专利号:EP-0791575-A1 优先权日:1996-02-16 标题 :Method of synthesis of a quaternary ammonium salt 发明人:NAKANO SHINJI 权利人:NIPPON PAINT CO LTD 摘要:The present invention provides an improved method of synthesis of a quaternary ammonium salt in which a tertiary amine is reacted with a benzyl halide optionally having on the benzene ring and/or at the α-site one ore more substituent groups inert to the reaction, which method is characterized in that the reaction is carried out in water or in a water-containing organic solvent.
专利号:US-2004101523-A1 优先权日:1989-07-27 标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.
专利号:US-9856205-B2 优先权日:2011-09-28 标 题:Method for the selective production of N-methyl-para-anisidine 发明人:IVANOV YURIY ALEXANDROVICH; BELIAKOV NIKOLAY GRIGORIEVICH 权利人:IVANOV YURIY ALEXANDROVICH; FROLOV ALEXANDER YURIEVICH; BELIAKOV NIKOLAY GRIGORIEVICH; IFOTOP LLC 摘要:The invention “Method for selective synthesis of N-methyl-para-anisidineâ€? relates to chemical technology processes, namely to catalytic alkylation of aromatic amines and nitro compounds. n The invention relates to the method for synthesis of N-methyl-para-anisidine (N-methyl-para-methoxyaniline; N-methyl-para-amino anisole) from para-anisidine (para-amino anisole; para-methoxyaniline) or para-nitro anisole (1-methoxy-4-nitrobenzene) and methanol in the presence of hydrogen or without hydrogen on heterogeneous catalyst. n Proposed method permits to use existing process plants used for obtaining aniline and 14-methylaniline. n The invention purpose is to provide the possibility to produce N-methyl-para-anisidine with purity at least 98% and high output that allows arrangement of highly profitable industry-scale manufacturing process.
专利号:US-9802952-B2 优先权日:2013-07-15 标 题:Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives 发明人:KOPETZKI DANIEL; MCQUADE DAVID TYLER; SEEBERGER PETER H; GILMORE KERRY 权利人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V; MAX-PLANK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V 摘要:The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C 1 -C 5 alcohol.
专利号:US-8106031-B2 优先权日:2006-05-02 标题:Hydrolytically-resistant boron-containing therapeutics and methods of use 发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A 权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:US-4388310-A 优先权日:1982-03-01 标 题:6-Amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids 发明人:CHRISTENSEN BURTON G; DININNO FRANK P; MUTHARD DAVID A; RATCLIFFE RONALD W 权利人:MERCK & CO INC 摘要:Disclosed are 6-amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids (I) which are useful as antibiotics and as intermediates in the synthesis of substituted pen-2-em-3-carboxylic acids: I wherein: R1 is H or acyl; R2 is hydrogen or methoxyl; R3 is alkyl having from 1-6 carbon atoms; phenylalkyl having 7-12 carbon atoms; and cycloalkyl having 3-6 carbon atoms; and R4 is hydrogen, a removable protecting group or a pharmaceutically acceptable salt or ester moiety.
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合成参考文献
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