- Preparation method for pralatrexate intermediate
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The invention specifically relates to a preparation method for a pralatrexate intermediate, belonging to the technical field of medicine. According to the preparation method for the intermediate alpha-propargyl-(4-methylformate)-methylphenyl acetate, operation is more convenient and the content of impurities is lower; and in particular, the ratio of dithropropyl impurities in the produced intermediate is obviously reduced, the yield of the target product alpha-propargyl-(4-methylformate)-methylphenyl acetate is significantly increased, and product purity is greatly improved. The preparation method can be applied to large-scale production of pralatrexate bulk drugs and preparation of pralatrexate intermediates.
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Paragraph 0025; 0026; 0028; 0030; 0032; 0033; 0034; 0036
(2018/04/02)
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- A suitable industrial production pula Qu Sha method for the preparation of
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The invention relates to the field of pharmaceutical chemistry technology, and more specifically relates to an anticarcinogen 10-Propargyl-10-deazaaminopterin (Pralatrexate) and synthesis of an intermediate thereof. The invention has the advantages of simple operation, low contents of related impurities, easiness in purification of intermediate, thereby avoiding purification mode of column chromatography, and the invention can be applied to large scale production of Pralatrexate bulk drug as well as preparation and purification method of important intermediates.
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Paragraph 0041-0042
(2017/01/23)
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- IMPROVED PROCESS FOR THE PREPARATION OF PRALATREXATE
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An improved process for the preparation of Pralatrexate which is less hazardous. The invention further relates to novel intermediates and process thereof useful for the preparation of Pralatrexate. The present invention also relates to a substantially pure Pralatrexate and a process for obtaining the same in high yield.
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Paragraph 0145; 0146
(2015/07/15)
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- PROCESS FOR PRALATREXATE
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The present invention provides a novel process for the purification of alpha-propargylhomoterephthalic acid dimethyl ester substantially free of homoterephthalic acid dimethyl ester. The present invention also provides a novel process for the purification of pralatrexate.
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Page/Page column 6
(2014/05/24)
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- IMPROVED PROCESS FOR THE PREPARATION OF PRALATREXATE
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An improved process for the preparation of Pralatrexate which is less hazardous. The invention further relates to novel intermediates and process thereof useful for the preparation of Pralatrexate. The present invention also relates to a substantially pure Pralatrexate and a process for obtaining the same in high yield.
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Page/Page column 20; 21
(2014/02/16)
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- PROCESS FOR PREPARATION OF AN ANTIFOLATE AGENT
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The specification relates to a process for preparation of an antifolate compound of formula 7, such as Pralatrexate. Also, disclosed are intermediates and processes for preparation of intermediates useful in the preparation of the antifolate compound. The substituents Y, Z, R, R1 and R2 are as described herein. The processes and intermediates can provide an alternate route to the synthesis of the antifolate compound. Further, the processes can help to avoid distillation or evaporation of high boiling point solvents, chromatographic purification and use of hazardous combination of solvents; and can also provide a product having high purity, all of which are desirable for synthesis on a large scale.
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Paragraph 0065
(2014/01/07)
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- Optically Pure Diastereomers of 10-Propargyl-10-Deazaaminopterin and Methods of Using Same
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The present invention relates to diastereomers of 10-propargyl-10-deazaminopterin, compositions comprising optically pure diastereomers of 10-propargyl-10-deazaminopterin, in particular the two (R,S) diastereomers about the C10 position. Methods of preparation of these diastereomers, compositions containing them, and their use for the treatment of conditions related to inflammatory disorders and cancer are also disclosed.
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Page/Page column 7
(2011/08/08)
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- Treatment of T-cell lymphoma using 10-propargyl-10-deazaaminopterin
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T cell lymphoma is treated by administering to a patient suffering from T cell lymphoma a therapeutically effective amount of 10-propargyl-10-deazaaminopterin. Remission is observed in human patients, even with drug resistant T cell lymphoma at weekly dosages levels as low as 30 mg/m2. In general, the 10-propargyl-10-deazaaminopterin is administered in an amount of from 30 to 275 mg/m2 per dose.
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Page/Page column 3; 4; Sheet 2
(2008/06/13)
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- Antiinflammatory and antineoplastic 5-deazaaminopterins and 5,10-dideazaaminopterins
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Antiinflammatory and antineoplastic 5-deazaaminopterins and 5,10-dideazaaminopterins and their 5 and 10 alkyl analogs. A method for the treatment and prevention of inflammatory disease, such as rheumatoid arthritis, and for suppression and prevention of neoplastic growth in tumors and in blood forming tissues. A process for preparation of 10-deazaaminopterins.
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- Heteroaroyl 10-deazaamino-pterine compounds and use for rheumatoid arthritis
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There is disclosed certain heteroaroyl 10-deazaaminopterin and 5, 10 and 8, 10 di deazaminopterin compounds and their use for treatment of rheumatoid arthritis and related diseases and preparative process. Also disclosed are 10 alkenyl-(and alkynyl) 10-deazaminopterins also disclosed for treatment of rheumatoid arthritis and for leukemia and ascites tumors and preparative process.
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- Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin
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Successive alkylation of dimethyl homoterephthalate with propargyl bromide and 2,4-diamino-6-(bromomethyl)pteridine followed by ester saponification at room temperature afforded 2,4-diamino-4-deoxy-10-carboxy-10-propargyl-10- deazapteroic acid. The 10-COOH was readily decarboxylated by heating in DMSO at a temperature of only 120 °C to yield the diamino-10-propargyl-10- deazapteroic acid intermediate. Coupling with diethyl L-glutamate and ester hydrolysis gave the title compound. The 10-propargyl analogue was about 5 times more potent than MTX as an inhibitor of growth in L1210 cells, but was only one-third as potent as an inhibitor of DHFR from L1210. The analogue was transported inward very effectively in L1210 cells showing a 10-fold advantage over MTX. At a dose of 36 mg/kg the 10-propargyl compound caused shrinkage of the E0771 solid murine mammary tumor to only 1% of untreated controls.
- DeGraw,Colwell,Piper,Sirotnak
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p. 2228 - 2231
(2007/10/02)
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