- METHODS AND COMPOSITIONS FOR TREATMENT OF CANCER
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In an aspect, the disclosure pertains to inhibitors of ANGPTL4; synthesis methods for making disclosed compounds; pharmaceutical compositions comprising disclosed compounds; methods of treating disorders of uncontrolled cellular proliferation, e.g., a cancer; and methods of treating a disease associated with an ANGPTL4 dysfunction using disclosed compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
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Paragraph 0135; 0136
(2021/07/30)
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- Preparation method of high-purity paliperidone intermediate
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The invention belongs to the technical field of medicine, and particularly discloses a preparation method of a high-purity paliperidone intermediate 3-(2-chloroethyl)-9-hydroxyl-2-methyl-6,7,8,9-tetrahydro-4H-pyridino[1,2-a] pyrimidine-4-ketone. The preparation method particularly comprises the following steps: preparing 9-(benzyloxy)-3-(2-chloroethyl)-2-methyl-4H-pyridino[1,2-a] pyrimidine-4-ketone by taking 2-amino-3-hydroxypyridine as a starting raw material and through benzyl protection, ring closure of alpha-acetyl-gamma-butyrolactone and chloro-substitution; dissolving the 9-(benzyloxy)-3-(2-chloroethyl)-2-methyl-4H-pyridino[1,2-a] pyrimidine-4-ketone into an alcohol solvent, adding acid and a palladium-charcoal catalyst, controlling hydrogen pressure, and after the reaction is completed, performing processes of filtering, concentrating, adjusting the pH value, extracting, concentrating and refining to obtain white-like powdered 3-(2-chloroethyl)-9-hydroxyl-2-methyl-6,7,8,9-tetrahydro-4H-pyridino[1,2-a] pyrimidine-4-ketone. The preparation method is short in cycle, the product is white-like, the yield reaches 70 percent or higher, the purity reaches 99 percent or higher, related impurities of chlorine-removed byproducts are avoided, and the preparation method is suitable for industrialized enlarged production.
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- Synthesis and absolute configuration assignment of 9-hydroxyrisperidone enantiomers
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The enantiomers of 9-hydroxyrisperidone, the major metabolite of risperidone and the active component of the antipsychotic drug Invega , were synthesized by efficient methods. Their optical rotation and enantiomeric purity were characterized for the first time. The absolute configurations were assigned by comparing 1H NMR chemical shifts of Mosher esters of a key stereoisomeric intermediate. Thus, the stereoisomeric center of (+)-9-hydroxyrisperidone has been assigned as the S configuration, and its enantiomer has the configuration R.
- Xu, Weichu,Wright, George E.,Yanachkova, Milka,Yanachkov, Ivan B.
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p. 470 - 473
(2014/05/20)
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- Processes for the preparation of paliperidone
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The present invention relates to a novel process for the preparation of paliperidone and its intermediates and also relates to an improved process for the preparation of paliperidone compound of formula (I).
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Page/Page column 17; 18
(2013/07/25)
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- PROCESS FOR THE PREPARATION OF PALIPERIDONE AND ITS INTERMEDIATES
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A process for the preparation of a psychotropic agent Paliperidone. Preferably, this invention relates to a method for the purification of Paliperidone by making its acid addition salts.
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Page/Page column 6
(2010/12/29)
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- Processes for the Preparation of Paliperidone and Pharmaceutically Acceptable Salts Thereof and Intermediates for Use in the Processes
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The present invention relates to novel compounds of formula (VIII) and (X), processes for their preparation and their use in the preparation of paliperidone or a salt thereof. There is also provided by the present invention novel processes for preparing intermediates for use in the preparation of paliperidone or a salt thereof, and novel processes for preparing paliperidone or a salt thereof.
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Page/Page column 13-14
(2010/12/29)
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- Novel Intermediate for the Preparation of Paliperidone
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A new compound of formula (IV) R represents a protecting group which is removable by hydrogenation, and use thereof as an intermediate for preparing paliperidone.
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Page/Page column 3-4
(2009/07/25)
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- AN IMPROVED, INDUSTRIALLY VIABLE PROCESS FOR THE PREPARATION OF HIGH PURITY PALIPERIDONE
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The present invention relates to an improved and industrially viable process for the preparation of high purity ≥ 99.8% chemical of paliperidone of formula-I (3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-6,7,8,9-tetra-hydro-9-hydroxy-2- methyl-4H-pyrido[l,2-a]pyrimidin-4-one), involving the novel intermediate, 3-(2- hydroxyethyl)-2-methyl-9-(phenylmethoxy)-4H-Pyrido[l,2-a]pyrimidin-4-one of formula-II. All intermediates encountered in the synthetic pathway of present invention are isolated by simple crystallization techniques in high pure. Paliperidone is useful as anti-psychotic agent in the treatment of psychotic disorders and is marketed under the brand name INVEGA.
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Page/Page column 13
(2009/03/07)
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- 3-[2-[4-(6-FLUORO-1,2-BENZISOXOZOL-3-YL)-1-PIPERIDINYL]ETHYL]-6,7,8,9 TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO [1,2-A]PYRIMIDIN-4-ONE, COMPOSITIONS AND METHOD OF USE
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The present invention relates to novel 3-piperidinyl-1,2-benzisoxazoles having long-acting antipsychotic properties and which are useful in the treatment of warm-blooded animals suffering from psychotic diseases. Methods of preparing said compounds and compositions containing the same.
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