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    • 5. 发明授权
    • Method for producing optically active naphthalene compound
    • 光学活性萘化合物的制造方法
    • US09181217B2
    • 2015-11-10
    • US14240466
    • 2012-08-24
    • Koji MatsuyamaMasanori HatsudaMasahiko YoshinagaMitsuhiro YadaKoichi Tanimoto
    • Koji MatsuyamaMasanori HatsudaMasahiko YoshinagaMitsuhiro YadaKoichi Tanimoto
    • C07B53/00C07C25/06C07C255/03C07D401/04
    • C07D401/04C07B53/00C07C25/06C07C255/03
    • The present invention provides an industrially advantageous method for producing an optically active naphthalene compound useful as a therapeutic agent for dermatitis or the like. Specifically, the present invention provides a method for producing an optically active naphthalene compound [I], which comprises: a step of reacting a compound [a-1] and a compound [b-1] with each other in the presence of a base and a catalyst that is composed of a Pd compound and a tertiary phosphine ligand (step a); a step of asymmetrically hydrogenating a compound [c-1] in the presence of a hydrogen donor and a complex that is prepared from a ruthenium compound and a chiral ligand, or alternatively in the presence of an optically active oxazaborolidine compound (a CBS catalyst) and a boron hydride compound (step b); and a step of treating a compound [d-1] with a reducing agent (step c). (In the above formulae, Ra and Rb represent the same or different lower alkyl groups; and X1 represents a halogen atom.).
    • 本发明提供了用于制造用作皮炎等的治疗剂的光学活性萘化合物的工业上有利的方法。 具体而言,本发明提供了一种光学活性萘化合物[I]的制造方法,其特征在于,在碱的存在下,使化合物[a-1]和化合物[b-1] 和由Pd化合物和叔膦配体组成的催化剂(步骤a); 在氢供体和由钌化合物和手性配体制备的络合物的存在下,或者在光学活性的恶唑硼烷化合物(CBS催化剂)存在下,不对称地氢化化合物[c-1] 和硼氢化合物(步骤b); 和用还原剂处理化合物[d-1](步骤c)的步骤。 (上述式中,Ra和Rb表示相同或不同的低级烷基,X1表示卤素原子。