Asymmetric oxidation synthesis of esomeprazole sodium:research advances / 国际药学研究杂志

Esomeprazole sodium is a widely used proton pump inhibitor which is mainly applied to the treatment of gastric ul-cer,duodenal ulcer,digestive esophagitis and gastritis. By reviewing the literature over the past decade on the asymmetric oxidation of esomeprazole sodium ,the paper summarizes the synthetic process and focuses on the comparison of the critical steps. To choose suit-able chiral catalyst to reduce the cost of synthesis of esomeprazole sodium,this paper compares beyond the yield,enantioselectivity and other aspects. The conclusion is that the catalysts used in the most of oxidation systems are with a large load and high cost ,and compared with the classical Kagan-Modena system,the Ti-salan catalyst has advantages in the synthesis of esomeprazole sodium,and can be widely used.

Improvement of the synthesis of gefitinib / 中国药学杂志

OBJECTIVE: To synthesize gefitinib. METHODS: Gefitinib was synthesized from vertraldethyde via nitration, hydrolysis, conversion of aldehyde to nitrile, condensation with N-(3-chloropropyl) morpholine, conversion of nitrile to amide, reduction, then cyclization to give 7-methoxy-6-(3-morpholinopropoxy) -3, 4-dihydroquinazolin-4-one, which was finally subjected to chlorination and condensation with 3-chloro-4-fluoroaniline. RESULTS: The chemical structure of the target compound was confirmed by MS, 1H-NMR and 13C-NMR. CONCLUSION: This article provides a novel and more reasonable process for the manufacturing of gefitinib.