cas 115956-12-2, (2alpha,6alpha,8alpha,9abeta)-Octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl-1H-indole-3-carboxylate

Articles about 115956-12-2Total 13 be found

Dolasetron N-oxide, preparation method and application thereof
The invention relates to a dolasetron N-oxide with a structure shown in a formula (I) or a salt thereof, and a preparation method and application of the compound, wherein the compound has a relatively strong inhibition effect on kinases Lyn and MST1, and can be used as an antitumor drug.
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Paragraph 0083-0085

(2021/06/26)

Dolasetron oxide and preparation method and application thereof
The invention relates to dolasetron oxide with a structure shown as a formula (I) or salt thereof, and a preparation method and application of the dolasetron oxide, and the dolasetron oxide has a strong inhibition effect on kinase Lyn and MST1, and can be used as an antitumor drug.
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Paragraph 0092-0094

(2020/05/14)

Dolasetron mesylate crystal form and preparation method
The invention provides a dolasetron mesylate crystal form. The molecular structural formula is represented in the description. The crystal form is a white powdery crystal, molecular composition is C19H20N2O3.CH3SO3H.H2O, a reflection angle 2 theta of X-ray powder diffraction of the crystal form has characteristic peaks at 11.8 degrees, 12.1 degrees, 15.1 degrees, 15.4 degrees, 22.9 degrees, 26.6 degrees, 29.9 degrees and 30.1 degrees, and differential scanning calorimetry shows that three absorption peaks exist at 150 DEG C, 164 DEG C and 260 DEG C. According to the dolasetron mesylate crystalform, product purity is high, few single impurities are contained, and heat stability of the crystal form is good. The invention further provides a preparation method of the dolasetron mesylate crystal form.
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(2019/04/04)

INTERMEDIATE COMPOUNDS USEFUL TO PREPARE DOLASETRON
The present invention relates to intermediates useful in the synthesis of Dolasetron and synthetic precursors thereof, as well as to processes for obtaining them. In addition, it refers to the hydrochloric salt of Dolasetron and polymorphic forms of Dolasetron and precursors thereof.
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Page/Page column 12

(2009/05/28)

Polymorphs of Dolasetron base and process for preparation thereof
The present invention provides polymorphic forms of dolasetron base and methods for their use and preparation.
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Page/Page column 6

(2009/02/11)

Polymorphic Forms of Dolasetron Base and Processes of Preparing Dolasetron Base, Its Polymorphic Forms and Salt Thereof
The present disclosure relates to a process for the preparation of endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one or Dolasetron base. It also discloses a process for the preparation of endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one mesylate or Dolasetron mesylate. Further, the present disclosure relates to a process for producing Form I of Dolasetron base, and to the novel crystalline polymorphs, Form II, III, IV and V of Dolasetron base and industrial processes for producing them.
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Page/Page column 11; 12

(2008/12/08)

METHOD FOR OBTAINING A PHARMACEUTICALLY ACTIVE COMPOUND, SYNTHESIS INTERMEDIATES THEREOF AND METHODS FOR OBTAINING THEM
The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.
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Page/Page column 16-17

(2008/06/13)

PRODUCTION OF DOLASETRON
The present invention provides an improved process for the preparation of Dolasetron salts, in particularly Dolasetron mesylate. % Also provided are intermediates for the process and methods of preparing the intermediates.
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Page/Page column 45; 50

(2008/06/13)

METHOD FOR PREPARING HEXAHYDRO-8-HYDROXY-2,6-METHANO-2H-CHINOLIZIN-3(4H)-ONE ESTERS
The invention concerns a method for preparing optionally substituted 3-indolcarboxylic acid esters, with hexahydro-8-hydroxy-2,6-methano-2H-chinolizin-3(4H)-one. The invention is characterized in that the optionally substituted 3-indolcarboxylic acid is c
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Page/Page column 3; 14-15

(2008/06/13)

USE OF 5-HT3 RECEPTOR ANTAGONISTS IN TREATING PANIC DISORDERS OR OBSESSIVE COMPULSIVE COMPULSIVE DISORDERS
5-HT 3 Receptor antagonists are useful in treating panic disorders or obsessive compulsive disorders.
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(2008/06/13)

Medicament compositions derived from quinolizine and quinolizinone and methods of use thereof
The present invention is directed to the use of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and hexahydro-8-hydroxy-2,6-methano-2H-quinolizines in the manufacture of a medicament for the treatment of anxiety, psychosis, glaucoma and for the stimulation of gastric motility.
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(2008/06/13)

Esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3-(4H)-one and related compounds
The present invention is directed to a group of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(3H)-ones and related compounds. The compounds are prepared from the appropriate carboxylic acids and alcohols by standard procedures or, where steric factors are significant, a new process which makes use of heavy metal salts of super acids can be used. The compounds involved are useful in the treatment of migraine and similar disorders and in cytotoxic drug-induced vomiting.
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(2008/06/13)

Use of quinolizine and quinolizinone derivatives in the manufacture of medicaments for the treatment of cardiac arrhythmia
The present invention is directed to the use of heterocyclic esters of hexahydro-8-hydroxy-2,6-methano-2H--quinolizin-3(4H)-ones and hexahydro-B-hydroxy-2,6-methano--2H-quinolizines in the manufacture of cardiac antiarrhythmic agents
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(2008/06/13)