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    • 32. 发明授权
    • Preparation of .alpha.-tocopherol
    • α-生育酚的制备
    • US4550182A
    • 1985-10-29
    • US588374
    • 1984-03-12
    • Hansgeorg ErnstHenning-Peter GehrkenJoachim Paust
    • Hansgeorg ErnstHenning-Peter GehrkenJoachim Paust
    • C07D317/60B01J31/16C07B61/00C07D311/72
    • C07D311/72
    • A process for the preparation of .alpha.-tocopherol of the formula I ##STR1## by reacting a chroman derivative with a C.sub.14 -Grignard reagent using a di-alkali metal tetrahalocuprate catalyst in a Schlosser-Fouquet reaction, wherein a chroman derivative of the general formula II ##STR2## where Y is a leaving group, especially Br, is used and is reacted, at from -70.degree. to 0.degree. C., first with a solution of about 1 equivalent of a Grignard compound of the general formula IIIX--Mg--R (III)where X is Cl, Br or I and R is straight-chain or branched alkyl of 1 to 14 carbon atoms, preferably methyl, ethyl or ##STR3## and then with a solution of a Grignard reagent of the formula IIIa ##STR4## in an ether solvent and a solution of a di-alkali metal tetrahalocuprate in an ether solvent. The novel process simplifies the preparation of 2RS,4'RS,8'RS-, 2R,4'RS,8'RS- or 2R,4'R,8'R-.alpha.-tocopherol by reacting a chroman structural unit, containing a C.sub.2 side-chain in the 2-position, with the corresponding C.sub.14 -Grignard compound.
    • 通过在Schlosser-Fouquet反应中使用二碱金属四卤代硼酸催化剂使苯并二氢吡喃衍生物与C14-格氏试剂反应制备式I的α-生育酚的方法,其中将 使用其中Y为离去基团,特别是Br的通式II(II),并且在-70℃至0℃下反应,首先用约1当量的Grignard化合物 通式III X-Mg-R(III)其中X为Cl,Br或I,R为1至14个碳原子的直链或支链烷基,优选为甲基,乙基或者“ 式IIIa的格利雅试剂(IIIa)在醚溶剂中和二碱金属四卤代硼酸酯在醚溶剂中的溶液。 该新方法简化了2RS,4'RS,8'RS-,2R,4'RS,8'RS-或2R,4'R,8'R-α-生育酚的制备,通过使色结构单元反应, 2-位的C2侧链与相应的C14-格利雅化合物。