A kind of preparation method of high-efficiency and low-toxicity vasopressin antagonist drug

A halogen and compound technology, which is applied in the field of preparation of tolvaptan, a selective non-peptidin arginine vasopressin V2 receptor antagonist, can solve problems such as difficulties in the preparation of analogues
CN105753735BActive Publication Date: 2020-01-17上海天慈中商药业有限公司

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
上海天慈中商药业有限公司
Publication Date
2020-01-17

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Abstract

The invention provides a preparation method of a high-efficiency low-toxicity pitressin antagonist. Specifically, the invention provides a compound having the formula A shown in the description, and a method for preparing tolvaptan through the compound having the formula A. All groups in the formula are defined in the description. The method has advantages of environmental protection, available raw materials, and high overall yield, and is suitable for industrial preparation of tolvaptan.
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Description

technical field

[0001] The invention belongs to the technical field of chemical pharmacy, and relates to a selective non-peptide arginine vasopressin (AVP) V 2 Method for preparing tolvaptan for receptor antagonists. Background technique

[0002] Tolvaptan English name Tolvaptan, trade name: Samsca. The drug is a selective vasopressin V 2 Receptor antagonists that prevent AVP from interacting with V at the distal end of the nephron 2 Receptor binding increases water excretion in urine, but does not change urine sodium and potassium secretion and blood potassium value, reduces urine osmotic pressure, and increases blood sodium value, so it is clinically used for the treatment of liver cirrhosis, heart failure, Hypervolemic and isovolemic hyponatremia due to syndrome of inappropriate antidiuretic hormone secretion (SIADH). The drug is well tolerated, does not disrupt electrolyte balance, and has mild adverse reactions. Tolvaptan was approved by the FDA in 2009 as an oral ...

Claims

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