protected N-4-cyanoalkylhydroxylamine which is acylated with a suitable anhydride. The resulting half-acid amide is subjected to a series of high yield condensations and reductions which vide desferrioxamine B in high overall yield. Alternatively, polyether analogs of desferrioxamine B can be prepared by reacting an activated polyether with the O-protected, N-protected hydroxylamine and subjecting the resulting product to a series of similar steps.
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