Process for the preparation of enantiomerically-enriched cyclopropylalanine derivates

    公开(公告)号:US06635784B2

    公开(公告)日:2003-10-21

    申请号:US09957549

    申请日:2001-09-20

    IPC分类号: C07C6974

    摘要: Disclosed are processes for the preparation of enantiomerically-enriched cyclopropylalanine derivatives by the hydrogenation of certain enamides in the presence of a catalyst comprising a transition metal and a substantially enantiomerically-pure bis-phosphine catalyst and certain novel enamide ester compounds which are intermediates in the processes. The processes include novel 2-step and 3-step processes for the preparation of enantiomerically-enriched cyclopropylalanine derivatives. The two-step process comprises the steps of reacting cyclopropanecarboxaldehyde with a substituted phosphorylglycine to afford an enamide ester which then is hydrogenated in the presence of a catalyst comprising a transition metal and a substantially enantiomerically-pure bis-phosphine catalyst. The three-step process comprises the steps of forming an azlactone from an N-acylglycine and cyclopropanecarboxaldehyde, converting the azlactone to the aforesaid enamide which then is hydrogenated in the presence of a catalyst comprising a transition metal and a substantially enantiomerically-pure bis-phosphine catalyst.

    HYDROXYALKANOIC ACID AND HYDROXYALKANOICE ACID OLIGOMER ESTERS OF RETINOL
    8.
    发明申请
    HYDROXYALKANOIC ACID AND HYDROXYALKANOICE ACID OLIGOMER ESTERS OF RETINOL 有权
    羟基羟基酸和羟基甘氨酸酸低聚物

    公开(公告)号:US20120215024A1

    公开(公告)日:2012-08-23

    申请号:US13031375

    申请日:2011-02-21

    申请人: Neil Warren Boaz

    发明人: Neil Warren Boaz

    摘要: Retinyl hydroxyesters and retinyl oligo-hydroxyesters were prepared using a chemoenzymatic process from retinol and short chain esters of hydroxycarboxylic acids or short chain esters of hydroxycarboxylic acids. The presence of the hydroxyl group on the acid can result in a mixture of esters from various oligomers of the hydroxycarboxylic acid. The retinyl ester products are readily enzymatically hydrolyzed in vitro, which indicates that application to the skin should result in release of the anti-aging ingredient retinol (without the inherent instability and irritation) along with the acid, which, if chosen appropriately, should also have desirable biological effects. This combination should be effective as an anti-aging skin care ingredient.

    摘要翻译: 使用视黄醇和羟基羧酸的短链酯或羟基羧酸的短链酯的化学酶法制备视黄基羟基酯和视黄酯低聚羟基酯。 酸上的羟基的存在可以产生来自羟基羧酸的各种低聚物的酯的混合物。 视黄酯产物在体外容易地酶水解,这表明施用于皮肤应该导致抗老化成分视黄醇的释放(没有固有的不稳定性和刺激性)以及酸,如果适当选择,也应当 具有理想的生物效应。 该组合应作为抗衰老护肤成分有效。

    Preparation of aminophosphines
    10.
    发明授权
    Preparation of aminophosphines 失效
    制备氨基膦

    公开(公告)号:US06906213B1

    公开(公告)日:2005-06-14

    申请号:US10876492

    申请日:2004-06-25

    申请人: Neil Warren Boaz

    发明人: Neil Warren Boaz

    摘要: Disclosed is a process for the preparation of phosphine-aminophosphines that are useful in the formation of catalysts useful in carrying out a wide variety of reactions such as asymmetric hydrogenations, asymmetric reductions, asymmetric hydroborations, asymmetric olefin isomerizations, asymmetric hydrosilations, asymmetric allylations, asymmetric conjugate additions, and asymmetric organometallic additions. The process comprises the steps of (1) contacting a compound of formula 2 R2P—L—NHR3  2 with phosphorus trihalide PX3 in the presence of an inert, organic solvent and an acid acceptor to produce intermediate compound having formula 3 (2) contacting intermediate compound 3 with a reactant having the formula R1—M1, R2—M1 or a mixture thereof.

    摘要翻译: 公开了一种制备膦 - 氨基膦的方法,其可用于形成可用于进行各种各样的反应的催化剂,例如不对称氢化,不对称还原,不对称氢化,不对称烯烃异构化,不对称氢化硅,不对称烯丙基化,不对称烯丙基化 共轭添加物和不对称有机金属添加剂。 该方法包括以下步骤:(1)使式2的化合物<?in-line-formula description =“In-Line Formulas”end =“lead”→> R 2 PL-NHR < 在惰性有机物的存在下,使用三卤代磷酸酯PX 3将“3”在线式描述=“In-line Formula”end =“tail”?> 溶剂和酸受体以产生具有式3(2)的中间体化合物,使中间体化合物3与具有式R 1,M 2,R 2, 或其混合物。