专利号:US-7361773-B2 优先权日:2002-03-12 标题 :Preparation of N1-(2'-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines 发明人:CHAN ANITA WAI-YIN; FEIGELSON GREGG BRIAN; ZELDIS JOSEPH; JIRKOVSKY IVO LADISLAV 权利人:WYETH CORP 摘要:A process for making a compound of the formula comprising dialkylating a benzodioxane aniline
专利号:US-4782061-A 优先权日:1984-12-21 标题:Method of treating psychotropic conditions employing substituted piperazine compounds 发明人:KRUSE CORNELIS G; VAN DER HEYDEN JOHANNES A M; VAN WIJNGAARDEN INEKE; HARTOG JAN; OLIVIER BEREND 权利人:DUPHAR INT RES 摘要:The invention relates to a group of new bicyclic heteroarylpiperazine derivatives of formula 1. It was found that these compounds have interesting psychotropic in particular anti-psychotic properties. The compounds can be prepared according to methods known for the synthesis of analogous compounds.
专利号:WO-2006135544-A1 优先权日:2005-06-10 标 题 :SYNTHESIS OF 11-(4[-(2-HYDROXYETHOXY)ETHYL]-PIPERAZINYL)-DIBENZO[b,f][1,4]THIAZEPINE AND ITS FUMARATE SALT 发明人:BUENGER GREG STEVEN; ALEXANDER ANATOLY 权利人:CAMBREX CHARLES CITY INC; BUENGER GREG STEVEN; ALEXANDER ANATOLY 摘要:The invention is directed a method for synthesizing l l-(4-[2-(2- hydroxyethoxy)ethyl]-piperazinyl)-dibenzo[b,f] [l,4]thiazepine (quetiapine) and for recovering quetiapine as its fumarate salt in which dibenzo[b,f][l,4]thiazepine- l l(10H)one is chlorinated in the presence of a trialkyl amine base using a slight molar excess of phosphorous oxychloride to produce l l-chloro-dibenzo[b,f] [l,4]thiazepine which then is alkylated with piperazine to l l-piperazinyldibenzo[b,f] [l,4]thiazepine, which finally is alkylated with 2-(2-chloroethoxy)ethanol.
专利号:US-6784294-B2 优先权日:2002-03-12 标题 :Preparation of N1-(2′-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines 发明人:CHAN ANITA WAI-YIN; FEIGELSON GREGG BRIAN; ZELDIS JOSEPH; JIRKOVSKY IVO 权利人:WYETH CORP 摘要:A process for making an N1-(2′-pyridyl)-1,2-alkanediamine sulfamic acid of formula II by reacting a compound of formula I with NH 2 R′ n wherein R and R′ are as defined in the specification. The invention also includes the compound of formula II, and optical isomers thereof. The compound of formula II is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT 1A receptor.
专利号:US-6960601-B2 优先权日:2001-09-24 标题 :Preparation and use of imidazole derivatives for treatment of obesity 发明人:SMITH ROGER A; O'CONNOR STEPHEN J; WIRTZ STEPHAN-NICHOLAS; WONG WAI C; CHOI SOONGYU; KLUENDER HAROLD C E; SU NING; WANG GAN; ACHEBE FURAHI; YING SHIHONG 权利人:BAYER PHARMACEUTICALS CORP 摘要:This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
专利号:JP-2005526088-A 优先权日:2002-03-12 标 题 :Synthesis of N1- (2'-pyridyl) -1,2-alkanediaminesulfamic acid and its use in the synthesis of biologically active piperazine
摘要:Arzneimittel-Forschung. Drug Research., 4(649), 1954 [] 摘要:WILLIAMS RT; 2ND ED, CHAPMAN AND HALL, 614 (1959) 摘要:Aronson, C.E. (ed.). Veterinary Pharmaceuticals & Biologicals, 1980-1981. Media, Pa.: Harwal Publishing Co., 1980., p. 19/15 摘要:Lide, DR (ed.). CRC Handbook of Chemistry and Physics. 71st ed. Boca Raton, FL: CRC Press Inc., 1990-1991., p. 3-405 摘要:Association of Official Analytical Chemists. Official Methods of Analysis. 10th ed. and supplements. Washington, DC: Association of Official Analytical Chemists, 1965. New editions through 13th ed. plus supplements, 1982., p. 13/663 38.211