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:US-8309716-B2 优先权日:2005-07-29 标题 :Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis 发明人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J 权利人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J; PFIZER 摘要:This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.
专利号:US-7390931-B2 优先权日:2004-04-01 标 题:Preparation of P-chirogenic phospholanes and their use in asymmetric synthesis 发明人:HOGE II GARRETT STEWART 权利人:PFIZER 摘要:Materials and methods for preparing P-chirogenic monophospholanes and bisphospholanes are disclosed. The methods employ stereoselective cyclization to generate the phospholane rings followed by pyramidal inversion to access a variety of P-chirogenic phospholanes. When bound to transition metals such as rhodium, the disclosed P-chirogenic phospholanes may be used as catalysts in asymmetric synthesis of valuable pharmaceutical chemical entities, including pregabalin.
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-9126906-B2 优先权日:2012-02-21 标 题:Asymmetric synthetic processes for the preparation of aminosulfone compounds 发明人:CONNOLLY TERRENCE J; RUCHELMAN ALEXANDER L; LEONG WILLIAM W 权利人:CELGENE CORP 摘要:Processes for synthesizing aminosulfone compounds are provided. The processes provided herein utilize asymmetric reduction reactions, e.g., asymmetric hydrogenation, of protected or unprotected enamine or ketone substrates. Aminosulfone compounds obtained using methods provided herein are useful in production or synthesis of sulfone group containing isoindoline based compounds.
专利号:EP-1595887-B1 优先权日:2004-05-06 标 题:Chiral C2-symmetric biphenyls, preparation thereof as well as metal complexes containing these ligands and the use as catalysts in chirogene synthesis 发明人:PESCHKO CHRISTIAN DR; POPP ALFRED DR; STOHRER JUERGEN DR 权利人:CONSORTIUM ELEKTROCHEM IND 摘要:Chiral symmetric biphenyl compounds (I), are new. Chiral symmetric biphenyl compounds of formula (I), are new. R1>, R2>H; R3>, R4>H, F, 1-10C alkyl or CF3; Y : divalent radical (CR9>2, CHR9>, (cis)-CH=CH, CR9>2CR10>2, CHR9>CHR10>, 1,2-arylene, CHR9>-O-CHR10> or CR9>2-O-CR10>2; Q : F, Cl, Br, I, CN, NO2, -NR7>R8>, -NR7>OR8>, -OR7>, -C(O)R7>, SR7>, -SO3R7>, -C(O)OR7>, -C(O)NR7>R8>, -OC(O)R7> or -NR7>C(O)R8>; R9>, R10>1-10C alkyl (mono, poly or unsubstituted (all optionally substituted by Q)), 3-10C cycloalkyl, 2-10C alkenyl, 4-10C cycloalkenyl, 2-10C alkynyl, 6-15C aryl, 1-15C heteroaryl, Q or H; R7>, R8>R9>; and R5>, R6>3-10C cycloalkyls (mono, poly or unsubstituted (all optionally substituted by Q)), 4-10C cycloalkenyl, 5-15C aryls or 1-15C heteroaryl. Independent claims are also included for: (1) the preparation of (I); (2) a biphenyl compound of formula (II); (3) preparing enantiomerically pure or enantiomerically enriched (II) by fractional crystallization of (II) in the presence of a complexing chiral compound; (4) preparing enantiomerically pure or enantiomerically enriched (I) by converting (II) into chiral palladium complexes; (5) a phosphine compound of formula (IIIa) and benzyl iodide compound of formula (IIIb); (6) a phenyl compound of formula (IV); (7) a complex (A) comprising a ligand of (I) and a metallic center; (8) preparing (A) comprising reacting (I) with a precursor containing the metallic center, in the presence of an organic solvent; an organic synthesis in which a metal complex catalyst is employed, where the improvement comprises selecting (A) as a catalyst; and (9) hydrogenating C=O, C=C or C=N groups in a substrate comprising hydrogenating in the presence of (A). X : halo. Provided that in (IV), CR3>2-Y-CR4>2 cannot be (CH2)3, when X is Br. [Image] [Image].
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