3-amino-3-carbamoyloxyalkylacrylic acid intermediates to dihydropyridines
    1.
    发明授权
    3-amino-3-carbamoyloxyalkylacrylic acid intermediates to dihydropyridines 失效
    3-氨基-3-氨基甲酰氧基烷基丙烯酸中间体转化为二氢吡啶

    公开(公告)号:US4739106A

    公开(公告)日:1988-04-19

    申请号:US865654

    申请日:1986-05-16

    CPC classification number: C07D295/205 C07D211/90

    Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

    Abstract translation: 一种制备由以下通式表示的2-氨基甲酰氧基烷基-1,4-二氢吡啶衍生物的方法:(I),其包括:(a)使由以下通式表示的3-氨基-3-氨基甲酰氧基烷基丙烯酸衍生物: (II)与通式(III)表示的亚苄基化合物反应:(b)使通式II的3-氨基-3-氨基甲酰氧基烷基丙烯酸衍生物与通式 (IV)和由通式R4-CO-CH2-COOR2(V)表示的β-酮酯化合物(c)(c)使由以下通式表示的3-氨基甲酰氧基烷基丙酸衍生物反应: (VI)与通式Ⅲ的亚苄基化合物和氨或其盐; 或(d)使通式VI的3-氨基甲酰基烷基丙酸衍生物与通式IV的醛化合物,通式V的β-酮酯化合物和氨或其盐反应。

    Process for the preparation of N-substituted imido-dicarboxylic acid
diaryl esters
    5.
    发明授权
    Process for the preparation of N-substituted imido-dicarboxylic acid diaryl esters 失效
    制备N-取代的亚氨基二羧酸二芳基酯的方法

    公开(公告)号:US4348331A

    公开(公告)日:1982-09-07

    申请号:US233249

    申请日:1981-02-10

    Abstract: This invention relates to a process for the preparation of N-substituted imido-dicarboxylic acid diaryl ester compound of the formulaR.sup.1 --N(CO--OR.sup.2).sub.2 (I)whereinR.sup.1 is an optionally substituted aliphatic, cycloaliphatic, araliphatic, aromatic or heterocyclic radical, andR.sup.2 is an optionally substituted aryl radical,which can be used as intermediates for the production of known herbicides, which process comprises reacting an amine salt of the formulaR.sup.1 --NH.sub.2.HX.sup.1 (II)wherein X.sup.1 is a halogen, with a carbonic acid aryl ester halide of the formulaR.sup.2 --O--CO--X.sup.2 (III)wherein X.sup.2 is halogen, at a temperature from 100.degree. C. to 300.degree. C.

    Abstract translation: 本发明涉及制备式R 1 -N(CO-OR 2)2(I)的N-取代的亚氨基二羧酸二芳基酯化合物的方法,其中R 1是任选取代的脂族,脂环族,芳脂族,芳族或杂环 并且R 2是任选取代的芳基,其可以用作制备已知除草剂的中间体,该方法包括使其中X 1为卤素的式R 1 -NH 2 H 2(II)的胺盐与 在其中X 2是卤素的式R 2 -O-CO-X 2(III)的碳酸芳酯卤化物,在100℃至300℃的温度下进行。

    .alpha.Acetylene and .alpha.-vinyl derivatives of amino acids
    7.
    发明授权
    .alpha.Acetylene and .alpha.-vinyl derivatives of amino acids 失效
    α乙炔和氨基酸的α-乙烯基衍生物

    公开(公告)号:US4323704A

    公开(公告)日:1982-04-06

    申请号:US225503

    申请日:1981-01-16

    Abstract: Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.b can be the same or different; with the provisos that when R.sub.2 is hydrogen, R.sub.1 is --C.tbd.CH; when A is ethylidene, R.sub.2 is hydrogen; and when R.sub.a is ##STR6## A is methylene; and pharmaceutically acceptable salts and individual optical isomers thereof.

    Abstract translation: 新颖的式(Ⅰ)化合物,其中A是亚甲基,亚乙基或亚乙基; R1是-C3BCH或-CH = CH2; R2是氢或COR,其中R是羟基,1至8个碳原子的直链或支链烷氧基,-NR4R5,其中R4和R5分别是氢或1-4个碳原子的直链或支链低级烷基或 其中R 6是氢,1至4个碳原子的直链或支链低级烷基,苄基或对羟基苄基; R a是氢,其中烷基部分具有1至4个碳原子并且是直链或支链的烷氧基羰基,其中烷氧基部分具有1至4个碳原子并且是直链或支链或其中R7被选定 由氢,1至4个碳原子的直链或支链低级烷基,苄基和对羟基苄基; 并且Rb具有与Ra所定义的相同的含义,不同之处在于Rb不是< IMAGE>并且Ra和Rb可以相同或不同; 条件是当R2是氢时,R1是-C3BCH; 当A为亚乙基时,R 2为氢; 而当Ra为亚甲基时, 及其药学上可接受的盐和单独的光学异构体。

    Carbamate compounds
    8.
    发明授权
    Carbamate compounds 失效
    氨基甲酸酯化合物

    公开(公告)号:US4686304A

    公开(公告)日:1987-08-11

    申请号:US341123

    申请日:1982-01-20

    CPC classification number: C07D203/14

    Abstract: The invention provides compounds of the formula ##STR1## wherein X is chloride, fluoride, bromide, iodide or alkoxy, and R is alkyl, arylalkyl, or phenyl which compounds are intermediates in the preparation of 3,6-bis(carboethoxyamino)-2,5-diaziridinyl-1,4-benzoquinone.

    Abstract translation: 本发明提供下式的化合物,其中X是氯化物,氟化物,溴化物,碘化物或烷氧基,R是烷基,芳基烷基或苯基,该化合物是制备3,6-双(乙氧羰基氨基)-2 ,5-二氮丙啶基-1,4-苯醌。

    Preparation of 1,3-di(alkoxycarbonylamino)propanes
    9.
    发明授权
    Preparation of 1,3-di(alkoxycarbonylamino)propanes 失效
    制备1,3-二(烷氧基羰基氨基)丙烷

    公开(公告)号:US4672137A

    公开(公告)日:1987-06-09

    申请号:US856971

    申请日:1986-04-29

    CPC classification number: C07C271/06

    Abstract: 1,3-Di(alkoxycarbonylamino)propanes of the general formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 can be identical or different and each is hydrogen, or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, and R.sup.4 is an aliphatic, cycloaliphatic or araliphatic radical, are prepared by reacting an .alpha.,.beta.-unsaturated aldehyde with a carbamic acid ester by reacting in a first stage as the .alpha.,.beta.-unsaturated aldehyde a compound of the general formula II ##STR2## where R.sup.1, R.sup.2 and R.sup.3 have the abovementioned meanings, with a carbamic acid ester of the general formula III ##STR3## where R.sup.4 has the abovementioned meanings, at 0.degree.-150.degree. C. to give a 1,1,3-tri(alkoxycarbonylamino)propane of the general formua IV ##STR4## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the abovementioned meanings, and in a second stage heating the compound of the general formula (IV) in the presence of a hydrogenation catalyst and hydrogen under 1-300 bar at 100.degree.-300.degree. C.

    Abstract translation: 通式I(I)的1,3-二(烷氧基羰基氨基)丙烷,其中R 1,R 2和R 3可以相同或不同,各自为氢,或脂族,脂环族,芳脂族或芳族基,R4为 通过使α,β-不饱和醛与氨基甲酸酯反应,通过在第一阶段中作为α,β-不饱和醛与通式II的化合物(II)反应来制备脂族,脂环族或芳脂族基团 )其中R 1,R 2和R 3具有上述含义,与0℃-150℃下具有上述含义的通式III(III)的氨基甲酸酯反应,得到1,1, (IV)的3-三(烷氧基羰基氨基)丙烷,其中R 1,R 2,R 3和R 4具有上述含义,在第二阶段中,在通式(Ⅳ)的化合物存在下加热通式 氢化催化剂和在1-300巴下在100-300℃的氢气

Patent Agency Ranking