2-hydrazino adenosine and preparation method thereof

A technology of hydrazinoadenosine and hydrazinoadenosine dihydrate, which is applied in the field of medicine and can solve the problems of cumbersome preparation and purification, high cost, and low yield
CN107056860AInactive Publication Date: 2017-08-18南京海辰药业股份有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
南京海辰药业股份有限公司
Publication Date
2017-08-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the field of pharmaceutical chemical engineering and relates to 2-hydrazino adenosine and a preparation method thereof. According to the method disclosed by the invention, a chemical compound shown as a formula II reacts with hydrazine hydrate in the presence or the absence of a polar solvent and the reaction formula is shown as follows. The 2-hydrazino adenosine crystal prepared by adopting the method is high in yield, high in purity and low in cost; the method has the advantages of being friendly to the environment, simple and convenient to operate and easy in industrial scale-up and has a very good industrial application prospect; and the 2-hydrazino adenosine can be used for preparing an adenosine receptor agonist, i.e. regadenoson.
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Description

technical field

[0001] The invention belongs to the technical field of medicine, and in particular relates to a new crystal form of 2-hydrazinoadenosine, a key intermediate of an adenosine receptor agonist Regadenoson, and a preparation method thereof. Background technique

[0002] 2-hydrazinoadenosine is a key intermediate in the synthesis of adenosine receptor agonist Regadenoson.

[0003]

[0004] Regadeson is a selective A drug jointly developed by American CV Pharmaceuticals and Astellas. 2a Adenosine receptor agonists, which have been marketed in the United States and Europe, are mainly used as coronary vasodilators for myocardial perfusion imaging. Prior art (WO00 / 78779, WO2007092372, US7183264, Journal of Medicinal Chemistry, 35 (24), 4557-61) methods for preparing 2-hydrazinoadenosine are all 2-halo (fluorine, chlorine, iodine) substituted adenosine Prepared by reacting with hydrazine hydrate. Moreover, only 2-hydrazinoadenosine was obtained in the description...

Claims

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