Detection and analysis method for quality control of raltitrexed synthesis

Abstract

The invention discloses a detection and analysis method for quality control of raltitrexed synthesis. The method includes purity detection of a starting material 6-bromomethyl-3,4-dihydro-2-methyl-quinazoline-4-one, purity detection of a starting material 5-nitro-2-thiophenecarboxylic acid, raltitrexed content determination, content detection of the 6-bromomethyl-3,4-dihydro-2-methyl-quinazoline-4-one, 6-hydroxymethyl-3,4-dihydro-2-methyl-quinazoline-4-one and the 5-nitro-2-thiophenecarboxylic acid in raltitrexed, and raltitrexed enantiomer detection. The method of the invention has the characteristics of high sensitivity and strong specificity, and can rapidly and accurately perform quality control on a synthesis process of the raltitrexed, thereby ensuring the quality of raltitrexed bulk medicine.

Description

technical field

[0001] The invention belongs to the field of drug analysis, in particular to a detection and analysis method for quality control of raltitrexed synthesis. Background technique

[0002] Raltitrexed was developed by the Cancer Research Unit at the Royal Marsden Hospital in the UK in collaboration with Zeneca. It is a thymonucleotide synthase inhibitor, a derivative of folic acid, used in the treatment of patients with advanced colorectal cancer. It was launched in the UK for the first time in 1996 under the trade name Tomudex, and it was launched in France and other countries in the same year. As a first-line treatment drug for advanced colorectal cancer, it has the advantages of less toxic and side effects, convenient administration, and low price, and is in great demand in China.

[0003]

[0004] There are multiple synthetic methods for raltitrexed, and the commonly used synthetic routes are as follows:

[0005]

[0006] In this route, using 5-nitro...

Images