Preparation method for dual inhibitor LCZ696 of angiotensin II receptor and neprilysin

A technology of dual inhibitors and angiotensin, which is applied in chemical instruments and methods, preparation of organic compounds, preparation of carboxylic acid amides, etc., can solve problems such as harsh conditions, complicated process, and low yield

Inactive Publication Date: 2015-12-23
TAILITE MEDICINE HUBEI
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Problems solved by technology

[0003] The present invention proposes a preparation method of LCZ696, an angiotensin II receptor and neprilysin receptor dual inhibitor, to solve the probl...

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  • Preparation method for dual inhibitor LCZ696 of angiotensin II receptor and neprilysin
  • Preparation method for dual inhibitor LCZ696 of angiotensin II receptor and neprilysin
  • Preparation method for dual inhibitor LCZ696 of angiotensin II receptor and neprilysin

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Embodiment Construction

[0067] The technical solutions in the embodiments of the present invention will be clearly and completely described below. Obviously, the described embodiments are only some of the embodiments of the present invention, but not all of them. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0068] A preparation method of angiotensin II receptor and neprilysin receptor dual inhibitor LCZ696, first preparing Valsartan (Valsartan), AHU-377 or AHU-377 calcium salt, and then mixing and stirring the two to prepare LCZ696.

[0069] Please refer to the preparation route, the preparation steps of Valsartan (Valsartan) are as follows:

[0070] Step 1), preparation and refining of 5-(4'-methyl-biphenyl-2-)tetrazolium (V-2)

[0071] In a reaction flask, add 19.3 g of 2-cyano-4'-methyl-biphenyl (V-1, 100 mmol) and 17.9 g of triet...

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Abstract

The invention specifically relates to a preparation method for a dual inhibitor LCZ696 of angiotensin II receptor and neprilysin, which belongs to the technical field of drug synthesis. The preparation method comprises the following steps: preparing valsartan and AHU-377 or AHU-377 calcium salt at first; and then mixing valsartan with AHU-377 or AHU-377 calcium salt under stirring so as to prepare LCZ696. The LCZ696 prepared in the invention has good quality and high purity; and the preparation method has the advantages of simplicity, low energy consumption, low cost and suitability for large batch production.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and in particular relates to a preparation method of LCZ696, an angiotensin II receptor and neprilysin receptor dual inhibitor. Background technique [0002] LCZ696 is a dual neprilysin and angiotensin receptor inhibitor developed by Novartis, which combines two components such as valsartan and AHU-377, among which valsartan can improve vasodilation, Stimulates the body to excrete sodium and water, while AHU-377 blocks 2 peptides that threaten to lower blood pressure. The production of LCZ696 in the prior art adopts the seed crystal method. The production conditions of the seed crystal method are relatively harsh, the synthesis process is relatively complicated, and the yield is low. Contents of the invention [0003] The present invention proposes a preparation method of LCZ696, a dual inhibitor of angiotensin II receptor and neprilysin receptor, to solve the problems of complex proces...

Claims

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Application Information

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IPC IPC(8): A61K31/41A61K31/216A61P9/08A61P7/10A61P9/12C07D257/04C07C233/47C07C231/02C07C231/12
Inventor 刘明星王瑜吴建宏
Owner TAILITE MEDICINE HUBEI
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