cas 146464-91-7, 6-Pteridinepropanoic acid, 2,4-diaMino-α-[4-(Methoxycarbonyl)phenyl]-α-2-propyn-1-yl-, Methyl ester

Articles about 146464-91-7Total 11 be found

A suitable industrial production pula Qu Sha method for the preparation of
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 0045-0046

(2017/01/23)

IMPROVED PROCESS FOR THE PREPARATION OF PRALATREXATE
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 0149

(2015/07/15)

PROCESS FOR PRALATREXATE
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; 7

(2014/05/24)

PROCESS FOR PREPARATION OF AN ANTIFOLATE AGENT
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 0067

(2014/01/07)

PROCESSES AND INTERMEDIATES FOR PREPARING PRALATREXATE
Processes for preparing and purifying Pralatrexate are described in the present application, as well as intermediates in these processes, and salts and solid state forms of the Pralatrexate intermediates.
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Page/Page column 00110

(2013/07/05)

Optically Pure Diastereomers of 10-Propargyl-10-Deazaaminopterin and Methods of Using Same
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)

Treatment of T-cell lymphoma using 10-propargyl-10-deazaaminopterin
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)

Synthesis and in vitro antitumor activity of new deaza analogues of the nonpolyglutamatable antifolate Nα-(4-amino-4-deoxypteroyl)-Nδ- hemiphthaloyl-L-ornithine (PT523)
Details are disclosed for the synthesis of Nα-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-N δ-hemiphthaloyl-L-ornithine (2) and Nα-[4-[5-(2,4-diaminoteridin-6-yl)pent-1-yn-4-yl]benzoyl]-N δ-hemiphthaloyl-L-
Vaidya, Chitra M.,Wright, Joel E.,Rosowsky, Andre
p. 1690 - 1696
(2007/10/03)

Antiinflammatory and antineoplastic 5-deazaaminopterins and 5,10-dideazaaminopterins
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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(2008/06/13)

Process for preparing 10-deazaaminopterins and 5,10-and 8,10-dideazaaminopterins from pteroic dicarboxylic acid diesters
A process is provided for the preparation of 10-deazaaminopterins and 5,10- and 8,10-dideazaaminopterins starting from the corresponding homoterephthalic acid diester coupling the corresponding dicarboxylic acid diester having the formula: STR1 with the c
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(2008/06/13)

Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin
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
p. 2228 - 2231
(2007/10/02)