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    • 5. 发明申请
    • Process for the Production of Asymmetric Transformation Catalysts
    • 不对称转化催化剂生产工艺
    • US20080281106A1
    • 2008-11-13
    • US10586204
    • 2005-01-14
    • Wei-Ping ChenJohn Whittall
    • Wei-Ping ChenJohn Whittall
    • C07F9/46C07F15/00
    • C07F17/02B01J31/1845B01J31/186B01J31/188B01J31/189B01J31/1895B01J31/2295B01J31/2404B01J31/2409B01J31/2452B01J31/2457B01J31/2495B01J2231/645B01J2531/0205B01J2531/82B01J2531/822B01J2531/842B01J2531/847
    • The present invention relates to process for the production of chiral ligands comprising providing a starting material of Formula (A): wherein X* is a chiral or achiral directing group; and (i) is an optionally substituted mono- or polycyclic aryl or cycloalkyl group; ortholithiating the substrate; converting the ortho-lithiated substrate to a phosphine group having the formula —PR1R1″, R1 being selected from substituted and unsubstituted, branched- and straight-chain alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted carbocyclic aryl, and substituted and unsubstituted heteroaryl wherein the or each heteroatom is independently selected from sulphur, nitrogen, and oxygen, R1″ being different from R1 and being selected from substituted and unsubstituted, branched- and straight-chain alkyl, substituted and unsubstituted cycloalkyl, substituted and unsubstituted carbocyclic aryl, and substituted and unsubstituted heteroaryl wherein the or each heteroatom is independently selected from sulphur, nitrogen, and oxygen; and optionally or if necessary converting X* to a different grouping to produce a chiral ligand.
    • 本发明涉及制备手性配体的方法,其包括提供式(A)的原料:其中X *是手性或非手性导向基团; 和(i)是任选取代的单环或多环芳基或环烷基; 使基板正交化; 将邻位锂化的底物转化为具有式-PR 1,R 1,R 2的膦基,其选自取代和未取代的 ,支链和直链烷基,取代和未取代的环烷基,取代和未取代的碳环芳基和取代和未取代的杂芳基,其中该杂原子或每个杂原子独立地选自硫,氮和氧,R 1' SUP>与R 1不同,并且选自取代和未取代的,支链和直链烷基,取代和未取代的环烷基,取代和未取代的碳环芳基和取代和未取代的杂芳基,其中所述或各个 杂原子独立地选自硫,氮和氧; 并且任选地或如果需要将X *转化成不同的基团以产生手性配体。