专利号:WO-2025119975-A1 优先权日:2023-12-04 标 题:A method for synthesis of harmine 发明人:HETT ROBERT; GRAB HANUSCH; LAGOUTTE ROMAN 权利人:RECONNECT LABS AG 摘要:The invention relates to a method of synthesis of a compound of formula (I), harmine, according to the method comprising a step of transforming the compound of formula (II), into the compound of formula (I). The invention further relates to a compound of formula (II), which is an intermediate in synthesis of harmine according to the present invention.
专利号:US-2025101006-A1 优先权日:2022-01-31 标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents 发明人:BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO 权利人:NOVARTIS AG 摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
专利号:US-11059835-B2 优先权日:2014-08-15 标 题 :Synthesis of cephalosporin compounds 发明人:WALLER DAVID; GAZDA GREGORY; MINDEN ZACHARY; BARTON LISA; LEIGH CLIFTON 权利人:MERCK SHARP & DOHME 摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
专利号:US-2024336649-A1 优先权日:2021-06-21 标 题 :Synthesis of covalent protein dimers that can inhibit myc-driven transcription 发明人:LOAS ANDREI; PENTELUTE BRADLEY L; POMPLUN SEBASTIAN; JBARA MUHAMMAD; SCHISSEL CARLY KATHERINE; RODRIQUEZ JACOB JOSHUA LEE; BUCHWALD STEPHEN LEFFLER; BOIJA ANN; KLEIN ISAAC; HAWKEN SUSANA WILSON; LI CHARLES HAN 权利人:MASSACHUSETTS INST TECHNOLOGY; WHITEHEAD INSTITUTE OF BIOMEDICAL RES 摘要:The disclosure relates to covalent protein dimers of MYC, MAX, and Omomyc; pharmaceutical compositions comprising the covalent protein dimers; methods of making the covalent protein dimers; and methods of treating disorders associated with MYC dysregulation (e.g., cancer) with the covalent protein dimers.
专利号:US-12049470-B2 优先权日:2021-02-01 标 题 :MK2 inhibitors, the synthesis thereof, and intermediates thereto 发明人:RUCHELMAN ALEXANDER L; COOMBS JOHN R; ZHU KEMING; LIM DANIEL; JOE CANDICE LEE; GEORGE DAVID T; ZHENG BIN; LIN DONG 权利人:CELGENE CORP 摘要:The present disclosure provides novel synthetic intermediates useful in the synthesis of MK2 kinase inhibitors.
专利号:US-9650355-B2 优先权日:2013-01-31 标 题 :Method for preparation of justicidin a derivatives of arylnaphthalene lignan structure 发明人:HAM JUNGYEOB; KIM TAE JUNG; KWON HAK CHEOL; JEONG KYU HYUK; SONG JUNGHO; CHUNG BONG CHUL 权利人:KOREA INST SCI & TECH 摘要:The present disclosure relates to a novel method for preparing an arylnaphthalene lignan compound. In synthesis of arylnaphthalene lignan compounds and derivatives according to the present disclosure, a naphthalene backbone may be constructed first and an aryl group may be introduced at the final stage. Through this, various kinds of derivatives that could not be prepared from the existing methods can be synthesized effectively. Further, the synthesis method according to the present disclosure is appropriate for large-scale production.
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