专利号:US-5057624-A 优先权日:1989-03-31 标 题 :Process for the synthesis of the n-methyl-3,4-dimethoxyphenylethylamine 发明人:CANNATA VINCENZO; TAMERLANI GIANCARLO; ZAGNONI GRAZIANO 权利人:ALFA WASSERMANN SPA 摘要:New process for the synthesis of the N-methyl-3,4-dimetoxyphenylethylamine of formula ##STR1## intermediate in the synthesis of the drug internationally known as verapamil. The process starts from the 3,4-dimethoxybenzaldehyde which, by means of a Darzens condensation, gives an epoxyester that, by alkaline hydrolysis and subsequent decarboxylation, gives the 3,4-dimethoxyphenylacetaldehyde. This aldehyde gives the amine of formula I by reaction with monomethylamine followed by reduction with sodium borohydride.
专利号:WO-2015058868-A1 优先权日:2013-10-25 标题 :Compositions and methods for the treatment of cancer 发明人:JIMENO DOÑAQUE JOSÉ Mª 权利人:PANGAEA BIOTECH S L 摘要:The invention relates to anti-tumor compounds which have been designed to functionally disrupt the cross-talk between AEG-1 and the p65 subunit of NF-κB. Therefore, the invention relates to methods and compositions for the treatment of cancer using the compounds identified in the present invention, as well as compositions adequate for sustained release of the compounds of the invention to be administered to the surgical site after resection of the tumor. The invention also provides methods for the synthesis of the compounds of the invention.
专利号:US-4536599-A 优先权日:1978-08-22 标题:Synthesis of amine derivatives 发明人:MASUKO FUJIO; KATSURA TADASHI 权利人:SUMITOMO CHEMICAL CO 摘要:An amine of the formula, ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are each hydrogen, alkyl or the like and n is 1, 2 or 3, including α-phenyl-β-(p-tolyl)-ethylamine, which is useful as an optically resolving agent, an intermediate of medicines and the like, is effectively produced by a novel process comprising hydrolysis of the corresponding nitrile of the formula, ##STR2## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above, followed by alkali-decomposition of the resulting amide of the formula, ##STR3## wherein R 1 , R 2 , R 3 , R 4 , R 5 and n are the same as above. An amide including the above one is effectively produced by hydrolysis of the corresponding nitrile in the presence of a base and hydrogen peroxide using an organic quaternary ammonium salt and/or a tertiary amine as a catalyst.
专利号:US-7569606-B2 优先权日:2006-01-26 标 题 :Platinum complexes with mononitrile-containing ligands 发明人:XIAO ZEJUN; HAUSHEER FREDERICK H; PETLURU PAVANKUMAR 权利人:BIONUMERIK PHARMACEUTICALS INC 摘要:Disclosed herein are novel platinum-based complexes possessing one nitrile substituent group (mononitrile) covalently-bonded to the platinum, one or more nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA and leaving groups (i.e., L 1 and L 2 )which can be hydrolyzed iii vivo to active species, which can then form coordinate adducts with DNA or RNA at the Guanine or Adenine bases thereof. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as methods of treatment of various types of cancer by the administration of a pharmaceutically-effective dose of said novel platinum complexes.
专利号:US-7893071-B2 优先权日:2001-04-23 标 题 :Synthesis and evaluation of novel phthalimide mimics as anti-angiogenic 发明人:BROWN MILTON L 权利人:UNIV VIRGINIA 摘要:The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R 1 is selected from the group consisting of H, halo, alkyl, haloalkyl, —NH 2 , hydroxy and alkoxy; R 2 is selected from the group consisting of optionally substituted bicyclic, optionally substituted aryl, and R 6 is H, or C 1 -C 8 alkyl; R 19 is optionally substituted aryl; and m is 0-6.
专利号:US-9893302-B2 优先权日:2013-03-06 标 题:Heterocyclic fluorescent dyes and method of production thereof 发明人:GRYKO DANIEL T; GRZYBOWSKI MAREK 权利人:BASF SE 摘要:The invention relates to novel compounds of formula (III) that can be used as heterocyclic dyes of unique structure and properties. These compounds can be obtained in a three-step synthesis from simple substrates. The compounds according to the invention have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the compounds according to the invention are used in organic field effect transistors, organic photovoltaics (solar cells) and photodiodes.
参考文献:10.1016/j.saa.2011.06.039 摘要:Jeyavijayan S, Arivazhagan M. FTIR and FT-Raman spectra, molecular geometry, vibrational assignments, first-order hyperpolarizability, ab initio and DFT calculations for 3,4-dimethoxybenzonitrile. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy. 2011 Oct;81(1):466–74. doi: 10.1016/j.saa.2011.06.039.