CAS: 99135-95-2; (3R,4R)-1-Benzyl-3,4-Bis(Diphenylphosphino)Pyrrolidine

该化合物是一种在非对称催化中广泛使用的阳性活性磷离心管,其硬性阳性骨和立体(R,R)配置对过渡性金属催化反应(如氢化和交叉相交)中的对等选择性具有极好的控制作用.二苯基磷(二苯基磷)组提供了很强的电子施药特性,加强了金属-约束和协调,而N苯基子组则提高了有机溶剂的溶解性.这种紧固性脊椎和立体(R,R)配置特别看重其稳定性和可预见性,因为它在产生高抗蛋白性过量方面表现的稳定性和可预见性.其结构设计使其适合于在精确的立体控制下进行制药合成和精细化学生产.

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CAS号90365-74-5 (3S,4S)-1-苄基吡咯烷... | CAS号100-46-9 苄胺 | CAS号75172-31-5 (3R,4R)-3,4-二羟基...

合成工艺路线路线简述

    📜(3S,4S)-1-苄基吡咯烷-3,4-二醇置于三乙胺体系中,用 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 0.5H,反应生成 (+)-N-苄基-(3R,4R)-双(二苯基膦)吡咯烷
    参考文献:Nagel,Ulrich; Kinzel,Elke; Andrade,Juan,Chemische Berichte,1986,Vol. 119,# 11,P. 3326-3343
    标题:Nagel,Ulrich; Kinzel,Elke; Andrade,Juan,Chemische Berichte,1986,Vol. 119,# 11,P. 3326-3343

    海关参考信息

    专利信息


    专利号:US-10745354-B2
    优先权日:2017-11-01
    标题 :Methods for enantioselective allylic alkylation of esters, lactones, and lactams with unactivated allylic alcohols
    发明人:STOLTZ BRIAN M; NGAMNITHIPORN AURAPAT; JETTE CARINA I; BACHMAN SHOSHANA; VIRGIL SCOTT C; LACKNER SEBASTIAN
    权利人:CALIFORNIA INST OF TECHN
    摘要:The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic α-quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation.

    专利号:US-6380416-B2
    优先权日:1997-06-13
    标题:Asymmetric synthesis catalyzed by transition metal complexes with rigid chiral ligands
    发明人:ZHANG XUMU
    权利人:PENN STATE RES FOUND
    摘要:This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral bidentate phosphine ligands with cyclic ring structures which could be used to restrict conformational flexibility of the ligands and thus the efficiency of chiral transfer can be enhanced through the ligand rigidity.

    专利号:EP-1030854-B1
    优先权日:1997-11-12
    标题 :Catalysts for asymmetric synthesis containing rigid chiral ligands
    发明人:ZHANG XUMU
    权利人:PENN STATE RES FOUND
    摘要:This invention is to develop novel transition metal catalysts for the pratical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral bidentate phosphine ligands with cyclic ring structures which could be used to restrict conformational flexibility of the ligands and thus the efficiency of chiral transfer can be enhanced through the ligand rigidity.

    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-6399787-B1
    优先权日:1997-06-13
    标 题:Catalytic asymmetric hydrogenation, hydroformylation, and hydrovinylation via transition metal catalysts with phosphines and phosphites
    发明人:ZHANG XUMU
    权利人:PENN STATE RES FOUND
    摘要:Novel transition metal catalysts with conformationally rigid chiral phosphines and phosphites are developed for asymmetric carbon-hydrogen and carbon-carbon bond formation. The invention emphasizes synthesis of chiral amines, beta-amino acids and related compounds via catalytic asymmetric hydrogenation based on chiral monodentate and bidentate phosphines with cyclic ring structures. The ligands contain rigid ring structures.

    专利号:US-9403766-B2
    优先权日:2008-01-17
    标 题:Intermediates for producing NEP inhibitors or prodrugs thereof
    发明人:HOOK DAVID; RISS BERNARD; KAUFMANN DANIEL; NAPP MATTHIAS; BAPPERT ERHARD; POLLEUX PHILIPPE; MEDLOCK JONATHAN; ZANOTTI-GEROSA ANTONIO
    权利人:HOOK DAVID; RISS BERNARD; KAUFMANN DANIEL; NAPP MATTHIAS; BAPPERT ERHARD; POLLEUX PHILIPPE; MEDLOCK JONATHAN; ZANOTTI-GEROSA ANTONIO; NOVARTIS AG
    摘要:The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, n nwherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.

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    合成参考文献


    摘要:Friestad, G. K., Science of Synthesis, (2009) 40, 331.
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