Novel cyclosporins
    7.
    发明授权
    Novel cyclosporins 失效
    新型环孢菌素

    公开(公告)号:US4771122A

    公开(公告)日:1988-09-13

    申请号:US103990

    申请日:1987-10-01

    申请人: Dieter Seebach

    发明人: Dieter Seebach

    摘要: Cylosporins e.g. of formula II ##STR1## in which X is -MeBmt- or -dihydro-MeBmt- andY is -.alpha.Abu-, -Thr-, -Val- or -Nva-,wherein the residue at the 3-position, i.e. the residue Z in formula II, is an optically active, .alpha.-N-methylated .alpha.-amino acid residue of the (D)-configuration, possess pharmaceutical, in particular immunosuppressive, anti-inflammatory and anti-parasitic activity, Intermediate cyclosporin poly-anions having a de-protonated sarcosyl residue at the 3-position, e.g. polyanions of cyclosporins of formula II above wherein X and Y have the meanings given above and Z is -Sar-, in which the said residue Z is de-protonated, are also novel and part of the invention.

    Taddol and titanium (IV) taddolate dendrimers
    9.
    发明授权
    Taddol and titanium (IV) taddolate dendrimers 失效
    鞑靼和钛(Ⅳ)杓状树枝状大分子

    公开(公告)号:US06211316B1

    公开(公告)日:2001-04-03

    申请号:US08959390

    申请日:1997-10-28

    申请人: Dieter Seebach

    发明人: Dieter Seebach

    IPC分类号: C08F13402

    CPC分类号: C08G83/003 Y10S525/902

    摘要: TADDOL dendrimers are described. Their use as crosslinkers in polymerisation reactions and the use of Ti salts of polymer-bound TADDOL dendrimers as catalysts in enantioselective addition reactions is disclosed.

    摘要翻译: 描述了TADDOL树枝状大分子。 公开了它们在聚合反应中作为交联剂的用途,以及在对映选择性加成反应中使用聚合物结合的TADDOL树枝状大分子的Ti盐作为催化剂。

    Method of producing optically active 1,3-imidazolidine-4-ones
    10.
    发明授权
    Method of producing optically active 1,3-imidazolidine-4-ones 失效
    光学活性1,3-咪唑烷-4-酮的制备方法

    公开(公告)号:US5386035A

    公开(公告)日:1995-01-31

    申请号:US974422

    申请日:1992-11-12

    CPC分类号: C07D233/32 C07D233/38

    摘要: 2.2. 1,3-imidazolidine-4-ones having the General Formula: ##STR1## are obtained in a pure form especially by means of precipitation, in which production an optically active acid can be used at 0.5-0.8 eq. for the separation of racemates. The non-desired enantiomer can be racemized in an inert solvent and the cyclization to imidazolidinone can take place by means of the optically active acid, whereupon the separation of racemates takes place directly thereafter. 1,3-imidazolidine-4-ones are valuable educts for the preparation of branched or unbranched, proteinogenic or non-proteinogenic .alpha.-amino acids by means of diastereoselective alkylation and subsequent ring splitting.

    摘要翻译: 2.2。 以纯度的形式,特别是通过沉淀获得具有以下通式的1,3-咪唑烷-4-酮:其中0.5-0.8当量可以使用光学活性的酸。 用于分离外消旋体。 非期望的对映异构体可以在惰性溶剂中进行外消旋化,并且通过光学活性的酸可以进行环化成咪唑啉酮,随后直接进行外消旋体的分离。 1,3-咪唑烷-4-酮是通过非对映选择性烷基化和随后的环分裂制备支链或非支链,蛋白质或非蛋白质的α-氨基酸的有价值的衍生物。