会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 1. 发明申请
    • THE ENZYMATIC METHOD OF MAKING 1,2-DIOL DERIVATIVES AND THEIR ESTERS WITH SUCCINE ANHYDRIDE
    • 制备1,2-二醇衍生物的方法及其与无水异氰酸酯的酯化
    • WO2004106534A1
    • 2004-12-09
    • PCT/KR2004/001313
    • 2004-06-02
    • ENZYTECH, LTD.HWANG, Soon OokKIM, Do HoonRYU, Hye YounLEE, Tae ImCHUNG, Sun Ho
    • HWANG, Soon OokKIM, Do HoonRYU, Hye YounLEE, Tae ImCHUNG, Sun Ho
    • C12P41/00
    • C12P7/62C12P7/04C12P41/004
    • The present invention relates to a new process for the preparation of optically active alcohols represented by the general formula 2 and their esters represented by the general formula 3 in scheme 1. In more detail, this invention relates to the process for the preparation of optically active alcohols and their esters which are used as pharmaceutical intermediates by reacting the hydroxyl group stereospecifically by lipase after adding racemic alcohols represented by the general formula 1 and succinic anhydride as an acylating agent to the organic solvent. According to this invention, the primary hydroxyl group of 1,2-diols is transformed by other functional group and the secondary hydroxyl group is esterified stereospecifically with succinic anhydride as an acylating agent. Optically active alcohols and their esters of high optical purity in high yield can be produced by using succinic anhydride as an acylating agent because alcohols can be separated from their esters more easily than those of other conventional methods.
    • 本发明涉及制备由通式2表示的光学活性醇的新方法及其在方案1中由通式3表示的酯。更详细地说,本发明涉及制备光学活性的方法 醇和它们的酯,其通过在将通式1表示的外消旋醇和琥珀酸酐作为酰化剂加入到有机溶剂中之后通过脂肪酶立体特异性地使羟基反应而用作药物中间体。 根据本发明,1,2-二醇的伯羟基被其它官能团转变,仲羟基与琥珀酸酐作为酰化剂立体特异性酯化。 通过使用琥珀酸酐作为酰化剂可以生产高产率的高光学纯度的光学活性醇及其酯,因为与其它常规方法相比,可以更容易地将醇与其酯分离。
    • 2. 发明申请
    • THE ENZYMATIC METHOD OF MAKING 1,2-DIOL DERIVATIVES AND THEIR ESTERS
    • 制备1,2-二醇衍生物及其酯的方法
    • WO2004097026A1
    • 2004-11-11
    • PCT/KR2004/001005
    • 2004-04-30
    • ENZYTECH, LTD.HWANG, Soon OokKIM, Do HoonRYU, Hye Youn
    • HWANG, Soon OokKIM, Do HoonRYU, Hye Youn
    • C12P41/00
    • C12P7/02C12P7/62C12P41/004
    • The present invention relates to a new process for the preparation of optically active alcohols represented by the general formula 2 and their esters represented by the general formula 3 by enzymatic method from racemic alcohols represented by the general formula 1 in scheme 1. In more details, this invention relates to a process for producing optically active alcohols and their esters which are used as pharmaceutical intermediates from alcohols represented by the general formula 1 by stereospecific transesterification of secondary hydroxyl group using lipases as catalyst with acyl donors in organic solvent or with acyl donors only without using organic solvent. According to this invention, optically active alcohols and esters of high optical purity in high yield can be produced by transforming the primary hydroxyl group of 1,2-diols by tosyl group and transesterifying the secondary hydroxyl group stereospecifically by lipase.
    • 本发明涉及由方案1中通式1表示的外消旋醇通过酶法由制备由通式2表示的光学活性醇及其由通式3表示的酯的新方法。更具体地, 本发明涉及一种用于制备光学活性醇及其酯的方法,其通过使用脂肪酶作为催化剂的有机溶剂中的酰基供体的催化剂或仅与酰基供体的立体特异性酯交换作为由通式1表示的醇用作药物中间体 不使用有机溶剂。 根据本发明,可以通过将1,2-二醇的伯羟基转化成甲苯磺酰基并通过脂肪酶立体特异性酯交换酯化,可以制备高产率的高光学纯度的光学活性醇和酯。