- 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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- 3-(2-chloroethyl)-9-hydroxy-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one
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The invention provides 3-(2-chloroethyl)-9-hydroxy-2-methyl-4H-pyrido [1, 2-a] pyrimidine-4-ketone, which is prepared by the following steps: carrying out substitution reaction on ethyl acetoacetate and 1-bromo-2-chloroethane under an alkaline condition to obtain 2-acetyl-4-chlorobutyric acid ethyl ester, and reacting the 2-acetyl-4-chlorobutyric acid ethyl ester with 3-hydroxy-2-aminopyridine. Compared with an existing preparation method of paliperidone, the preparation method has the advantages that the use of high-pollution chlorinating agents such as thionyl chloride, phosphorus oxychloride and the like can be avoided by preparing the intermediate 3-(2-chloroethyl)-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one, no waste gas and waste liquid are generated, the raw materials are cheap and easy to obtain, harsh reaction conditions are not needed, and the method has the advantages of excellent yield and purity, high safety, simplicity and convenience in operation, high process economy and suitability for industrial production.
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Paragraph 0039-0042; 0057-0062
(2021/06/22)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF PALIPERIDONE
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The present invention relates to a process for preparation and purification of 3-[2-[4-(6- fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H- pyrido[1,2-a]pyrimidin-4-one, also known as paliperidone or 9-hydroxy risperidone.
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Page/Page column 26; 27
(2012/10/18)
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- PROCESS FOR PREPARING PALIPERIDONE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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The present invention discloses the process for the preparation of paliperidone and its pharmaceutically acceptable salts comprising (a) condensing 2-amino-3-hydroxy- pyridine with 2-acetylbutyro lactone in the presence of an acid catalyst to isolate 9- hydroxy-3-(2-hydroxyethyl)-2-rnethyl-4H-pyrido[l, 2-a] pyrimidin-4-one; treating 9- hydroxy-3-(2-hydroxyethyl)-2-methyl-4H-pyrido[l, 2-a] pyrimidin-4-one with a chlorinating agent; hydrogenating the product in the presence of one or more lewis acids to obtain 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[l,2-a]- pyrimidin-4-one; and condensing3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2- methyl-4H-pyrrido[l,2-a]-pyrimidin-4-one. The present invention also discloses processes for the preparation of intermediates useful in the preparation of paliperidone and its pharmaceutically acceptable salts.
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Page/Page column 14
(2011/07/07)
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- PROCESS FOR PREPARATION OF 9-HYDROXY-3-(2-CHLOROETHYL)-2-METHYL-4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE HYDROCHLORIDE
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Described herein is an improved, commercially viable and industrially advantageous process for the preparation of paliperidone intermediate 9-hydroxy-3-(2-chloroethyl)-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one and its hydrochloride salt. The process provides the paliperidone intermediate in higher yield and reduced reaction time compared to the previously disclosed processes, thereby providing for production of paliperidone and its pharmaceutically acceptable acid addition salts in high purity and in high yield.
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Page/Page column 3
(2010/02/16)
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- A PROCESS FOR THE PREPARATION OF PALIPERIDONE INTERMEDIATES
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The present invention relates to a process for the preparation of 3-(2-chloroethyl)-6, 7, 8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one; and its use in the synthesis of paliperidone.
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Page/Page column 17-18
(2009/12/05)
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- PREPARATION OF PALIPERIDONE
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Processes for preparing paliperidone.
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- AN IMPROVED PROCESS FOR PREPARATION OF PALIPERIDONE
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The present invention relates to a process for preparation and purification of 3-[2-[4- (6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl- 4H-pyrido[l,2-a]pyrimidin-4-one, also known as paliperidone or 9-hydroxy risperidone. The invention also relates to the preparation of intermediates useful in the process.
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Page/Page column 11
(2009/10/22)
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