专利号:US-4749806-A 优先权日:1984-12-28 标题:Process for the synthesis of isocyanates and of isocyanate derivatives 发明人:TKATCHENKO IGOR; JAOUHARI RABIH; BONNET MICHEL; DAWKINS GORDON; LECOLIER SERGE 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The present invention relates to a process for the synthesis of isocyanates and of isocyanate derivatives. Isocyanates are obtained by reacting an organic halide with a metal cyanate in an organic medium in the presence of a catalyst consisting of a complex of nickel with at least one organic ligand, in which complex the nickel is in the zero oxidation state. A carbamate or a urea, respectively, are obtained by a subsequent reaction with a hydroxy compound or a primary or secondary amine. Isocyanates and their derivatives are used especially either as refined synthesis agents for the production of pesticides and medications, or as monomers or comonomers for the preparation of many macromolecular compounds.
专利号:US-5569786-A 优先权日:1987-01-06 标 题 :Isolation, structural elucidation and synthesis of novel antineoplastic substances denominated 'combretastatins' 发明人:PETTIT GEORGE R; SINGH SHEO B 权利人:UNIV ARIZONA 摘要:New antineoplastic substances have been isolated, structurally elucidated and synthesized having a general structural formula of: (I) or H or OCH3; or R1R2 is -OCH2O-; R3 is H or OH; and R4 is OH or OCH3. These substances have been denominated 'combretastatin A-1, -A-2, -A-3, -B-1, -B-2, -B-3 and -B-4'. preparation containing the substances and methods of treating a host inflicted with a neoplastic growth with the preparation is described.
专利号:US-2007275962-A1 优先权日:2003-09-10 标 题:Heterobicyclic Compounds as Pharmaceutically Active Agents 发明人:KOUL ANIL; KLEBL BERT; MULLER GERHARD; MISSIO ANDREA; SCHWAB WILFRIED; HAFENBRADL DORIS; NEUMANN LARS; SOMMER MARC-NICOLA; MULLER STEFAN; HOPPE EDMUND; FREISLEBEN ACHIM; BACKES ALEXANDER; HARTUNG CHRISTIAN; FELBER BEATRICE; ZECH BIRGIT; ENGKVIST OLA; KERI GYORGY; ORFI LASZLO; BANHEGYI PETER; GREFF ZOLTAN; HORVATH ZOLTAN; VARGA ZOLTAN; MARKO PETER; PATO JANOS; SZABADKAI ISTVAN; SZEKELYHID ZSOLT; WACZEK FRIGYES 权利人:GPC BIOTECH AG 摘要:Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.
专利号:EP-1200395-B1 优先权日:1999-07-28 标 题:Urea derivatives as inhibitors of ccr-3 receptor 发明人:PADIA JANAK; HOCKER MICHAEL D; OHASHI HIROSHI; NISHITOBA TSUYOSHI; SAWA EIJI 权利人:KIRIN BREWERY 摘要:Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.
专利号:US-4709087-A 优先权日:1984-12-28 标题:Process for the synthesis of isocyanates and of isocyanate derivatives
专利号:US-6054464-A 优先权日:1996-02-23 标题:Azabicyclic esters of carbamic acids useful in therapy 发明人:MACOR JOHN; WU EDWIN 权利人:ASTRA AB 摘要:A compound of formula ##STR1## X is O or S; Y is O or S; G and D are independently nitrogen or carbon with the proviso that no more than one of G, D, or E is nitrogen; E is N or C--R 4 ; R 1 is hydrogen or methyl; R 2 is hydrogen or fluoro; R 3 is hydrogen, halogen, C 1 to C 3 alkyl, --OR 5 , --CN, --CONH 2 , --CO 2 R 5 , --NR 5 R 6 or phenyl optionally substituted with one to three of the following substituents: halogen, C 1 to C 3 alkyl, --NO 2 , --CN, or --OCH 3 ; R 4 is hydrogen, halogen, C 1 to C 3 alkyl, --OR 5 , --CN, --CONH 2 , --CO 2 R 5 , --NR 5 R 6 or phenyl optionally substituted with one to three of the following substituents: halogen, C 1 to C 3 alkyl, --NO 2 , --CN, or --OCH 3 ; n or R 2 and R 3 or R 3 and R 4 may together represent a fused phenyl ring optionally substituted with one or two of the following substituents: halogen, C 1 to C 3 alkyl, --NO 2 , --CN, or --OCH 3 ; R 5 and R 6 are independently hydrogen or C 1 to C 3 alkyl; n or an enantiomer thereof, and pharmaceutically acceptable salts thereof, processes for preparing the, compositions containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders, as well as intermediates and use of intermediates in synthesis.
参考标题:1-Propanephosphonic Acid Cyclic Anhydride (T3P) As An Efficient Promoter For The Lossen Rearrangement: Application To The Synthesis Of Urea And Carbamate Derivatives 作者:Vommina Sureshbabu,Basavalingappa Vasantha,Hosahalli Hemantha |发布日期:2010.9 摘要:The Synthesis Of Hydroxamic Acids Starting From Carboxylic Acids Employing 1-Propanephosphonic Acid Cyclic Anhydride (T3P) Activation Is Described. Application Of Ultrasonication Accelerates This Conversion. Further, The T3P Has Also Been Employed To Activate The Hydroxamates, Leading To Isocyanates Via The Lossen Rearrangement. The Isocyanates Were Trapped With Suitable Nucleophiles To Afford The
合成参考文献
摘要:Merino, P., Science of Synthesis, (2010) 45, 137. 摘要:Ibrahim, H., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 180.