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Leuprorelin synthesis process

A technology of leuprolide and synthesis technique, applied in the field of synthesis technique of leuprolide, can solve problems such as being unsuitable for large-scale production, complicated production process, low production efficiency, etc., and achieves the improvement of single-pass conversion rate and product. Productivity, overcoming the effect of many processes, and improving work efficiency

Inactive Publication Date: 2016-06-08
吕艳
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Problems solved by technology

In the current leuprolide synthesis process method, the technical process is not easy to implement, the resulting leuprolide finished product has low purity, the single-pass conversion rate of the reactant is low, the production process is complicated, the production efficiency is low and the cost is high, so it is not suitable for large-scale production. mass production

Method used

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Experimental program
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Embodiment

[0014] The synthetic technique of the leuprolide of the present embodiment comprises the following steps:

[0015] (1) Fmoc-Pro-HMPB-AM resin was obtained from Fmoc-Pro-OH and HMPB-AM resin with a substitution degree of 0.9 mmol / g as starting materials;

[0016] (2) The Fmoc-Pro-HMPB-AM resin was coupled one by one by the Fmoc / tBu solid-phase method to link amino acids with protective groups one by one, and the side chain fully protected leuprolide precursor peptide-HMPB-AM was synthesized resin;

[0017] (3) Cleavage of fully protected side chain leuprolide precursor peptide-HMPB-AM resin to obtain leuprolide precursor peptide with fully protected side chain;

[0018] (4) The side chain fully protected leuprolide precursor peptide was ethilated to obtain the side chain fully protected leuprolide;

[0019] (5) The leuprolide crude peptide is obtained by removing the side chain protecting group for fully protected leuprolide;

[0020] (6) The crude leuprolide peptide was sep...

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Abstract

The present invention discloses a leuprorelin synthesis process, which comprises: 1) adopting Fmoc-Pro-OH and a HMPB-AM resin as starting raw materials to obtain a Fmoc-Pro-HMPB-AM resin; 2) carrying out sequential coupling synthesis of a side chain full protection leuprorelin precursor peptide-HMPB-AM resin; 3) cutting to obtain a side chain full protection leuprorelin precursor peptide; 4) carrying out ethylamine treatment on the side chain full protection leuprorelin precursor peptide to obtain side chain full protection leuprorelin; 5) carrying out a side chain protection group removing reaction on the side chain full protection leuprorelin to obtain a leuprorelin crude product; and 6) separating and purifying the leuprorelin crude product, and carrying out freeze drying to obtain the leuprorelin fine peptide. According to the present invention, the leuprorelin synthesis process has characteristics of large-scale production capacity, easy operation, stable process, low production cost, considerable economic and practical value, and broad application prospects, wherein the total yield exceeds 50%.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and in particular relates to a synthesis process of leuprolide. Background technique [0002] The effect of leuprolide is the same as that of buserelin. Repeated administration of large doses of luteinizing-releasing hormone (LH-RH) or its highly active derivative leuprolide acetate can produce a transient excitatory effect on the pituitary-gonadal system immediately after the first administration (acute effect), It then inhibits the production and release of gonadotropins by the pituitary gland. It also further suppresses the response of the ovaries and testes to gonadotropins, thereby reducing the production of estradiol and testosterone (chronic effect). In the current leuprolide synthesis process method, the technical process is not easy to implement, the resulting leuprolide finished product has low purity, the single-pass conversion rate of reactants is low, the production proces...

Claims

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Application Information

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IPC IPC(8): C07K7/23C07K1/06C07K1/04
CPCY02P20/55
Inventor 吕艳
Owner 吕艳
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