Process for the resolution of enantiomers of
5-heteroaryl-1,3,4-thiadiazinones
    64.
    发明授权
    Process for the resolution of enantiomers of 5-heteroaryl-1,3,4-thiadiazinones 失效
    5-羟基-1,3,4-噻二嗪酮类化合物的分解方法

    公开(公告)号:US5206363A

    公开(公告)日:1993-04-27

    申请号:US939754

    申请日:1992-09-02

    CPC分类号: C07D417/04 C07D417/14

    摘要: The invention relates to a process for the resolution of enantiomers of 5-heteroaryl-1,3,4-thiadiazinones of formula I by the kinetic resolution of racemates, characterized in that racemic I is dissolved in an inert solvent or solvent mixture and acylated with a chiral acid chloride. The resulting mixture of diastereoisomers is reacted with an amine or alcohol, thereby achieving a complete resolution of one of the diastereoisomers and a very slight or partial resolution of the other diastereoisomer into the enantiomers on which they are based, the resolution products are then separated off and the remaining pure diastereoisomer is converted to the corresponding pure enantiomer by reaction with an amine or an alcohol.

    摘要翻译: 本发明涉及通过外消旋体的动力学拆分来拆分式I的5-杂芳基-1,3,4-噻二嗪酮的对映异构体的方法,其特征在于将外消旋I溶于惰性溶剂或溶剂混合物中并用 手性酰氯。 所得到的非对映异构体混合物与胺或醇反应,从而实现非对映异构体之一的完全拆分和其他非对映异构体非常轻微或部分拆分成基于其的对映异构体,然后将分离产物分离出 并且通过与胺或醇反应将剩余的纯非对映异构体转化为相应的纯对映异构体。

    Diphenylmethane protective agent
    70.
    发明授权

    公开(公告)号:US11485747B2

    公开(公告)日:2022-11-01

    申请号:US17074668

    申请日:2020-10-20

    IPC分类号: C07F7/18 C07B51/00

    摘要: An object of the present invention is to develop a protecting group, which can prevent solidification or insolubilization of a compound by protecting a functional group to achieve easy separation and purification after a reaction.
    A diphenylmethane compound represented by general formula (1): wherein Y represents —OR19 (wherein R19 represents a hydrogen atom or an active ester-type protecting group), —NHR20 (wherein R20 represents, for example, a hydrogen atom, a C1-6 linear or branched alkyl group, or an aralkyl group, at least one of R1 to R10 represents a group represented by formula (2): —O—R11—X-A  (2) and the others each independently represent a hydrogen atom, a halogen atom, a C1-4 alkyl group, or a C1-4 alkoxy group; R11 represents a C1-16 linear or branched alkylene group; X represents O or CONR21 (wherein R21 represents a hydrogen atom, or a C1-4 alkyl group; and A represents, for example, a group represented by formula (3).