专利号:US-8901352-B2 优先权日:2011-01-13 标题 :Method for the synthesis of rasagiline 发明人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN 权利人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN; NOBEL ILAÇ SANAYII VE TICARET A S 摘要:We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.
专利号:US-7786156-B2 优先权日:2004-01-28 标 题 :Synthesis methods and intermediates for the manufacture of Rizatriptan 发明人:MARTIN PIERRE; BERENS ULRICH; BOUDIER ANDREAS; DOSENBACH OLIVER 权利人:RATIOPHARM GMBH 摘要:The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], n nor a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B]n n nwherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent.n n In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.
专利号:US-2008312430-A1 优先权日:2004-10-20 标题:Method of Preparing or Synthesizing Polyazamacrocycle Derivatives 发明人:CIHELNIK SIMON; DROZ LADISLAV; SRAMEK MARTIN 权利人:THERAPHARM GMBH 摘要:The present invention relates to novel processes for the synthesis of polyazamacrocycle derivatives. Furthermore, the present invention relates to novel polyazamacrocycle derivatives as well as novel intermediates for the synthesis of said polyazamacrocycle derivatives.
专利号:US-11583842-B2 优先权日:2019-07-24 标题 :Zwitterionic catalysts for (trans)esterification: application in fluoroindole-derivatives and biodiesel synthesis 发明人:YEUNG YING-YEUNG; LAM YING-PONG; KE ZHIHAI; WANG XINYAN; TAN FEI; NG WING-HIN; TSE YING-LUNG STEVE 权利人:UNIV HONG KONG CHINESE 摘要:An amide/iminium zwitterion catalyst has a catalyst pocket size that promotes transesterification and dehydrative esterification. The amide/iminium zwitterions are easily prepared by reacting aziridines with aminopyridines. The reaction can be applied a wide variety of esterification processes including the large-scale synthesis of biodiesel. The amide/iminium zwitterions allow the avoidance of strongly basic or acidic condition and avoidance of metal contamination in the products. Reactions are carried out at ambient or only modestly elevated temperatures. The amide/iminium zwitterion catalyst is easily recycled and reactions proceed in high to quantitative yields.
专利号:US-11498846-B2 优先权日:2020-07-15 标 题 :Method for synthesis of solvent-free lithium boron cluster based salts 发明人:TUTUSAUS OSCAR; MOHTADI RANA 权利人:TOYOTA ENG & MFG NORTH AMERICA 摘要:An effectively solvent-free alkali metal or alkali earth metal closo-borate salt is prepared in the presence of a non-aqueous solvent where the solvent can be removed to levels below one mole percent of the salt. The process involves the exchange of cations with a closo-borate anion via an acid-base process or a metathesis process. The solvent is removed from the alkali metal or alkali earth metal closo-borate salt by heating. The temperature can be greater than the melting point of the salt but lower than temperatures where decomposition occurs.
专利号:US-7208604-B2 优先权日:1999-12-06 标题 :Methods for the synthesis of alfentanil, sufentanil, and remifentanil 发明人:MATHEW JACOB; KILLGORE J KENDALL 权利人:MALLINCKRODT INC 摘要:Synthetic pathways are disclosed for synthesizing derivatives or analogs of fentanyl. Specifically set out are pathways for synthesizing alfentanil, sufentanil and remifentanil. The disclosed methods require fewer steps and produce a greater yield of product than methods reported in the prior art.