专利号:US-7452994-B2 优先权日:2001-09-12 标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 发明人:MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN 权利人:ANORMED INC 摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.
专利号:US-2023278959-A1 优先权日:2020-05-04 标题:Synthesis of Optically Active Indoline Derivatives Via Ruthenium(II)-Catalyzed Enantioselective C-H Functionalization 发明人:CUI XIN; LI ZHONG-YUAN; CHAMINDA LAKMAL HETTI HANDI 权利人:UNIV MISSISSIPPI STATE 摘要:Provided herein are a method of Ru(II)-catalyzed enantioselective synthesis of a cyclic compound and cyclic compounds formed therefrom. The method includes providing a precursor compound having an unfunctionalized C—H bond and activating the unfunctionalized C—H bond by reacting the precursor compound in the presence of co-catalysts including a Ru(II) arene complex and a chiral transient directing group (CTDG).
专利号:US-5574186-A 优先权日:1995-03-08 标 题 :Enantioselective synthesis of cyclic amino alcohols 发明人:BOUDREAU CHARLES; TILLYER RICHARD D; TSCHAEN DAVID M 权利人:MERCK & CO INC 摘要:There is disclosed a novel process for the enantioselective synthesis of chiral amino alcohols from keto oxime ethers, which are derived from cyclic ketones, via catalytic asymmetric reduction, employing oxazaborolidine-borane complex (OAB-BH 3 ). In this catalytic reduction process two chiral centers are created in a single step with high levels of stereoselectivity.
专利号:US-8084630-B2 优先权日:2007-05-31 标 题 :Process for the synthesis of ramelteon and its intermediates 发明人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL 权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL; TEVA PHARMA 摘要:The present invention provides processes and intermediates for the synthesis of ramelteon.
专利号:US-8759584-B2 优先权日:2007-12-14 标 题 :Synthesis of biguanidines and triazines, and biguanidino-aluminium complexes as intermediates 发明人:FORD MARK JAMES 权利人:FORD MARK JAMES; BAYER CROPSCIENCE AG 摘要:Compounds of formula (I) or salts thereof, n nin which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X and Y are defined as in claim 1 , can be prepared by a process characterized in that a compound of the formula (II) or a salt thereof,n n nis reacted to a compound of the formula (III) or a salt thereof,n n nand an aluminium(III) source, optionally, in the presence of a protic additive or solvent selected from the group consisting of alcohols or amines.n n The compounds (I) are suitable to be used for the preparation of heterocyclic compounds corresponding to (I) where the group Al(X)(Y) is replaced with an optionally substituted carbon atom, or s-triazine derivatives thereof.
专利号:US-2009281176-A1 优先权日:2007-11-01 标题:Process for the synthesis of ramelteon and its intermediates 发明人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; PATEL RAKESH; JADAV ARPAN M 权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; PATEL RAKESH; JADAV ARPAN M 摘要:A process for the preparation of ramelteon and intermediates useful in the process. The process suitable for industrial scale provides increased yield and/or greater purity with fewer process steps.