异丁酸异丁酯置于盐酸体系中,用 丙酮 作为反应溶剂,化学反应 4.0H,以87%的收率获得产物异丁酸 参考文献: Processes For Producing Carboxylic Acids[fr] Procédés De Production D'Acides Carboxyliques 标题: Processes For Producing Carboxylic Acids[fr] Procédés De Production D'Acides Carboxyliques 摘要:公开了从有机酯制备羧酸的过程,该过程包括在酸催化剂和均相溶剂存在下将酯与水接触,以形成羧酸的有效条件.均相溶剂以足够量存在,以形成包括酯,水和均相溶剂的单相反应混合物.均相溶剂可以选择自乙腈,二甲基亚砜和1,4-二氧六环.
专利号:WO-2013138200-A1 优先权日:2012-03-13 标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof 发明人:FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER 权利人:UNIV HOWARD 摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.
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-2008119665-A1 优先权日:2004-09-07 标 题:Process for the Synthesis of Zirconium Carboxylates 发明人:FRITZ PETER; BOLT HEINZ; SCHERSCHLICHT KARL-HEINZ; MOSA FUAD; ALI TALAL K; AL-OTAIBI SULTAN 权利人:FRITZ PETER; BOLT HEINZ; SCHERSCHLICHT KARL-HEINZ; MOSA FUAD; ALI TALAL K; AL-OTAIBI SULTAN 摘要:A process for the synthesis of zirconium tetra carboxylates is disclosed. To overcome the disadvantageous characteristics of the currently used production process, which include highly corrosive starting substances and products, and complex removal of HCl, ZrCI 4 is suspended in an apolar solvent and reacted with the anhydride of an organic acid. The sole products of this reaction are slightly corrosive Zr tetra carboxylate and an organic acid chloride, which is a valuable basic chemical in the chemicals and pharmaceuticals industry. The reactors required for the synthesis need not necessarily consist of glass and/or enamel, but may instead be manufactured from stainless steel, which is cheaper. Apparatuses for the removal and treatment of hydrochloric acid are not necessary.
专利号:US-8293930-B1 优先权日:2004-06-25 标题 :One pot synthesis of taxane derivatives and their conversion to paclitaxel and docetaxel 发明人:NAIDU RAGINA 权利人:NAIDU RAGINA; CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction of protecting the C-7 and C-10 positions and attaching a side chain at the C-13 position and subsequently deprotecting the group to form paclitaxel or docetaxel, and taxane intermediates.
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-9376461-B2 优先权日:2011-06-06 标 题:Non-enzymatic synthesis of O-acetyl-ADP-ribose and analogues thereof 发明人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B 权利人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B; GLAXOSMITHKLINE LLC 摘要:Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2′- and 3′-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.
参考文献:10.1007/s11095-011-0516-4 摘要:Ibrahim N, Handa H, Cosset A, Koulintchenko M, Konstantinov Y, Lightowlers RN, Dietrich A, Weber-Lotfi F. DNA delivery to mitochondria: sequence specificity and energy enhancement. Pharm Res. 2011 Nov;28(11):2871–82. doi: 10.1007/s11095-011-0516-4. 参考文献:10.1155/2011/978583 摘要:Houston MA, Augenlicht LH, Heerdt BG. Stable Differences in Intrinsic Mitochondrial Membrane Potential of Tumor Cell Subpopulations Reflect Phenotypic Heterogeneity. International Journal of Cell Biology. 2011;2011():1–11. doi: 10.1155/2011/978583. 参考文献:10.1021/pr2003598 摘要:Le Gall G, Noor SO, Ridgway K, Scovell L, Jamieson C, Johnson IT, Colquhoun IJ, Kemsley EK, Narbad A. Metabolomics of fecal extracts detects altered metabolic activity of gut microbiota in ulcerative colitis and irritable bowel syndrome. J Proteome Res. 2011 Sep 02;10(9):4208–18. doi: 10.1021/pr2003598. 参考文献:10.1016/j.tiv.2005.10.006 摘要:Seeling K, Boguhn J, Strobel E, Dänicke S, Valenta H, Ueberschär KH, Rodehutscord M. On the effects of Fusarium toxin contaminated wheat and wheat chaff on nutrient utilisation and turnover of deoxynivalenol and zearalenone in vitro (Rusitec). Toxicol In Vitro. 2006 Aug;20(5):703–11. doi: 10.1016/j.tiv.2005.10.006.