METHOD FOR PRODUCING CARBONYL COMPOUNDS
    1.
    发明申请
    METHOD FOR PRODUCING CARBONYL COMPOUNDS 审中-公开
    生产碳化合物的方法

    公开(公告)号:WO2004000827A1

    公开(公告)日:2003-12-31

    申请号:PCT/RU2003/000062

    申请日:2003-02-26

    IPC分类号: C07D307/32

    摘要: The invention relates to a method for producing carbonyl compounds. The inventive method is based on the reaction of liquid-phase oxidation of unsaturated heterocyclic compounds and the derivatives thereof including a link in C=C cycle into carbonyl compounds by means of nitrogen monoxide or the mixture thereof with an inert gas. The reaction is carried out at a temperature ranging from 20 DEG C to 250 DEG C and a pressure of nitrogen monoxide of 0.01-100 atm. Said method ensures the high selectivity with respect to target products, explosion safety at production and can be promising for industrial use.

    摘要翻译: 本发明涉及一种生产羰基化合物的方法。 本发明的方法是基于不饱和杂环化合物及其衍生物的液相氧化反应,其中包括通过一氧化氮或其与惰性气体的混合物在C = C循环中连接到羰基化合物中。 反应在20℃至250℃的温度和0.01-100atm的一氧化氮压力下进行。 所述方法确保了目标产品的高选择性,生产中的爆炸安全性,并且对于工业使用是有希望的。

    PROCESS FOR PRODUCING AMIDE DERIVATIVES AND INTERMEDIATES
    4.
    发明申请
    PROCESS FOR PRODUCING AMIDE DERIVATIVES AND INTERMEDIATES 审中-公开
    生产酰胺衍生物和中间体的方法

    公开(公告)号:WO1997011937A1

    公开(公告)日:1997-04-03

    申请号:PCT/JP1996002756

    申请日:1996-09-24

    IPC分类号: C07C323/25

    摘要: A process for producing amide derivatives represented by general formula [XV] or enantiomers thereof, novel intermediate compounds useful for producing these compounds, etc., and a process for producing the same, wherein each symbol is as defined in the specification. Compared with the conventional processes, the above process can be very easily effected and enables an efficient production of the compounds [XV], i.e., those involving the compounds [XVI] having an HIV protease inhibitory effect in high yields. The n ovel intermediates are highly advantageous as intermediates for producing not only the above compounds [XVI] but also those which are useful as an X-ray contrast medium, etc.

    摘要翻译: 制备由通式[XV]表示的酰胺衍生物或其对映异构体的方法,用于制备这些化合物的新型中间体化合物等及其制备方法,其中每个符号如说明书中所定义。 与常规方法相比,上述方法可以非常容易地实现,并能高效率地生产具有高蛋白酶抑制作用的化合物[ⅩⅥ]的化合物[ⅩⅤ]。 这些中间体作为不仅产生上述化合物[XVI]的中间体是非常有利的,而且也用作用作X射线造影剂等的那些。

    PRODUCTION OF CYCLIC ACETALS OR KETALS USING SOLID ACID CATALYSTS
    6.
    发明申请
    PRODUCTION OF CYCLIC ACETALS OR KETALS USING SOLID ACID CATALYSTS 审中-公开
    使用固体酸催化剂生产循环乙醇或咖啡

    公开(公告)号:WO2012177417A1

    公开(公告)日:2012-12-27

    申请号:PCT/US2012/041459

    申请日:2012-06-08

    IPC分类号: C07D317/12

    摘要: A process for making a cyclic compounds such as cyclic acetal or cyclic ketones by feeding aldehyde or ketone compounds and polyhydroxyl compounds to a reaction zone at a molar ratio of polyhydroxyl compounds to aldehyde or ketone compounds of at least 3:1, reacting these compounds in the presence of a solid acid such as an acidic ion exchange resin, to generate a liquid reaction mixture without separating water from the reaction mixture as it is being formed in the reaction mixture, withdrawing the liquid reaction mixture from the reaction zone as a liquid product stream, and feeding the liquid reaction product stream to a distillation column to separate cyclic acetal compounds from unreacted polyhydroxyl compounds, and optionally recycling back the unreacted polyhydroxyl compounds to the reaction zone. The process produces cyclic acetal compounds in yields of at least 90% with long catalyst life. The process is also suitable to make cyclic ketals from ketone compounds.

    摘要翻译: 通过将醛或酮化合物和多羟基化合物以多羟基化合物与醛或酮化合物的摩尔比至少为3:1的比例将醛或酮化合物和多羟基化合物进料到反应区中来制备环状化合物如环缩醛或环酮的方法, 固体酸如酸性离子交换树脂的存在,以便在反应混合物中形成液体反应混合物而不从反应混合物中分离出水,以液体产物的形式从反应区抽出液体反应混合物 流,并将液体反应产物流进料到蒸馏塔中以从未反应的多羟基化合物中分离出环状缩醛化合物,并任选地将未反应的多羟基化合物回收到反应区。 该方法产生环状缩醛化合物,产率至少为90%,催化剂寿命长。 该方法也适用于由酮化合物制备环状缩酮。

    PROTEASE INHIBITORS
    7.
    发明申请
    PROTEASE INHIBITORS 审中-公开
    PROTEASE抑制剂

    公开(公告)号:WO00054769A1

    公开(公告)日:2000-09-21

    申请号:PCT/US2000/006888

    申请日:2000-03-16

    CPC分类号: C07D321/06

    摘要: The present invention provides 7-membered ring 1,3-dioxepin-5-one protease inhibitors, particularly such inhibitors of cysteine and serine proteases, and methods of treating diseases which may be therapeutically modified by altering the activity of such proteases.

    摘要翻译: 本发明提供7-元环1,3-二氧杂环庚烯-5-酮蛋白酶抑制剂,特别是半胱氨酸和丝氨酸蛋白酶抑制剂,以及治疗可通过改变这种蛋白酶的活性来治疗性疾病的疾病的方法。

    LIGNANS, A PROCESS FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
    8.
    发明申请
    LIGNANS, A PROCESS FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF 审中-公开
    LIGNANS,其生产和药物组合物的方法及其用途

    公开(公告)号:WO1997014670A1

    公开(公告)日:1997-04-24

    申请号:PCT/EP1995004096

    申请日:1995-10-18

    IPC分类号: C07C69/734

    摘要: The present invention provides a process for the production of lignan derivatives, which comprises the step of subjecting benzyl substituted succinyl diesters to a Stobbe condensation using lithium methanolate as base in order to produce dibenzyl substituted half esters of succinic acid, which may subsequently be converted into the lignans. Additionally, novel lignans are provided by the invention, as well as pharmaceutical compositions containing these compounds. Furthermore the use of lignans in the manufacture of medicaments effective as SHBG inhibiting agents, anti-tumour agents and agents against prostate cancer is described.

    摘要翻译: 本发明提供一种生产木脂素衍生物的方法,其包括使用甲醇锂作为碱使苄基取代的琥珀酰二酯进行Stobbe缩合以制备二苄基取代的琥珀酸半酯的步骤,随后将其转化为 木脂素。 此外,本发明提供新的木脂素,以及含有这些化合物的药物组合物。 此外,描述了在制造有效作为SHBG抑制剂,抗肿瘤剂和抗前列腺癌剂的药物中使用木脂素。

    CHIRAL CATALYSTS AND EPOXIDATION REACTIONS CATALYZED THEREBY
    9.
    发明申请
    CHIRAL CATALYSTS AND EPOXIDATION REACTIONS CATALYZED THEREBY 审中-公开
    催化剂和环氧化反应催化

    公开(公告)号:WO1994003271A1

    公开(公告)日:1994-02-17

    申请号:PCT/GB1993001666

    申请日:1993-08-05

    IPC分类号: B01J31/18

    摘要: A compound of formula (I), in which M is a transition metal ion; A is a counter-ion if required; r, s and t are independently 0 to 3 such that r+s+t is in the range of 1 to 3; Ra, Rb, Rc are each independently hydrogen or CH2OR' where R' is hydrogen or an organic group; B and E are independently oxygen, CH2, NRd in which Rd is alkyl, hydrogen, alkylcarbonyl, or arylcarbonyl or SOn where n is 0 or an integer 1 or 2, with the proviso that B and E are not simultaneously CH2 and that when B is oxygen, NRd or SOn, then r cannot be 0, and when E is oxygen, NRd or SOn, then t cannot be 0; R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently hydrogen, alkyl or alkoxy.

    摘要翻译: 式(I)化合物,其中M为过渡金属离子; 如果需要,A是反离子; r,s和t独立地为0〜3,使得r + s + t在1〜3的范围内; R a,R b,R c各自独立地为氢或CH 2 OR',其中R'为氢或有机基团; B和E独立地是氧,CH 2,NR d,其中R d是烷基,氢,烷基羰基或芳基羰基或SO n,其中n是0或整数1或2,条件是B和E不同时为CH2,当B 是氧,NRd或SOn,那么r不能为0,当E是氧,NRd或SOn时,t不能为0; R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8,R 9和R 10独立地为氢,烷基或烷氧基。