Process for preparation of tirofiban hydrochloride

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

Active Publication Date: 2009-09-09
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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

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  • Process for preparation of tirofiban hydrochloride
  • Process for preparation of tirofiban hydrochloride
  • Process for preparation of tirofiban hydrochloride

Examples

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Embodiment Construction

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

[0022] 1. The 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 ...

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Abstract

The invention discloses a method suitable for industrial production of tirofiban hydrochloride, a medicine for treating angina pectoris.

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

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/22
Inventor 赵志全彭立增
Owner LUNAN PHARMA GROUP CORPORATION
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