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    Process for the manufacture of 1-sulpho-2-oxoazetidine carboxylic acid intermediates via catalytic ester cleavage
    2.
    发明授权
    Process for the manufacture of 1-sulpho-2-oxoazetidine carboxylic acid intermediates via catalytic ester cleavage 失效

    公开(公告)号：US4652651A

    公开(公告)日：1987-03-24

    申请号：US852046

    申请日：1986-04-14

    申请人： Andre Furlenmeier ,  Werner Hofheinz ,  Christian N. Hubschwerlen ,  Hans P. Isenring

    发明人： Andre Furlenmeier ,  Werner Hofheinz ,  Christian N. Hubschwerlen ,  Hans P. Isenring

    IPC分类号： C07D205/085 ,  C07D263/48 ,  C07D277/20 ,  C07D277/74 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D277/40 ,  C07D213/73 ,  C07D231/38 ,  C07D233/44 ,  C07D285/08

    CPC分类号： C07D277/587 ,  C07D205/085 ,  C07D263/48 ,  C07D277/74 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

    摘要： The manufacture of 1-sulpho-2-oxazetidine derivatives of the formula ##STR1## in which Het is an optionally amino-substituted, 5- or 6-membered, aromatic heterocycle containing 1 or 2 nitrogen atoms and optionally also an oxygen or sulphur atom, R.sup.1 is hydrogen, lower alkyl, phenyl-lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl-lower-alkoxycarbonyl-lower alkyl, nitrophenyl-lower-alkoxycarbonyl-lower alkyl or carboxy-lower alkyl and R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxycarbonyl, lower alkanoyloxy-lower alkyl, lower alkoxycarbonyl-lower alkenyl, hydroxyiminomethyl, lower alkoxyiminomethyl, carbamoyl, carbamoyl-lower alkenyl or carbamoyloxy-lower alkyl, the group .dbd.NOR.sup.1 being present at least partially in the syn-form,in racemic form or in the form of the 3S-enantiomer, and of readily hydrolyzable esters and pharmaceutically compatible salts of these compounds, by acylating a compound of the formula ##STR2## in which R.sup.20 equals R.sup.2 or can also represent a 2,2-dimethyl-1,3-dioxolan-4-yl group and R.sup.3 is hydrogen or sulpho,or a salt thereof with a thioester of the formula ##STR3## in which Het is as above and R.sup.10 has any of the values of R.sup.1 except carboxy-lower alkyl, and can also represent a tri-lower alkyl-silyl-lower-alkoxycarbonyl-lower alkyl group or a carboxy-lower alkyl group converted into a readily hydrolyzable ester group, and the group .dbd.NOR.sup.10 is present at least partially in the syn-form, and carrying out subsequent steps (N-sulphonation, conversion of R.sup.20 into R.sup.2, R.sup.10 into R.sup.1), some of which are optional.The invention also provides certain novel products of formula I and benzthiazolyl thioesters of formula III per se and the preparation of the benzthiazolyl thioesters by esterifying corresponding carboxylic acids. Finally, the invention provides a process for the preparation of carboxylic acids in which R.sup.1 is t-alkoxycarbonylmethyl.The compounds of formula I have antimicrobial activity.

    Certain 2,4-dichloro-phenyl(loweralkylidene) pyridines having fungicidal activity
    3.
    发明授权
    Certain 2,4-dichloro-phenyl(loweralkylidene) pyridines having fungicidal activity 失效
    某些具有杀真菌活性的2,4-二氯 - 苯基（低级亚烷基）吡啶

    公开(公告)号：US5036074A

    公开(公告)日：1991-07-30

    申请号：US481264

    申请日：1990-02-20

    申请人： Hans P. Isenring ,  Beat Zehnder ,  Hugo Ziegler

    发明人： Hans P. Isenring ,  Beat Zehnder ,  Hugo Ziegler

    IPC分类号： A01N43/40 ,  C07D213/26 ,  C07D213/30 ,  C07D213/89 ,  C07F1/00

    CPC分类号： C07D213/30 ,  A01N43/40 ,  C07D213/26 ,  C07D213/89 ,  C07F1/005

    摘要： The invention concerns new pyridine derivatives of the formula ##STR1## wherein X signifies a group ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the significances given in the description, and their N-oxides, N-amino salts, copper complexes and acid addition salts, processes for the manufacture of these substances, fungicidal compositions which contain these substances as the active ingredient and the use of such substances and compositions for the control of fungi in agriculture and in horticulture.

    摘要翻译： 本发明涉及式（I）所示的新的吡啶衍生物，其中X表示基团（a）或（IMA）（b），R1，R2，R3，R4和R5具有说明书中给出的含义， 它们的N-氧化物，N-氨基盐，铜络合物和酸加成盐，这些物质的制造方法，含有这些物质作为活性成分的杀真菌组合物，以及使用这些物质和组合物来控制农业中的真菌 和园艺。

    Process for the manufacture of 1-sulpho-2-oxoazetidine derivatives
    4.
    发明授权
    Process for the manufacture of 1-sulpho-2-oxoazetidine derivatives 失效

    公开(公告)号：US4948898A

    公开(公告)日：1990-08-14

    申请号：US317081

    申请日：1989-02-28

    申请人： Andre Furlenmeier ,  Werner Hofheinz ,  Christian N. Hubschwerlen ,  Hans P. Isenring

    发明人： Andre Furlenmeier ,  Werner Hofheinz ,  Christian N. Hubschwerlen ,  Hans P. Isenring

    IPC分类号： C07D205/085 ,  C07D231/12 ,  C07D263/48 ,  C07D277/20 ,  C07D277/40 ,  C07D277/74 ,  C07D403/12 ,  C07D405/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07F7/08

    CPC分类号： C07D277/20 ,  C07D205/085 ,  C07D263/48 ,  C07D277/587 ,  C07D277/74 ,  C07D403/12 ,  C07D405/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07F7/0812

    摘要： The manufacture of 1-sulpho-2-oxazetidine derivatives of the formula ##STR1## in which Het is an optionally amino-substituted, 5- or 6-membered, aromatic heterocycle containing 1 or 2 nitrogen atoms and optionally also an oxygen or sulphur atom, R.sup.1 is hydrogen, lower alkyl, phenyl-lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl-lower-alkoxycarbonyl-lower alkyl, nitrophenyl-lower-alkoxycarbonyl-lower alkyl or carboxy-lower alkyl and R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxycarbonyl, lower alkanoyloxy-lower alkyl, lower alkoxycarbonyl-lower alkenyl, hydroxyiminomethyl, lower alkoxyiminomethyl, carbamoyl, carbamoyl-lower alkenyl or carbamoyloxy-lower alkyl, the group .dbd.NOR.sup.1 being present at least partially in the syn-form,in racemic form or in the form of the 3S-enantiomer, and of readily hydrolyzable esters and pharmaceutically compatible salts of these compounds, by acylating a compound of the formula ##STR2## in which R.sup.20 equals R.sup.2 or can also represent a 2,2-dimethyl-1,3-dioxolan-4-yl group and R.sup.3 is hydrogen or sulpho,or a salt thereof with a thioester of the formula ##STR3## in which Het is as above and R.sup.10 has any of the values of R.sup.1 except carboxy-lower alkyl, and can also represent a tri-lower alkyl-silyl-lower-alkoxycarbonyl-lower alkyl group or a carboxy-lower alkyl group converted into a readily hydrolyzable ester group, and the group .dbd.NOR.sup.10 is present at least partially in the syn-form,and carrying out subsequent steps (N-sulphonation, conversion of R.sup.20 into R.sup.2, R.sup.10 into R.sup.1), some of which are optional.The invention also provides certain novel products of formula I and benzthiazolyl thioesters of formula III per se and the preparation of the benzthiazolyl thioesters by esterifying corresponding carboxylic acids. Finally, the invention provides a process for the preparation of carboxylic acids in which R.sup.1 is t-alkoxycarbonylmethyl.The compounds of formula I have antimicrobial activity.