132463-02-6Relevant articles and documents
Synthetic method of leraltrexed
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, (2021/05/05)
The invention provides two method for preparing a compound disclosed as Formula 4. The scheme 1 comprises the following steps: reacting the raw material methyl 5-bromothienyl-2-formate with 6-((methylamino)methyl)-3,4-dihydro-2-methyl-4-oxo-6-quinazoline (compound 1) to obtain methyl 2-[N-(2-methyl-4-oxoquinazolinyl-6-methyl)-N-methyl]-aminothienyl-2-formate, hydrolyzing in an alkaline water solution, and carrying out condensation reaction with diethyl L-glutamate to obtain the compound disclosed as Formula 4. The scheme 2 comprises the following steps: carrying out condensation on the raw material 5-bromothienyl-2-formic acid and di L-glutamate to obtain diethyl N-(5-bromothienyl-2-yl)glutamate, and reacting with a compound disclosed as Formula 1 to obtain the compound disclosed as Formula 4. The invention also provides a method for preparing raltitrexed, which comprises the following steps: hydrolyzing the compound disclosed as Formula 4 in an alkaline water solution, and acidifying with hydrochloric acid to obtain the raltitrexed. The synthesis route has the advantages of fewer reaction steps, low environmental pollution and high product yield, and is simple to operate.
Raltitrexed pharmaceutical composition and preparation method thereof
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, (2018/04/02)
The invention relates to a raltitrexed pharmaceutical composition which is high in safety and a preparation method thereof. The raltitrexed pharmaceutical composition comprises raltitrexed and thiophene related substances, wherein the content of the thiophene related substances is not higher than 0.3%. The raltitrexed pharmaceutical composition is good in safety, effectiveness and stability and can relieve the blood toxicity of the raltitrexed to a certain degree.
New synthesis of thymidylate synthase inhibitor raltitrexed
Cao, Sheng-Li,Wan, Rong,Feng, Yu-Ping
, p. 3519 - 3526 (2007/10/03)
The quinazoline-based inhibitor of thymidylate synthase, Raltitrexed, was synthesized from 2,5-thiophenedicarboxylic acid via monocoupling with diethyl L-glutamate, modified Curtius reaction, N-methylation, removal of Boc-protecting group, condensation with (bromomethyl)quinazolinone and saponification in 18.2% overall yield.