专利号:US-2025026768-A1 优先权日:2023-06-30 标题:Method for the synthesis of axially chiral organoboron compounds 发明人:PING YIFAN; CHE CHI-MING 权利人:LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:A highly efficient and atroposelective Rh-catalyzed [2+2+2] cycloaddition for the synthesis of axially chiral aryboron compounds is developed. The reactions of diynes and alkynylborons smoothly occur in an atom-economical manner, affording a variety of C—B atropisomers in excellent yields and enantioselectivities. The protocol features mild conditions, broad substrate scope, and good functional tolerance. The obtained C—B atropisomers show powerful synthetic applications in terms of producing novel chiral phosphine ligands.
专利号:WO-2010048138-A1 优先权日:2008-10-21 标 题 :Synthesis of intermediates useful for the production of certain cgrp inhibitors and intermediates used in such synthesis 发明人:HADDAD NIZAR; KRISHNAMURTHY DHILEEPKUMAR; REEVES DIANA C; SENANAYAKE CHRIS H; TANG WENJUN; YEE NATHAN K 权利人:BOEHRINGER INGELHEIM INT; HADDAD NIZAR; KRISHNAMURTHY DHILEEPKUMAR; REEVES DIANA C; SENANAYAKE CHRIS H; TANG WENJUN; YEE NATHAN K 摘要:A method for making the compound of the formula (I), (IV), (VI), (VII) and (VIII), wherein R 1 is C -1-5 -alkyl, C(O)-O benzyl, C(O)-O- tert .butyl or benzyl; and R 2 is C 1 -C 6 alkyl.
专利号:US-2024308959-A1 优先权日:2021-06-29 标 题:Processes for the preparation of (s)-2-(4-chloro-2-methoxyphenyl)-2-((3 -methoxy-5-(m ethylsulfonyl)phenyl)amino)-1 -(1h-indol-3-yl)ethenone derivatives 发明人:WU KAI; OOST RIK; SCHWEITZER-CHAPUT BERTRAND; ERIKSSON CARL ARNE MAGNUS; COESEMANS ERWIN 权利人:JANSSEN PHARMACEUTICALS INC 摘要:The present invention relates to novel chiral synthesis of mono- or di-substituted indole compounds of formula (I) n n n n n n n n n n n n wherein: n R 1 is H, R 2 is F and R 3 is H or CH 3 , n R 1 is H, CH 3 or F, R 2 is OCH 3 and R 3 is H and n R 1 is H, R 2 is OCH 3 and R 3 is CH 3 , n R 1 is CH 3 , R 2 is F and R 3 is H, n R 1 is CF 3 or OCF 3 , R 2 is H and R 3 is H, n R 1 is OCF 3 , R 2 is OCH 3 and R 3 is H and n R 1 is OCF 3 , R 2 is H and R 3 is CH 3 .
专利号:US-7495123-B2 优先权日:2004-04-05 标 题:Process for the preparation of enantiomerically enriched beta amino acid derivatives 发明人:XIAO YI; SUN YONGKUI; ROSNER THORSTEN; RIVERA NELO R; KRSKA SHANE W; CLAUSEN ANDREW M; ARMSTRONG III JOSEPH D; SPINDLER FELIX; MALAN CHRISTOPHE 权利人:SOLVIAS AG; MERCK & CO INC 摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.
专利号:US-11629137-B2 优先权日:2017-04-24 标 题:Methods of manufacturing of niraparib 发明人:STEWART ALISTAIR; TOTO ANTHONY JOSEPH; CHEN FRANK XING; WU GEORGE 权利人:TESARO INC 摘要:Disclosed herein are methods and processes of preparing niraparib and pharmaceutically acceptable salts thereof, and intermediates and their salts useful for the synthesis of niraparib.
专利号:US-9758499-B2 优先权日:2014-06-12 标 题:Stereo controlled synthesis of (E,Z)-dienals via tandem Rh(I) catalyzed propargyl claisen rearrangement 发明人:VIDHANI DINESH V; KRAFFT MARIE E; ALABUGIN IGOR 权利人:UNIV FLORIDA STATE RES FOUND 摘要:A novel Rh(I)-catalyzed approach to synthesizing functionalized (E,Z) dienal compounds has been developed via tandem transformation where a stereoselective hydrogen transfer follows a propargyl Claisen rearrangement. Z-Stereochemistry of the first double bond suggests the involvement of a six-membered cyclic intermediate whereas the E-stereochemistry of the second double bond stems from the subsequent protodemetallation step giving an (E,Z)-dienal. The reaction may be represented by the following sequence.