PROCESS FOR PRODUCING PHOSPHORUS-CONTAINING DEHYDROAMINO ACID
    5.
    发明申请
    PROCESS FOR PRODUCING PHOSPHORUS-CONTAINING DEHYDROAMINO ACID 有权
    生产含磷酸脱氢山梨醇酸的方法

    公开(公告)号:US20110009662A1

    公开(公告)日:2011-01-13

    申请号:US12529953

    申请日:2008-03-19

    CPC classification number: C07F9/4006 C07F9/3217

    Abstract: A process for efficiently producing through a small number of steps an N-substituted 2-amino-4-(substituted-oxymethylphosphinyl)-2-butenoic ester which is an intermediate for herbicide L-AMPB. The process comprises reacting a compound represented by the following formula (1): (where R1 represents C1-4 alkyl group) with a compound represented by the following formula (2): (wherein R2, R2′, and R3 each represents C1-4 alkyl and R4 represents benzyloxycarbonyl) in the presence of a base.

    Abstract translation: 通过少量步骤有效地制备作为除草剂L-AMPB的中间体的N-取代的2-氨基-4-(取代的 - 氧甲基氧膦基)-2-丁烯酸酯的方法。 该方法包括使由下式(1)表示的化合物(其中R 1表示C 1-4烷基)与下式(2)表示的化合物反应:(其中R2,R2'和R3各自表示C1- 4烷基,R 4表示苄氧基羰基)。

    Salts of 2-�(2,6-dichlorophenyl)amine!phenylacetoxyacetic acid with
organic basic cations
    8.
    发明授权
    Salts of 2-�(2,6-dichlorophenyl)amine!phenylacetoxyacetic acid with organic basic cations 失效
    2 - [(2,6-二氯苯基)胺]苯基乙酰氧基乙酸与有机碱性阳离子的盐

    公开(公告)号:US5708024A

    公开(公告)日:1998-01-13

    申请号:US750811

    申请日:1996-12-17

    Inventor: Alfred Sallmann

    Abstract: A salt of 2-�(2,6-dichlorophenyl)amine!phenylacetoxyacetic acid with an organic basic cation of formula (I); Wherein R.sub.1 and R.sub.2 independently are lower alkyl, or if R.sub.1 is hydrogen H--N(R.sub.1)(R.sub.2) has the meaning of arginine or lysine or if R.sub.1 is methyl H--N(R.sub.1)(R.sub.2) has the meaning of N-methylglucamine. This compound pocesses analgesic activity as well as antiinflammatory activity, suitable in the treatment of conditions such as rheumatoid arthritis, ankylosing spondylitis, lumbar pains, luxations and ocular inflammation. The compound further has an improved stability in aqueous solutions in comparison to the alkali metal salts, e.g. sodium and potassium.

    Abstract translation: PCT No.PCT / IB95 / 00524 Sec。 371日期1996年12月17日第 102(e)日期1996年12月17日PCT提交1995年6月28日PCT公布。 公开号WO96 / 00716 日期1996年1月11日2 - [(2,6-二氯苯基)胺]苯乙酰氧基乙酸与式(I)的有机碱性阳离子的盐; 其中R1和R2独立地是低级烷基,或者如果R1是氢,H-N(R1)(R2)具有精氨酸或赖氨酸的含义,或者如果R1是甲基H-N(R1)(R2)具有N-甲基葡糖胺的含义。 该化合物治疗镇痛活性以及抗炎活性,适用于治疗类风湿关节炎,强直性脊柱炎,腰痛,脱垂和眼部炎症等症状。 与碱金属盐相比,该化合物在水溶液中的稳定性进一步提高。 钠和钾。

    Preparation of 3-amino-2-(het)aroyl-acrylic acid derivatives
    10.
    发明授权
    Preparation of 3-amino-2-(het)aroyl-acrylic acid derivatives 失效
    3-氨基-2-(羟基)丙烯酸 - 丙烯酸衍生物的制备

    公开(公告)号:US5182401A

    公开(公告)日:1993-01-26

    申请号:US694692

    申请日:1991-05-02

    Applicant: Klaus Grohe

    Inventor: Klaus Grohe

    Abstract: A process for the preparation of a 3-amino-2-(het)aroyl-acrylic acid derivative fo the formula ##STR1## in which Y represents a nitrile, or an ester group, --COOR.sub.1, or an acetyl group, whereR.sup.1 denotes C.sub.1 -C.sub.4 -alkyl, andR denotes optionally substituted alkyl, cyclopropyl, alkoxy, phenyl or amino,A represents nitrogen or C--R.sub.2, whereR.sub.2 denotes hydrogen, methyl, halogen, nitro, methoxy or cyano,X.sub.1 and X.sub.2 are identical or different and denote halogen, andX.sub.3 denotes hydrogen, halogen or nitro andX.sub.4 denotes halogen, nitro, methoxy or methylthio, which comprises reacting a 3-dialkylamino-2-(het)aroyl-acrylic acid derivative of the formula ##STR2## in which R.sub.3 and R.sub.4 are the same or different and represent an alkyl group having 1 to 4 carbon atoms, or, together with the nitrogen atom to which they are bonded, form a ring,with a primary amine of the formula R--NH.sub.2 in the presence of at least one equivalent of an acid HX in a solvent or in excess acid.

    Abstract translation: 制备式(I)的3-氨基-2-(het)芳酰基 - 丙烯酸衍生物的方法,其中Y表示腈或酯基-COOR1或乙酰基, 其中R1表示C1-C4-烷基,R表示任选取代的烷基,环丙基,烷氧基,苯基或氨基,A表示氮或C-R2,其中R2表示氢,甲基,卤素,硝基,甲氧基或氰基,X1和X2 是相同或不同的并且表示卤素,并且X 3表示氢,卤素或硝基,X 4表示卤素,硝基,甲氧基或甲硫基,其包括使下式的图案化的3-二烷基氨基-2-(叔丁基)芳酰基 - 丙烯酸衍生物 其中R 3和R 4相同或不同并且表示具有1至4个碳原子的烷基,或者与它们所键合的氮原子一起形成环,与式 R-NH 2在至少一当量的酸HX存在下在溶剂中或过量的酸中。

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