专利号:WO-2023019298-A1 优先权日:2021-08-20 标 题:Improved method of synthesis of 1-(3',4'-methylene dioxyphenyl)-2-(methylamino) propane (mdma) 发明人:O'MALLEY WILLIAM IAN; WYNNE PAUL MICHAEL 权利人:MIND MEDICINE AUSTRALIA LTD 摘要:The present invention relates to an improved method of synthesis of 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA) that is of sufficient purity that it can be used for pharmaceutical applications. In particular the present invention provides a method of synthesising MDMA comprising the steps of (a) condensation of piperonal and nitroethane in the presence of a catalysing base to form 1-(3',4'-methylenedioxyphenyl)-2-nitroprop-1-ene (MDP-2-nitropropene), (b) oxidative hydrolysis of MDP-2-nitropropene to form 1-(3',4'methylenedioxyphenyl)-propan-2-one (MDP2P), and (c) reductive amination of MDP2P to 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA).
专利号:WO-2012100419-A1 优先权日:2011-01-26 标 题 :Process for synthesis of 3-(n,n-disubstituted-amino)-2- substituted acrylate 发明人:GU HAINING; LI XIAOLING; ZHANG PENGFEI; ZHANG XIKUN; CHEN LIANG 权利人:HANGZHOU GREAT FOREST BIOMEDICAL LTD; GU HAINING; LI XIAOLING; ZHANG PENGFEI; ZHANG XIKUN; CHEN LIANG 摘要:Disclosed is a process for synthesis of 3-(N,N-disubstituted-amino)-2-substituted acrylate, which comprises carrying out amine-substitution reaction and elimination reaction for 2-substituted formylacetate alkali metal salt represented by formula (III) and amine complex represented by formula (II) in organic solvent 1 to obtain 3-(N,N-disubstituted-amino)-2-substituted acrylate represented by formula (I). The process uses N,N-disubstituted amine and carbon dioxide, or a liquid complex obtained by N,N-disubstituted amine and carbon dioxide as raw material, thereby it doesn't produce a side product influencing environment. The process has the advantages of reacting simply and operating easily.
专利号:WO-2008134923-A1 优先权日:2007-04-28 标题 :A preparation method of thiol derivative as side chain intermediate for synthesis of carbapenem derivative 发明人:CAI JIANPING; FAN ENHAI 权利人:ZHEJIANG NEXCHEM PHARMACEUTICA; CAI JIANPING; FAN ENHAI 摘要:A preparation method of thiol derivative as side chain intermediate for synthesis of carbapenem derivative. The method is starting with trans-4-hydroxy-L-proline derivative as starting material, following by one-pot method that 2-carbonyl group is protected, 4-hydroxy is protected and 2-postion is substituted to obtain 2-amide proline derivative, then 4-postion is substituted and 4-postion is hydrolyzed in the presence of base to obtain thiol side chain derivative as important intermediate for Meropenem. The present method is simple, without separating intermediates, with high yield and easy to operate and has advantages over the prior patent methods. It is suitable for industrial production.
专利号:US-2024025939-A1 优先权日:2020-03-06 标 题:High sequence fidelity nucleic acid synthesis and assembly 发明人:POTTER ROBERT; NETUSCHIL NIKOLAI 权利人:LIFE TECHNOLOGIES CORP; THERMO FISHER SCIENT GENEART GMBH 摘要:The present disclosure generally relates to compositions and methods for the synthesis of nucleic acid molecules with low error rates. Provided, as examples, are compositions and methods for high throughput synthesis and assembly of nucleic acid molecules, in many instances, with high sequence fidelity. In many instances, thermostable mismatch recognition proteins (e.g., thermostable mismatch binding protein, thermostable mismatch endonucleases) will be present in compositions and use methods provided.
专利号:WO-2012089181-A1 优先权日:2010-12-30 标题 :O-substituted (2r,3r)-3-(3-hydroxyphenyl)-2-methyl-4-pentenoic acids and a method of obtaining the same 发明人:VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF 权利人:ZENTIVA KS; VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF 摘要:The compounds of general formula II are new and represent important intermediates in the synthesis of tapentadol. In the synthesis of tapentadol of formula I and its pharmaceutically acceptable salts, O-protected (2R,3R)-acids of general formula II, in step A, are reacted in an inert organic solvent with an activating agent, optionally in presence of a catalyst or a base; in step B, the obtained compounds of general formula V, wherein R has the above mentioned meaning and X stands for chlorine or alkoxycarbonyloxyl group O-CO-OR 1 or pivaloyloxyl O-CO-t-Bu group, wherein R 1 is methyl or ethyl, are reacted with dimethylamine or its salts optionally in presence of a base; in step C, the obtained N, N-dimethylamides of general formula VI, wherein R has the above mentioned meaning, are reduced by means of hydride agents in a suitable solvent; in step D, the produced alkeneamines of general formula VII, wherein R has the above mentioned meaning, are hydrogenated on a metal catalysts in a suitable solvent; and, finally, in step E, the produced alkaneamines of general formula VIII, wherein R has the above mentioned meaning, are O-dealkylated by means of dealkylating agents, and, if required, the obtained tapentadol is converted by the action of a pharmaceutically acceptable acid to respective salts, e.g. hydrochloride.
专利号:WO-2013056547-A1 优先权日:2011-10-22 标题 :Synthesis of a group of hydantoin derivatives and use thereof 发明人:CHEN DEGUI 权利人:CHEN DEGUI 摘要:Provided in the present invention are the pharmaceutical composition, synthesis procedure and medicinal use of a group of HYDANTOIN derivatives. Since these compounds have an inhibiting effect on an androgen receptor, the compounds can be used to treat prostate cancer and other diseases and physiological disorders related to androgen receptor activity.
摘要:Ipaktschi, J.; Saidi, M. R., Science of Synthesis Knowledge Updates, (2012) 4, 446. 摘要:Tomás-Gamasa, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 27.