Novel reactions of bicyclic amide acetals with reactive protic compounds
having the formula HN(R')YR.sup.2
    33.
    发明授权
    Novel reactions of bicyclic amide acetals with reactive protic compounds having the formula HN(R')YR.sup.2 失效
    双环酰胺缩醛与式HN(R')YR2的反应性质子化合物的新反应

    公开(公告)号:US4826960A

    公开(公告)日:1989-05-02

    申请号:US850656

    申请日:1986-04-11

    申请人: Anil B. Goel

    发明人: Anil B. Goel

    摘要: The process for the reaction of bicyclic amide acetals with reactive protic compounds of the general Formula ##STR1## wherein Y represents a member selected from the group consisting of ##STR2## R.sup.1 represents a member selected from the group consisting of hydrogen, an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 12 carbon atoms, and R.sup.2 represents a member selected from the group consisting of an alkyl group having from 1 to 10 carbon atoms, an aryl group having from 6 to 12 carbon atoms, an alkylene ether group having from 1 to 50 carbon atoms, an arylene ether group having from 6 to 50 carbon atoms such as ethyl carbamate to form novel products which are useful as curing agents, blowing agents and monomers is disclosed.

    摘要翻译: 双环酰胺缩醛与通式“IMAGE”的反应性质子化合物反应的方法,其中Y表示选自下组的成员:(脒,咪唑,偕胺肟基),IMA图 + TR<图像> R1表示选自氢,碳原子数1〜10的烷基,碳原子数6〜12的芳基,R2表示选自由 具有1至10个碳原子的烷基,具有6至12个碳原子的芳基,具有1至50个碳原子的亚烷基醚基团,具有6至50个碳原子的亚芳基醚基团,例如氨基甲酸乙酯, 公开了可用作固化剂,发泡剂和单体的新产品。

    7-oxabicycloheptane amino-alcohol intermediates useful in making
thromboxane A.sub.2 receptor antagonists
    34.
    发明授权
    7-oxabicycloheptane amino-alcohol intermediates useful in making thromboxane A.sub.2 receptor antagonists 失效
    可用于制备血栓素A2受体拮抗剂的7-氧杂双环庚烷氨基醇中间体

    公开(公告)号:US4816579A

    公开(公告)日:1989-03-28

    申请号:US157181

    申请日:1988-01-27

    CPC分类号: C07D493/08

    摘要: A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## (wherein the above structure represents (D) of (L) isomers) which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesoanhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.1 is alkyl, that is ##STR6## such alcohol may be hydrogenated to form the aminoalcohol intermediate. All of the above 7-oxabicycloheptane compounds are novel and also form part of the present invention.

    摘要翻译: 提供了制备用于制备血栓素A2受体拮抗剂的通用结构“IMAGE”或“IMAGE”(其中上述结构表示(L)异构体的(D))的7-氧杂双环庚烷氨基醇中间体的方法。 该中间体通过使中间位酐与芳基胺反应制备,其中R是烷基,CH 2 OH,CO 2 H或CO 2烷基,以形成酸,通过用氢化铝锂或氢化二异丁基铝或Red-Al处理而还原 当R为CO 2 H,CO 2烷基或CH 2 OH,且R 1为烷基时,R 1为CH 2 OH的醇 在上述醇中,R 1为CH 2 OH时,在碱如碱金属醇盐存在下,用氯甲酸烷基酯处理该醇化合物,形成通过用碱金属,氨和酸处理而进行裂解的醇 氨基醇中间体。 在上述醇中,R 1为烷基时,可以将该醇氢化形成氨基醇中间体。 所有上述7-氧杂双环庚烷化合物都是新的,也构成本发明的一部分。

    Process and intermediates for beta-lactam antibiotics
    36.
    发明授权
    Process and intermediates for beta-lactam antibiotics 失效
    β-内酰胺抗生素的工艺和中间体

    公开(公告)号:US4734495A

    公开(公告)日:1988-03-29

    申请号:US13521

    申请日:1987-02-11

    摘要: 1-Benzyl(or substituted benzyl)-3.beta.-[4(S)-aryloxazolidin-2-one-3-yl]-4.beta.-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic .beta.-lactam antibiotics.

    摘要翻译: 1-苄基(或取代的苄基)-3β-[4(S) - 芳基恶唑烷-2-酮-3-基]-4β-(2-芳基乙烯基)氮杂环丁烷-2-酮通过环(4) S) - 芳基恶唑烷-2-酮-3-基乙酰卤和由苄胺和3-芳基丙烯醛形成的亚胺,例如 肉桂醛。 氮杂环丁酮是1-咔唑(1-脱氢)-3-羟基-3-头孢烯-4-羧酸和酯与单环β-内酰胺抗生素不对称合成中有用的手性中间体。

    Preparation of N- and S-1,2-ethylenically unsaturated organic compounds
    37.
    发明授权
    Preparation of N- and S-1,2-ethylenically unsaturated organic compounds 失效
    制备N-和S-1,2-烯属不饱和有机化合物

    公开(公告)号:US4680410A

    公开(公告)日:1987-07-14

    申请号:US585945

    申请日:1984-03-02

    申请人: Pen C. Wang

    发明人: Pen C. Wang

    CPC分类号: C07D263/22

    摘要: The invention is a process for the preparation of a N- or S-1,2-ethylenically unsaturated organic compound which comprises(a) contacting a N- or S-silylated organic compound with an aldehyde, wherein the aldehyde has a hydrogen atom bonded to the carbon adjacent to the carbonyl moiety, at elevated temperatures under conditions such that a N- or S-1-siloxyalkyl-substituted organic compound is prepared; and(b) pyrolyzing the N- or S-1-siloxyalkyl-substituted organic compound under conditions such that the siloxy moiety is elminated to prepare a N- or S-1,2-ethylenically unsaturated compound.

    摘要翻译: 本发明是制备N-或S-1,2-烯属不饱和有机化合物的方法,其包括(a)使N-或S-甲硅烷基化的有机化合物与醛接触,其中醛具有氢原子键合 在相对于羰基部分的碳上,在升高的温度下,制备N-或S-1-硅氧烷基取代的有机化合物的条件下, 和(b)在使甲硅烷氧基部分馏分以制备N-或S-1,2-烯属不饱和化合物的条件下热解N-或S-1-硅氧烷基取代的有机化合物。

    Process for preparation of 2-oxazolidinones
    39.
    发明授权
    Process for preparation of 2-oxazolidinones 失效
    2-恶唑烷酮的制备方法

    公开(公告)号:US4500717A

    公开(公告)日:1985-02-19

    申请号:US479400

    申请日:1983-03-28

    IPC分类号: C07D263/22

    CPC分类号: C07D263/22

    摘要: The invention is a process for the preparation of 2-oxazolidinones which comprises contacting a 2-hydroxyalkyl carbamate with an alkylene oxide or alkylene carbonate in the presence of a catalytic amount of a quaternary ammonium halide, quaternary phosphonium halide, a group I metal carbonate, hydroxide, oxide or halide, or a group II metal carbonate, hydroxide, oxide or halide under conditions such that a 2-oxazolidinone is prepared.

    摘要翻译: 本发明是制备2-恶唑烷酮的方法,其包括在催化量的季铵卤化物,季卤化鏻,第I族金属碳酸盐存在下使氨基甲酸2-羟烷基酯与烯化氧或碳酸亚烃酯接触, 氢氧化物,氧化物或卤化物,或第II族金属碳酸盐,氢氧化物,氧化物或卤化物,以制备2-恶唑烷酮。