Method for preparing 2-oxygen-2,4,5,6,7,7alpha-hexahydro thieno [3,2-c]pyridine

Abstract

The invention relates to a preparation method for 2-oxygen-2, 4, 5, 6, 7, 7alpha-hexahydro thiophene and (3, 2-c) pyridine, which includes the following steps: a compound of the following formula or the corresponding salt under the acidic condition is hydrolyzed and a target product is obtained by post-processing; wherein, R stands for alkyl. The method adopts the existing ordinary compound materials, and obtains 2-oxygen-2, 4, 5, 6, 7, 7alpha-hexahydro thiophene and (3, 2-c) pyridine by one step of hydrolysis reaction. Meanwhile, the method has the advantages of the high yield, the mild reaction condition, and is very suitable for the industrial mass production.

Description

Preparation method of 2-oxo-2,4,5,6,7,7α-hexahydrothieno[3,2-c]pyridine technical field The invention relates to a preparation method of 2-oxo-2,4,5,6,7,7α-hexahydrothieno[3,2-c]pyridine. Background technique Thrombosis can cause ischemia and infarction of major organs, and can also cause edema and venous insufficiency, thereby causing various dysfunctions. Representative antithrombotic drugs currently in clinical use are aspirin, clopidogrel, and asimumab. The effect of clopidogrel is stronger than that of aspirin and has less side effects. It is clinically used to treat atherosclerosis, acute coronary syndrome, and prevent in-stent restenosis and thrombotic complications after coronary stent implantation. Prasugrel is a tetrahydrothienopyridine compound similar to clopidogrel. It has shown better activity, tolerance and safety than clopidogrel in the third phase of clinical trials, and it is expected to become a good antithrombotic drug. The chemical name of prasugrel ...

AI Technical Summary

Problems solved by technology

It can be seen from the above method that the compound of formula (I) is an important raw material for the preparation of prasugrel, and the problem that exists now is that there is no cheap industrial product to buy

The reaction conditions are very harsh, requiring a low temperature of -40°C. At the same time, n-butyllithium is flammable and explosive, which will bring danger to large-scale production.

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