Solid-phase synthesis process of angiotensinamide as well as intermediate and application thereof

A technology of blood-increasing hormone and condensation reaction, which can be used in medical preparations containing active ingredients, drug combinations, cardiovascular system diseases, etc., and can solve problems such as difficulty in complete dissociation
CN103374058AActive Publication Date: 2013-10-30SPH NO 1 BIOCHEM & PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SPH NO 1 BIOCHEM & PHARMA CO LTD
Publication Date
2013-10-30

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Abstract

The invention discloses a process for producing angiotensinamide with a chemical structure of H-Asn-Arg-Val-Tyr-Val-His-Pro-Phe-OH by adopting solid-phase synthesis technology and an intermediate adopted in the method. The method comprises the following steps of: (a) preparing protected angiotensinamide with a chemical structure of R1-Asn-Arg(R2)-Val-Tyr(R3)-Val-His(R4)-Pro-Phe-R5, wherein R1 is an amino protecting group, R2, R3 and R4 are side chain protecting groups, and R5 is carboxyl resin; and (b) under the action of a cutting reagent, deprotecting and separating the protected angiotensinamide obtained in the step (a) from the resin to generate angiotensinamide with the chemical structure of H-Asn-Arg-Val-Tyr-Val-His-Pro-Phe-OH. The method for synthesizing angiotensinamide is environment-friendly and efficient, has low requirements for equipment, and can be applied to large-scale industrial production.
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Description

technical field

[0001] The invention belongs to the field of pharmaceutical synthesis technology. More specifically, the present invention relates to a solid-phase synthesis process of vasopressin, its intermediates and applications. Background technique

[0002] Hypertensin is a blood pressure-increasing drug, CAS registration number 53-73-6, English name angiotensinamide or [Asn 1 , Val 5 ]-angiotensin II, the chemical structure is H-Asn-Arg-Val-Tyr-Val-His-Pro-Phe-OH (2003 National Drug Standard WS-10001-(HD-1448)-2003). Vasopressin is used for hypotension caused by trauma or postoperative shock and general anesthesia or lumbar anesthesia, etc., can prevent or treat perioperative hypotension, and can be used as emergency medicine to treat shock hypotension, and can also be used to treat vascular tension In case of overdose of the conversion enzyme inhibitor and conventional treatment is ineffective.

[0003] When cardiovascular homeostasis is threatened, neurohormonal...

Claims

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