Process for the preparation of 3-hydroxyoxetanes
    3.
    发明授权
    Process for the preparation of 3-hydroxyoxetanes 失效
    3-羟基氧杂环丁烷的制备方法

    公开(公告)号:US5663383A

    公开(公告)日:1997-09-02

    申请号:US671905

    申请日:1996-06-28

    CPC分类号: C07D305/08

    摘要: A process for the preparation of 3-hydroxyoxetanes of formula I ##STR1## wherein R.sub.9 and R.sub.10 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, by(1) reaction of a carboxylic acid R--CO.sub.2 H, wherein R is branched alkyl, with an epichlorohydrin of formula II ##STR2## wherein R.sub.9 and R.sub.10 are as defined hereinbefore, to form an ester of formula III ##STR3## wherein R, R.sub.9 and R.sub.10 are as defined hereinbefore, (2) reaction of that ester with an ether of formula IVCHR.sub.1 .dbd.CH--O--R.sub.2 (IV),wherein R.sub.1 is hydrogen or methyl, R.sub.2 is C.sub.1 -C.sub.6 alkyl, or R.sub.1 and R.sub.2 together form a radical of formula --(CH.sub.2).sub.3 --, in the presence of a catalyst, to form an ester of formula V ##STR4## (3) hydrolysis and cyclization of that ester in the presence of a base to form a compound of formula VI ##STR5## wherein R.sub.1, R.sub.2, R.sub.9 and R.sub.10 are as defined hereinbefore,(4) acetal cleavage in the presence of an acid to form the corresponding 3-hydroxyoxetane and(5) isolation of that 3-hydroxyoxetane.

    摘要翻译: 制备式I的3-羟基氧杂环丁烷的方法其中R 9和R 10各自独立地为氢或C 1 -C 4烷基,通过(1)羧酸R-CO 2 H的反应,其中R为 (II)表示的支链烷基,其中R9和R10如上所定义,以形成式III的酯其中R,R 9和R 10如上所定义,(2) )其中R 1是氢或甲基,R 2是C 1 -C 6烷基,或者R 1和R 2一起形成式 - (CH 2)3的基团) 在催化剂的存在下,形成式V的酯(V)(3)在碱的存在下水解和环化该酯以形成式VI化合物(VI) 其中R 1,R 2,R 9和R 10如上所定义,(4)在酸存在下缩醛裂解以形成相应的3-羟基氧杂环丁烷和(5)该3-羟基氧杂环丁烷的分离。