Processes for the production of hydrogenated products
    4.
    发明授权
    Processes for the production of hydrogenated products 有权
    生产氢化产物的方法

    公开(公告)号:US08410291B2

    公开(公告)日:2013-04-02

    申请号:US13051688

    申请日:2011-03-18

    Abstract: A process for making a hydrogenated product includes providing a clarified DAS-containing fermentation broth, distilling the broth to form an overhead that includes water and ammonia, and a liquid bottoms that includes MAS, at least some DAS, and at least about 20 wt % water, cooling and/or evaporating the bottoms, and optionally adding an antisolvent to the bottoms, to attain a temperature and composition sufficient to cause the bottoms to separate into a DAS-containing liquid portion and a MAS-containing solid portion that is substantially free of DAS, separating the solid portion from the liquid portion, recovering the solid portion, hydrogenating the second solid portion in the presence of at least one hydrogenation catalyst to produce the hydrogenated product comprising at least one of THF, GBL or BDO, and recovering the hydrogenated product.

    Abstract translation: 制备氢化产物的方法包括提供澄清的含DAS的发酵液,蒸馏培养液以形成包含水和氨的塔顶馏出物,以及液体塔底物,其包括MAS,至少一些DAS和至少约20wt% 水,冷却和/或蒸发塔底物,以及任选地向塔底物中加入抗溶剂,以获得足以使塔底物分离成含有DAS的液体部分的温度和组合物,以及基本上没有的含MAS的固体部分 的DAS,将固体部分与液体部分分离,回收固体部分,在至少一种氢化催化剂的存在下氢化第二固体部分以产生包含THF,GBL或BDO中的至少一种的氢化产物,并回收 氢化产物。

    Semisynthesis process for the preparation of 10 deacetyl-N-debenzoyl-paclitaxel
    5.
    发明授权
    Semisynthesis process for the preparation of 10 deacetyl-N-debenzoyl-paclitaxel 有权
    制备10种脱乙酰-N-去苯甲酰紫杉醇的半合成方法

    公开(公告)号:US08318957B2

    公开(公告)日:2012-11-27

    申请号:US12104715

    申请日:2008-04-17

    CPC classification number: C07D413/12 C07D305/14

    Abstract: A process for the preparation of 10-deacetyl-bis-7,10-trichloroacetylbaccatin III (VI) said process comprising: reacting 10-deacetylbaccatin III with a trichloroacetic acid activated derivative to obtain a reaction mixture, and performing an isolation step on said reaction mixture obtain purified 10-deacetyl-bis-7,10-trichloroacetylbaccatin III (VI) having a content, of corresponding 7- or 10 mono-trichloroacetyl derivatives lower than 0.1% as determined by HPLC.

    Abstract translation: 一种制备10-脱乙酰基 - 双-7,10-三氯乙酰基浆果赤霉素III(VI)的方法,所述方法包括:使10-脱乙酰基浆果赤霉素III与三氯乙酸活化的衍生物反应,得到反应混合物,并对所述反应进行分离步骤 混合物通过HPLC测定具有相应的7-或10个单三氯乙酰基衍生物低于0.1%的纯化的10-脱乙酰基 - 双-7,10-三氯乙酰基浆果赤霉素III(VI)。

    Combination cancer therapy with bis(thiohydrazide) amide compounds
    8.
    发明授权
    Combination cancer therapy with bis(thiohydrazide) amide compounds 有权
    联合癌症治疗与双(硫代酰肼)酰胺化合物

    公开(公告)号:US08017654B2

    公开(公告)日:2011-09-13

    申请号:US11918357

    申请日:2006-04-13

    Abstract: A method of treating a subject with cancer includes the step of co-administering to the subject over three to five weeks, a taxane in an amount of between about 243 μmol/m2 to 315 μmol/m2 (e.g., equivalent to paclitaxel in about 210-270 mg/m2); and a bis(thiohydrazide amide) in an amount between about 1473 μmol/m2 and about 1722 μmol/m2 (e.g., Compound (1) in about 590-690 mg/m2). The bis(thiohydrazide amide) is represented by Structural Formula (I), Y is a covalent bond or an optionally substituted straight chained hydrocarbyl group, or, Y, taken together with both >C=Z groups to which it is bonded, is an optionally substituted aromatic group. R1-R4 are independently —H, an optionally substituted aliphatic group, an optionally substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R7-R8 are independently —H, an optionally substituted aliphatic group, or an optionally substituted aryl group. Z is O or S.

    Abstract translation: 用癌症治疗受试者的方法包括在三至五周内共同给予受试者的步骤,量为约243μmol/ m 3至315μmol/ m 2的紫杉烷(例如,相当于约210的紫杉醇 -270 mg / m2); 和约1473μmol/ m 2与约1722μmol/ m 2之间的量的二(硫代酰肼)酰胺(例如化合物(1),约590-690mg / m 2)。 双(硫代酰肼)由结构式(I)表示,Y为共价键或任选取代的直链烃基,或Y与它们所键合的两个> C = Z基团一起为 任选取代的芳族基团。 R 1 -R 4独立地是-H,任选取代的脂族基团,任选取代的芳基,或者R 1和R 3与它们所键合的碳原子和氮原子一起,和/或R 2和R 4与碳和 与它们键合的氮原子形成任选地与芳环稠合的非芳族杂环。 R 7 -R 8独立地为-H,任选取代的脂族基团或任选取代的芳基。 Z是O或S.

    Semi-synthetic conversion of paclitaxel to docetaxel
    10.
    发明授权
    Semi-synthetic conversion of paclitaxel to docetaxel 有权
    将紫杉醇半合成转化为多西紫杉醇

    公开(公告)号:US07906661B2

    公开(公告)日:2011-03-15

    申请号:US11631466

    申请日:2005-06-29

    CPC classification number: C07D305/14

    Abstract: A process is provided for the semi-synthesis of taxane derivatives useful in the preparation of docetaxel, in particular, the semi-synthesis of protected taxane derivatives in a one pot reaction of protecting the C-2′, C-7 and C-10 positions and introducing a t-Boc group at the nitrogen of the amide group at the C-3′ position in paclitaxel and subsequently conversion to docetaxel, and derivatives used therein.

    Abstract translation: 提供了一种用于制备多西他赛的紫杉烷衍生物的半合成方法,特别是在保护C-2',C-7和C-10的一锅反应中保护的紫杉烷衍生物的半合成 在紫杉醇的C-3'位置的酰胺基的氮上引入t-Boc基团,随后转化为多西他赛及其中所用的衍生物。

Patent Agency Ranking