Abstract:
The invention is directed to a process for the preparation of substituted threonolactone and substituted threose compounds which are intermediates in the synthesis of phosphonate nucleosides being useful antiviral agents.
Abstract:
Disclosed is a method of crystallizing a taxane comprising combining the taxane and methylene chloride to obtain a solution and adding an anti-solvent to the solution to obtain a crystalline taxane, wherein the anti-solvent is selected from the group consisting of hexane and heptane.
Abstract:
The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.
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:
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:
Additives for paper making are disclosed herein. Specifically, the additives are wax-free alternatives to conventional coatings, including ASA, AKD and optionally an acrylic containing composition. Other additives may be included in the coating, such as cationic particles or compositions. The coatings may be used at a variety of points during the paper making process, including on the calender stack and in the wet end.
Abstract:
A process for making a hydrogenated product includes providing a clarified DAS-containing fermentation broth; distilling the broth under super atmospheric pressure at a temperature of >100° C. to about 300° C. to form an overhead that includes water and ammonia, and a liquid bottoms that includes SA, and at least about 20 wt % water; cooling the bottoms to a temperature sufficient to cause the bottoms to separate into a liquid portion in contact with a solid portion that is substantially pure SA; separating the solid portion from the liquid portion; recovering the solid portion; hydrogenating the solid portion in the presence of at least one hydrogenation catalyst to produce the hydrogenated product including at least one of THF, GBL or BDO; and recovering the hydrogenated product.
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.
Abstract:
The invention relates to a novel antibiotic from the macrolactin group and a microbial method for production of macrolactins and a novel isolated Bacillus subtilis, of application as the producing strain for the known Macrolactin A and the novel derivative.
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.