Process for preparing (R) and (S)-1,2-isopropylideneglycerol by
crystallizing racemic benzoyl ester
    3.
    发明授权
    Process for preparing (R) and (S)-1,2-isopropylideneglycerol by crystallizing racemic benzoyl ester 失效
    通过结晶外消旋苯甲酸酯制备(R)和(S)-1,2-异丙基甘油的方法

    公开(公告)号:US5332674A

    公开(公告)日:1994-07-26

    申请号:US16882

    申请日:1993-02-12

    IPC分类号: C12N11/04 C12P17/04 C12P41/00

    摘要: A process is described for separating the optical isomers of 1,2-isopropylideneglycerol, of formula (I), comprising partially stereoselective enzymatic hydrolysis of 1,2-isopropylideneglycerol benzoyl ester (II) catalyzed by a free or immobilized lipase, the hydrolysis being conducted in the presence of a cosolvent and followed by crystallization enabling crystals of (II) in raceme form and mother liquor containing (II) in the form of the pure enantiomer to be selectively obtained.The compound (I) is widely used industrially as an intermediate in the synthesis of chiral drugs such as (R)-(-)-carnitine, (S)-beta-blockers, (S)-antiviral agents, analgesic drugs etc.

    摘要翻译: 描述了用于分离式(I)的1,2-异亚丙基甘油的光学异构体的方法,其包括由游离或固定的脂肪酶催化的1,2-异丙叉基甘油苯甲酰酯(II)的部分立体选择性酶水解,水解进行 在共溶剂的存在下,然后结晶使得可以选择性地获得具有外消旋形式的(II)的结晶和含有纯对映异构体形式的(II)的母液。 化合物(I)在工业上广泛用作合成手性药物如(R) - ( - ) - 肉碱,(S) - β-阻断剂,(S) - 病毒药物,止痛药物等的中间体。

    Process for the enzymatic separation of the optical isomers of racemic
oxazolidinonic derivatives
    5.
    发明授权
    Process for the enzymatic separation of the optical isomers of racemic oxazolidinonic derivatives 失效
    外消旋恶唑烷酮衍生物的光学异构体的酶分离方法

    公开(公告)号:US4933290A

    公开(公告)日:1990-06-12

    申请号:US137721

    申请日:1987-12-24

    IPC分类号: C12P17/14 C12P41/00

    CPC分类号: C12P17/14 C12P41/004

    摘要: There is disclosed a process for the biotechnological resolution, by enzymatic esterification of the corresponding racemic mixture of the S(+) and R(-) optical isomers of the oxazolidinonic compounds having formula (I): ##STR1## wherein R represents a, linear or branched, C.sub.1 -C.sub.8 alkyl group, which process is characterized in that, the racemic 3-alkyl-5-hydroxymethyl-oxazolidin-2-one derivative of formula (I) is reacted with an esterifying compound, selected from esters having formula (III): ##STR2## wherein R represents a, linear or branched, C.sub.1 -C.sub.10 alkyl or alkenyl group and R" represents a linear or branched, C.sub.1 -C.sub.4 alkyl, alkenyl group, a haloalkyl (chlorine, bromine) group or a diacyl glycerolic group or from acids having formula (IV):R'"--COOH (IV)wherein R'" represents a, linear or branched, C.sub.1 -C.sub.20 alkyl or alkenyl group or from anhydrides having formula (V): ##STR3## wherein R.sup.IV represents a, linear or branched, C.sub.1 -C.sub.6 alkyl group, in the presence of an enzyme, immobilized on a porous carrier, capable of giving rise selectively to the esterification reaction of the R(-) isomer, while leaving the S(+) isomer substantially unchanged, which latter is then separated according to known techniques.

    Process for the enzymatic separation of the optical isomers of racemic
.alpha.-alkyl-substituted primary alcohols
    7.
    发明授权
    Process for the enzymatic separation of the optical isomers of racemic .alpha.-alkyl-substituted primary alcohols 失效
    用于酶分离外消旋的α-烷基取代的伯醇的光学异构体的方法

    公开(公告)号:US4980291A

    公开(公告)日:1990-12-25

    申请号:US307913

    申请日:1989-02-09

    IPC分类号: C12P7/62 C12P41/00

    CPC分类号: C12P41/004 C12P7/62

    摘要: Biotechnological resolution by means of enzymatic transesterification of the relevant racemic mixture of the optical isomers of .alpha.-alkyl-substituted primary alcohols having the formula (I): ##STR1## wherein: R represents a linear or branched (C.sub.1 -C.sub.20)-alkyl or alkenyl group or an aryl group, also substituted or condensed with other groups, in particular a group of formula (II) or (III): ##STR2## wherein: R.sup.ii represents a (C.sub.1 -C.sub.8)-alkyl group, a (C.sub.1 -C.sub.4)-alkenyl group, an alkoxy, phenyl, phenoxy, benzoyl, or heterocyclic group;R.sup.iii represents a hydrogen or halogen atom;R.sup.iv represents a (C.sub.1 -C.sub.4)-alkyl group, and whereinR.sup.i represents a (C.sub.1 -C.sub.4)-alkyl group either equal to, or different from, R,in the presence of an enzyme either free or immobilized on a support capable of selectively causing the S isomer to be esterified, with the R isomer being left substantially unchanged, said isomers being then separated according to techniques known from the prior art. The process is used in the synthesis of antiinflammatory agents.