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    • 36. 发明申请
    • ORGANOCATALYSTS AND METHODS OF USE IN CHEMICAL SYNTHESIS
    • 化学合成中的有机物和使用方法
    • WO2006007586A1
    • 2006-01-19
    • PCT/US2005/023691
    • 2005-06-30
    • SCIENCE & TECHNOLOGY CORPORATION @ UNMWANG, WeiWANG, JianLI, Hao
    • WANG, WeiWANG, JianLI, Hao
    • C07D211/08
    • C07D207/09C07B2200/07C07C45/511C07C45/54C07C45/72C07C45/74C07C47/56C07C49/203C07C49/21C07C49/235C07C49/647C07C49/653C07C49/683C07C49/697C07C49/753C07C49/86C07C67/343C07C201/12C07C205/44C07C205/45C07C213/02C07C215/42C07C227/32C07C239/20C07C253/30C07C319/14C07C391/02C07C2601/08C07C2601/14C07C2601/16C07C2601/18C07D309/30C07D317/72C07D333/22C07C49/258C07C49/245C07C69/76C07C323/22C07C255/56C07C229/22C07C229/28C07C229/30C07C229/36
    • The present invention pertains generally to compositions comprising organocatalysts that facilitate stereo-selective reactions and the method of their synthesis and use. Particularly, the invention relates to metal-free organocatalysts for facilitation of stereo-­selective reactions, and the method of their synthesis and use. These compounds have the structure of the Formulas (I) and (II). Where X is independently selected from CH 2 , N-R a , O, S or C=O; Y is CH 2 , N-R a , O, S or C=O, with the proviso that at least one of X or Y is CH 2 , and preferably both of X and Y are CH 2 ; R a is H, an optionally substituted C 1 -C 12 alkyl, preferably an optionally substituted C 1 -C 6 alkyl including a C 3 -C 6 cyclic alkyl group, or an optionally substituted aryl group, preferably an optionally substituted phenyl group; R b is H, an optionally substituted C 1 -C 12 alkyl, preferably an optionally substituted C 1 -C 6 acyclic or a a C 3 -C 6 cyclic alkyl group, CHO, N(Me)O, CO(S)R a or the group of Formula (III). Where R c and R d are each independently H, F, C1, an optionally substituted C 1- C 20 alkyl, preferably an optionally substituted C 1 -C 12 alkyl, more preferably a C 1 -C 6 alkyl, and an optionally substituted aryl group, or together R c and R d form an optionally substituted carbocyclic or optionally substituted heterocyclic ring; R 1 is OH, OR, NR'R", NHC(=O)R, NHSO 2 R; R 2 is H, F, C1, an optionally substituted C 1- C 20 alkyl, preferably an optionally substituted C 1 ­C 6 alkyl, an optionally substituted aryl group or a =O group (which establishes a carbonyl group with the carbon to which =O is attached; R 3 is H, OH, F, C1, Br, I, Cl, an optionally substituted C 1 -C 20 alkyl, alkenyl or alkynyl ("hydrocarbyl") group, preferably an optionally substituted C 1 -C 6 alkyl, or an optionally substituted aryl, such that the carbon to which R 3 is attached has an R or S configuration; R is H, an optionally substituted C 1 -C 20 alkyl, preferably an optionally substituted C 1 -C 6 alkyl, or an optionally substituted aryl group, R' and R" are each independently H, an optionally substituted C 1 -C 20 alkyl group, preferably an optionally substituted C 1 -C 6 alkyl, or an optionally substituted aryl group; or together R' and R" form an optionally substituted heterocyclic, preferably a 4 to 7 membered optionally substituted heterocyclic group or an optionally substituted heteroaryl ring with the nitrogen to which R' and R" are attached; and wherein said compound is free from a metal catalyst.
    • 本发明通常涉及促进立体选择性反应的有机催化剂及其合成和使用方法的组合物。 特别地,本发明涉及促进立体选择性反应的无金属有机催化剂及其合成和使用方法。 这些化合物具有式(I)和(II)的结构。 其中X独立地选自CH 2,N-R a,O,S或C = O; Y是CH 2,NR a,O,S或C = O,条件是X或Y中的至少一个是CH 2 2 >,并且优选X和Y两者都是CH 2 2; R a是H,任选取代的C 1 -C 12烷基,优选任选取代的C 1 -C 12 - 包括C 3 -C 6环烷基的C 6 -C 6烷基或任选取代的芳基,优选任选取代的苯基; R b是H,任选取代的C 1 -C 12烷基,优选任选取代的C 1 -C 12烷基, C 6不饱和环或C 3 -C 6环烷基,CHO,N(Me)O,CO(S)R SUP > III或式(III)的基团。 其中R 0和R d各自独立地为H,F,C 1,任选取代的C 1 -C 20 >烷基,优选任选取代的C 1 -C 12烷基,更优选C 1 -C 12烷基,更优选C 1 -C 12 - 烷基和任选取代的芳基,或一起R和C和R d形成任选取代的碳环或任选取代的杂环; R 1是OH,OR,NR'R“,NHC(= O)R,NHSO 2 R; R 2是H,F ,C 1,任选取代的C 1 -C 20烷基,优选任选取代的C 1 -C 6烷基 ,任选取代的芳基或= O基团(其中与O连接的碳上形成羰基; R 3是H,OH,F,Cl,Br,I,Cl ,任选取代的C 1 -C 20烷基,烯基或炔基(“烃基”)基团,优选任选取代的C 1 -C C 6 -C 6烷基或任选取代的芳基,使得R 3连接的碳具有R或S构型; R是H,任选取代的C