(R)-(+)-苯乙醇腈置于咪唑,4-二甲氨基吡啶,Zinc(II) Tetrahydroborate体系中,用 乙醚 用作溶剂,化学反应 1.0H,反应生成(1R,2S)-2-氨基-1,2-二苯基乙醇 参考文献:Applications Of Optically Active Aryl Cyanohydrins In The Synthesis Of α-Hydroxy Aldehydes,α-Hydroxy Ketones And β-Hydroxy Amines 标题:Applications Of Optically Active Aryl Cyanohydrins In The Synthesis Of α-Hydroxy Aldehydes,α-Hydroxy Ketones And β-Hydroxy Amines 摘要:从芳基醛中制备的高光学纯度氰基卤素可转化为 α-羟基醛,β-羟基酮和β-羟基胺,且无任何外消旋化现象,在新引入的立体中心处,赤式二对映异构体通常具有非常好的立体选择性(90%). Doi:10.1071/ch9902045
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:EP-1730108-B1 优先权日:2004-03-18 标 题:Stereoselective synthesis of vitamin d analogues 发明人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN 权利人:LEO PHARMA AS 摘要:The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.
专利号:EP-1735276-B1 优先权日:2004-04-02 标题:Novel method for the preparation of intermediates useful for the synthesis of vitamin d analogues 发明人:HANSEN ERIK TORNGAARD; SABROE THOMAS PETER; CALVERLEY MARTIN JOHN; PEDERSEN HENRIK; DEUSSEN HEINZ-JOSEF WILHELM 权利人:LEO PHARMA AS 摘要:The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making calcipotriol or calcipotriol monohydrate.
专利号:US-8759555-B2 优先权日:2004-03-18 标 题:Stereoselective synthesis of vitamin D analogues 发明人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN 权利人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN; LEO PHARMA AS 摘要:The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.
专利号:US-6509506-B1 优先权日:1997-05-21 标 题 :Two step synthesis of D- and L- α-amino acids and D- and L- α-amino aldehydes 发明人:SHARPLESS K BARRY; LI GUIGEN 权利人:SCRIPPS RESEARCH INST 摘要:D- and L- α-amino acids and D- and L-α-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively, divalent ligands are preferred over monovalent ligands because of their enhanced regio-and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant β-hydoxycarbamate is deprotected to yield the corresponding β-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant β-hydroxysulfonamide is deprotected to yield the corresponding β-hydroxyamine. The resultant β-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L- α-amino acid or D- and L-α-amino aldehyde.
专利号:WO-2025104679-A1 优先权日:2023-11-16 标题 :Processes for making intermediates for isoindolinone inhibitors of the mdm2-p53 interaction having anticancer activity 发明人:SHAKYA SAGAR; JOHNSON MATT; WONG NICHOLAS; BODHURI PRABHUDAS; DAVAR NIPUN 权利人:OTSUKA PHARMA CO LTD 摘要:The present disclosure relates to processes for preparing synthetic intermediates for the synthesis of isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity.
参考标题:Pcn Pincer Palladium(II) Complex Catalyzed Enantioselective Hydrophosphination Of Enones: Synthesis Of Pyridine-Functionalized Chiral Phosphine Oxides As NcSp3O Pincer Preligands 作者:Xin-Qi Hao,Juan-Juan Huang,Tao Wang,Jing Lv,Jun-Fang Gong,Mao-Ping Song |发布日期:2014.10.17 摘要:A Series Of Chiral Pcn Pincer Pd(II) Complexes Vi-Xiii With Aryl-Based Aminophosphine-Imidazoline Or Phosphinite-Imidazoline Ligands Were Synthesized And Characterized. They Were Examined As Enantioselective Catalysts For The Hydrophosphination Of Enones. Among Them, Complex Ix, Which Features A Ph2Po Donor As Well As An Imidazoline Donor With (4S)-Phenyl And N-Tol-P Groups, Was Found To Be The Optimal
合成参考文献
参考文献:10.1055/s-0029-1216920 摘要:Li G, Carlson LJ, Sagamanova IK, Slafer BW, Hsung RP, Gilardi C, Sklenicka HM, Sydroenko N. A Stereodivergent Approach for Accessing Both C2,8a-Syn and C2,8a-Anti Relative Stereochemical Manifolds in the Lepadin Family via a TiCL(4)-Promoted Aza-[3 + 3] Annulation. Synthesis (Stuttg). 2009 Sep 01;2009(17):2905.