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    • 5. 发明专利
    • Manufacturing method of optically active alcohol
    • 光学活性醇的制备方法
    • JP2011236180A
    • 2011-11-24
    • JP2010111120
    • 2010-05-13
    • Kanto Chem Co Inc関東化学株式会社
    • HATAKEYAMA YASUTOMURATA KUNIHIKOTSUTSUMI KUNIHIKOUCHIUMI NORIYUKI
    • C07B53/00B01J31/22C07B61/00C07C29/143C07C33/20C07C33/22C07C33/46C07C67/31C07C69/66C07C253/30C07C255/36C07D311/22
    • C07B53/00C07B2200/07C07C29/143C07C29/157C07C67/31C07C253/30C07C33/26C07C33/46C07C69/732C07C255/36
    • PROBLEM TO BE SOLVED: To find out a more improved reaction condition for inhibiting racemization of a product to obtain an optically active alcohol of high optical purity.SOLUTION: The manufacturing method of an optically active alcohol comprises causing a ketone substrate to react using a hydrogen source in the presence of an asymmetric catalyst in a solvent, where the asymmetric catalyst is a metal complex represented by general formula (1) (wherein Rand Rare the same or different and are each a hydrogen atom, an alkyl group, an optionally substituted phenyl group, or the like; Ris an alkyl group, a perfluoroalkyl group, an optionally substituted naphthyl group, an optionally substituted benzyl group, or the like; Ris a hydrogen atom or an alkyl group; Ar is an optionally substituted benzene or an optionally substituted cyclopentadienyl group; X is an anionic group; M is ruthenium, rhodium or iridium; n is 0 or 1 and, when n is 0, X does not exist; and * represents an asymmetric carbon); the hydrogen source is a formic acid salt; and the solvent is (1) an organic solvent (provided that polyethylene glycol is excluded) and/or (2) water and an aprotic solvent miscible with water, each capable of dissolving the asymmetric catalyst and the formic acid salt. There can be exemplified reaction formula (A) as a concrete example.
    • 要解决的问题:为了找出抑制产物外消旋化的更好的反应条件,得到高光学纯度的光学活性醇。 解决方案:光学活性醇的制造方法包括:使用氢源在不对称催化剂存在下在溶剂中使酮底物反应,其中不对称催化剂是由通式(1)表示的金属络合物, (其中R 1 和R 2 相同或不同,各自为氢原子,烷基,任选取代的 苯基等; R 2是烷基,全氟烷基,任意取代的萘基,任意取代的苄基等; R SP SP =“POST”> 4 是氢原子或烷基; Ar是任选取代的苯或任选取代的环戊二烯基; X是阴离子基团; M是钌,铑或铱; n是0或 1,当n为0时,X不存在; *表示不对称碳); 氢源是甲酸盐; 溶剂是(1)排除有机溶剂(不含聚乙二醇)和/或(2)水和与水混溶的非质子溶剂,各自能溶解不对称催化剂和甲酸盐。 作为具体实例可以列举反应式(A)。 版权所有(C)2012,JPO&INPIT