Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Process for preparation of tirofiban hydrochloride

A technology for tirofiban and hydrochloric acid, which is applied in the field of producing tirofiban hydrochloride, can solve the problems of high risk, harsh reaction conditions, troublesome operation, etc., and achieve the effects of less discharge of three wastes, no risk of operation, and easy operation

Active Publication Date: 2006-10-11
LUNAN PHARMA GROUP CORPORATION
View PDF7 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This route still uses n-butyllithium, which also has the problems of high risk, harsh reaction conditions and difficult industrialization, and multiple extractions with different mixed solvents for the post-treatment of the acylation step, the solvent consumption is large, and the operation trouble

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Process for preparation of tirofiban hydrochloride
  • Process for preparation of tirofiban hydrochloride
  • Process for preparation of tirofiban hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0021] The preparation method of the present invention is further described in detail below by way of examples.

[0022] 1. Preparation of 4-(4-piperidinyl)butyl chloride 3:

[0023] Method A: 4-(4-pyridyl) butyl chloride (507 grams, 3 moles), 10% Pd / C (25.4 grams, 5% by weight) were dissolved in 6 liters of ethanol, at a hydrogen pressure of 0.35 MPa and 65 ℃, hydrogenation to complete (about 8 hours). The catalyst was removed by filtration, and the filtrate was concentrated under reduced pressure to obtain a colorless viscous liquid, which was 4-(4-piperidinyl)butyl chloride, about 525 g.

[0024] Method B: 4-(4-pyridyl)butyl chloride (507 g, 3 moles) was dissolved in 6 liters of absolute ethanol, heated to reflux, and sodium metal (575 g, 25 moles) was added. After the reaction, most of the ethanol was evaporated, cooled to room temperature, 500 ml of saturated ammonium chloride aqueous solution was added, extracted with ethyl acetate (500 ml × 3), the ethyl acetate layer...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a process for the industrial production of Tirofiban hydrochloride, a medicament for treating angina.

Description

technical field [0001] The invention relates to a new chemical method for preparing tirofiban hydrochloride. Background technique [0002] Tirofiban hydrochloride (English name: Tirofiban hydrochloride, chemical name: (S)-N-(n-butylsulfonyl)-O-[4-(4-piperidinyl)butane]-L-tyrosine Hydrochloride monohydrate) is a salt compound of a platelet inhibitor. [0003] [0004] In the prior art, EP478328 and EP478363, US522756 first disclose this kind of compound and a kind of synthetic method thereof, take 4-piperidine-2-ethanol as starting material, make 4-(4-N-tert Butyloxycarbonylpiperidinyl) butyl bromide, and then carry out acylation reaction with N-CBZ-L-tyrosine in NaH / DMF, and then react with CH under basic conditions 3 I reaction is esterification, hydrogenation to remove the CBZ protecting group, sulfonamidation, ester hydrolysis, and hydrochloric acid to remove the BOC protecting group to obtain the final product. A total of eleven steps of reaction, the reaction step...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/22
Inventor 赵志全彭立增
Owner LUNAN PHARMA GROUP CORPORATION
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com