Method for preparing zaltoprofen

Abstract

The invention discloses a method for preparing zaltoprofen. The method, which is simple in operation route, environmentally-friendly and suitable for industrial mass production, can realize industrialization. The zaltoprofen is a non-steroid anti-inflammatory medicament having effects of relieving inflammation, pain and heat.

Description

technical field The invention relates to the technical field of pharmaceutical synthesis technology, in particular to an organic synthesis method which is simple to operate, environmentally friendly and suitable for large-scale industrial production, and specifically relates to a new preparation method of zaltoprofen. Background technique The chemical name of zaltoprofen is 10,11-dihydro-α-methyl-10-oxydibenzo[b,f]thiapine-2-acetic acid, the main mechanism of action is through the metabolism of arachidonic acid It hinders cyclooxygenase and inhibits the synthesis of prostaglandins. Others play a role in membrane stabilization by inhibiting leukocyte migration and inhibiting the release of lysosomal enzymes. Inhibition of prostaglandin synthesis, selective and strong inhibition of prostaglandin production in cells (in vitro), inhibition of prostaglandin synthesis in gastric tissue is weaker than that of indomethacin, and slightly inhibits excretion of prostaglandins in urine....

AI Technical Summary

Problems solved by technology

Routes 1, 2, and 3 all use o-chloroacetophenone as the starting material to synthesize the parent ring 10,11-dihydrodibenzo[b,f]thiazepine-10 through condensation, rearrangement, and hydrolysis. -ketone, and then introduce isopropionic acid; 4,5,6,7,8 routes are to use methyl o-chlorophenylacetate as the starting material to introduce side chains and then cyclize, and the above-mentioned 8 routes have a long reaction time , the post-processing operation is complicated

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