专利号:US-8642766-B2 优先权日:2008-05-05 标题 :Synthesis of (+) cortistatin A and related compounds 发明人:SHENVI RYAN A; GUERRERO CARLOS A; SHI JUN; LI CHUANG-CHUANG; BARAN PHIL S 权利人:SHENVI RYAN A; GUERRERO CARLOS A; SHI JUN; LI CHUANG-CHUANG; BARAN PHIL S 摘要:An in vitro synthesis of (+) cortistatin A from readily available precursors is disclosed, as are the syntheses of related 17-aryl substituted compounds, the 17-aryl substituted compounds themselves and novel compounds useful in their preparation.
专利号:US-6388083-B2 优先权日:2000-07-07 标题 :Process for the synthesis of (2S)-phenyl-3-piperidone 发明人:LEE JAEMOON; ASKIN DAVID; HOANG THOA 权利人:MERCK & CO INC 摘要:The present invention is concerned with novel processes for the preparation of (2S)-phenyl-3-piperidone. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
专利号:US-8383810-B2 优先权日:2004-12-20 标题:Process for the synthesis of azetidinones 发明人:THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 权利人:MERCK SHARP & DOHME; THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L 摘要:A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.
专利号:US-2023183246-A1 优先权日:2020-05-19 标题 :Continuous flow sonogashira coupling synthesis method 发明人:THOMPSON DAVID HARLEY; SINTIM HERMAN O; QI QINGQING; BIYANI SHRUTI 权利人:PURDUE RESEARCH FOUNDATION 摘要:The present disclosure relates to a telescoped continuous flow Sonogashira coupling synthesis for some lead compounds to support in vivo studies and pre-clinical evaluation. The application of high throughput tools combined with the telescoped continuous synthesis method can enable an efficient and safe synthesis of compounds of interest involving hazardous coupling reagents such as HATU, while minimizing by-product formation.
专利号:US-9267213-B1 优先权日:2005-03-25 标题:Electrochemical deblocking solution for electrochemical oligomer synthesis on an electrode array 发明人:MAURER KARL; COOPER JOHN J 权利人:CUSTOMARRAY INC 摘要:There is disclosed an electrochemical deblocking solution for use on an electrode microarray. There is further disclosed a method for electrochemical synthesis on an electrode array using the electrochemical deblocking solution. The solution and method are for removing acid-labile protecting groups for synthesis of oligonucleotides, peptides, small molecules, or polymers on a microarray of electrodes while substantially improving isolation of deblocking to active electrodes. The method comprises applying a voltage or a current to at least one electrode of an array of electrodes. The array of electrodes is covered by the electrochemical deblocking solution.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
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合成参考文献
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