Solid-phase synthesis method of human relaxin-2

Abstract

The invention discloses a solid-phase synthesis method of human relaxin-2, which comprises the following steps of: 1) solid-phase synthesis of a single-ring chain A; 2) solid-phase synthesis of a chain B; and 3) chemical synthesis of the human relaxin-2. By using the method to produce the human relaxin-2, the yield is high and can be up to 74-82%. The method disclosed by the invention has the advantages of convenient production steps and no impurity production in the production process, and effectively solves the problems that the solid-phase synthesis of the chain B of the human relaxin-2 isdifficult to complete by the Fmoc strategy and the synthesis process is too complicated.

Description

technical field

[0001] The invention relates to a synthetic method of human relaxin-2, in particular to a solid-phase synthetic method of human relaxin-2. Background technique

[0002] Human relaxin-2, usually abbreviated as RLN2, and the drug name is also named Relaxin, namely relaxin, is a polypeptide hormone found in the human body. Human relaxin-2 consists of two chains, the A chain contains 24 amino acids and has intra-chain disulfide bonds, the B chain contains 29 amino acids, and the A chain and the B chain are connected by two disulfide bonds. Its structural formula is as follows:

[0003]

[0004] A series of studies in recent years have found that human relaxin-2 has a significant therapeutic effect on cardiovascular diseases such as heart failure, and can expand blood vessels in the systemic circulation, expand renal blood vessels, and increase arterial compliance. U.S. Patent US5166191 has disclosed the method patent of human relaxin for the treatment of card...

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