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    Synthesis of N-protected-.alpha.-substituted-glycine racemic esters by zinc-mediated addition of organic halide to glycine cation equivalent
    4.
    发明授权
    Synthesis of N-protected-.alpha.-substituted-glycine racemic esters by zinc-mediated addition of organic halide to glycine cation equivalent 失效
    通过锌介导的将有机卤化物加成到甘氨酸阳离子当量中合成N-保护的α-取代的 - 甘氨酸外消旋酯

    公开(公告)号：US5508466A

    公开(公告)日：1996-04-16

    申请号：US227217

    申请日：1994-04-13

    申请人： Norman A. Abood ,  Roger A. Nosal

    发明人： Norman A. Abood ,  Roger A. Nosal

    IPC分类号： C07C269/06 ,  C07C271/22 ,  C12P13/04 ,  C12P41/00 ,  C12S1/00 ,  C12S9/00 ,  C07C269/04 ,  C07C271/12

    CPC分类号： C07C271/22 ,  C07C269/06 ,  C12P13/04 ,  C12P41/005

    摘要： A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with .alpha.-chymotrypsin provides N-Boc-L-propargylglycine in high yield.

    摘要翻译： 描述了用于合成N-Boc-L-炔丙基甘氨酸的方法，其是用于制备高效口服活性的肾素抑制剂的关键中间体。 该方法包括在锌粉存在下将有机卤化物与甘氨酸阳离子当量如N-Boc-2-乙酰氧基甘氨酸甲酯反应，以高产率得到Boc-保护的氨基酸衍生物。 通常有用的有机卤化物是烯丙基，苄基和炔丙基卤化物。 用α-胰凝乳蛋白酶拆分甲基N-Boc-炔丙基甘氨酸以高产率提供N-Boc-L-炔丙基甘氨酸。

    N,N-Di-alkyl(phenoxy)benzamide derivatives
    5.
    发明授权
    N,N-Di-alkyl(phenoxy)benzamide derivatives 失效
    N，N-DI-ALKYL（PHENOXY）BENZAMIDE DERIVATIVES

    公开(公告)号：US5223539A

    公开(公告)日：1993-06-29

    申请号：US796513

    申请日：1991-11-21

    申请人： Roger A. Nosal ,  Michael A. Stealey ,  Richard M. Weiser

    发明人： Roger A. Nosal ,  Michael A. Stealey ,  Richard M. Weiser

    IPC分类号： C07C233/65 ,  C07C235/42 ,  C07C235/54 ,  C07C235/84 ,  C07C237/38 ,  C07D317/60 ,  C07D317/64

    CPC分类号： C07C235/54 ,  C07C233/65 ,  C07C235/42 ,  C07C235/84 ,  C07C237/38 ,  C07D317/60 ,  C07D317/64 ,  C07C2101/08 ,  C07C2101/14 ,  Y10S514/826 ,  Y10S514/886

    摘要： The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Z can be: ##STR2## wherein R.sup.3 is alkyl having 1 to 6 carbon atoms and, when n is greater than 1, each R.sup.3 can be the same or different; and n is an integer from 1 to 3;R.sup.1 and R.sup.2 can each independently be hydrogen, straight or branched chain alkyl, or cycloalkyl having 3 to 8 carbon atoms which can optionally be substituted at one or more positions by alkyl of 1 to 6 carbon atoms; X is oxygen, sulfur, NR.sup.4, wherein R.sup.4 is hydrogen or alkyl having 1 to 4 carbon atoms, C.dbd.O, CHOH, or CH.sub.2 ; Y is hydrogen, alkoxy, halogen, alkyl, or hydroxy; and m is an integer from 0 to 3. The compounds are antagonists of platlet-activating factor (PAF).

    摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐，其中Z可以是：（a）其中R 3是具有1至6个碳原子的烷基，当n大于1时， 每个R3可以相同或不同; n为1〜3的整数， R 1和R 2可各自独立地为氢，直链或支链烷基或具有3至8个碳原子的环烷基，其可以任选地在一个或多个位置被1-6个碳原子的烷基取代; X是氧，硫，NR 4，其中R 4是氢或具有1至4个碳原子的烷基，C = O，CHOH或CH 2; Y是氢，烷氧基，卤素，烷基或羟基; m是0-3的整数。化合物是铂弹性因子（PAF）的拮抗剂。

    Synthesis of chiral N-protected-.alpha.-substituted-glycine free acids by zinc-mediated addition of organic halide to glycine cation equivalent
    6.
    发明授权
    Synthesis of chiral N-protected-.alpha.-substituted-glycine free acids by zinc-mediated addition of organic halide to glycine cation equivalent 失效
    通过锌介导的将有机卤化物加成到甘氨酸阳离子当量中合成手性N-保护的α-取代 - 甘氨酸游离酸

    公开(公告)号：US5665598A

    公开(公告)日：1997-09-09

    申请号：US593732

    申请日：1996-01-29

    申请人： Norman A. Abood ,  Roger A. Nosal

    发明人： Norman A. Abood ,  Roger A. Nosal

    IPC分类号： C07C269/06 ,  C07C271/22 ,  C12P13/04 ,  C12P41/00 ,  C12S1/00 ,  C12S9/00 ,  C07C271/12 ,  C07C269/04

    CPC分类号： C07C271/22 ,  C07C269/06 ,  C12P13/04 ,  C12P41/005

    摘要： A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with .alpha.-chymotrypsin provides N-Boc-L-propargylglycine in high yield.

    摘要翻译： 描述了用于合成N-Boc-L-炔丙基甘氨酸的方法，其是用于制备高效口服活性的肾素抑制剂的关键中间体。 该方法包括在锌粉存在下将有机卤化物与甘氨酸阳离子当量如N-Boc-2-乙酰氧基甘氨酸甲酯反应，以高产率得到Boc-保护的氨基酸衍生物。 通常有用的有机卤化物是烯丙基，苄基和炔丙基卤化物。 用α-胰凝乳蛋白酶拆分甲基N-Boc-炔丙基甘氨酸以高产率提供N-Boc-L-炔丙基甘氨酸。