📜盐酸普鲁卡因胺置于sodium Hydroxide体系中,用 水 作为反应溶剂,化学反应生成 普鲁卡因胺 参考文献:Synthesis Of Some Low Molecular Weight Derivatives Of Procainamide 标题:Synthesis Of Some Low Molecular Weight Derivatives Of Procainamide 摘要:Abstractlow Molecular Weight Derivatives Of Procainamide,With A Terminal Functional Group Have Been Prepared. The Synthesis And Characterization Of The Succinic Half‐amide Respectively Of N‐(ω‐amino Alkanoyl)Derivatives Of The Parent Drug Are Reported. DOI:10.1002/bscb.19840930610
专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
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-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-5516891-A 优先权日:1992-06-16 标题:Liquid phase synthesis of peptides and peptide derivatives 发明人:SIWRUK GARY A; EYNON JOHN S 权利人:KINERTON LTD 摘要:PCT No. PCT/US93/05783 Sec. 371 Date May 25, 1994 Sec. 102(e) Date May 25, 1994 PCT Filed Jun. 16, 1993 PCT Pub. No. WO93/25571 PCT Pub. Date Dec. 23, 1993.A liquid phase peptide synthetic method which uses (1) Fmoc as the protecting group for the non-side chain amino functionality, (2) ammonia, a primary or secondary amine to remove the Fmoc protecting group, and (3) substituted carbodiimide as the coupling agent for the C to N synthesis of peptides or peptide derivatives in a proper organic solvent.
专利号:US-2017348280-A1 优先权日:2016-06-06 标题 :Counteracting the inhibition of collagen synthesis by select calcium and sodium channel blockers using ascorbic acid and ascorbyl palmitate 发明人:RATH MATTHIAS W; NIEDZWIECKI ALEKSANDRA; IVANOV VADIM O; IVANOVA SVETLANA V 权利人:RATH MATTHIAS W; NIEDZWIECKI ALEKSANDRA; IVANOV VADIM O; IVANOVA SVETLANA V 摘要:A therapeutic use of ascorbyl palmitate, ascorbic acid and/or derivatives thereof to reverse or counter the adverse effects of channel blockers in the medical management of cardiovascular disease in a subject is presented. Effects of select Na- and Ca-channel blockers on collagen synthesis and deposition were evaluated in cultured human dermal fibroblasts and aortic smooth muscle cells by immunoassay. Ca and Na-channel blockers inhibited the synthesis of collagen type I and collagen type IV, the basic molecules of vascular wall stability. The inhibitory effects of the calcium and sodium channel blockers on collagen synthesis was reversed by introducing ascorbic acid and/or ascorbyl palmitate. It can be concluded that calcium and sodium channel blockers have a direct inhibitory effect on collagen synthesis, favoring the instability of the vascular wall and the progression of cardiovascular disease, an effect that is mitigated by treatment with, ascorbyl palmitate, ascorbic acid and or derivatives thereof.
专利号:US-2008300418-A1 优先权日:2004-11-08 标 题:Synthesis of Cardiolipin Analogues and Uses Thereof 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.