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Synthesis method of valganciclovir as hydrochloric acid

A kind of valganciclovir hydrochloride, the technology of synthetic method, is applied in the preparation field of antiviral drug, can solve the problem such as active reagent is not easy to obtain, synthetic route is long, achieves few synthetic steps, safety improves, and is suitable for industrialized production Effect

Inactive Publication Date: 2014-05-14
江苏盈科生物制药有限公司
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Problems solved by technology

Finally, it is also very important to select a suitable active reagent that can be esterified with ganciclovir. Most of the active reagents are not easy to obtain and need to be synthesized, making the synthetic route longer

Method used

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  • Synthesis method of valganciclovir as hydrochloric acid
  • Synthesis method of valganciclovir as hydrochloric acid

Examples

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Comparison scheme
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Embodiment

[0025] The synthetic technique of embodiment valganciclovir hydrochloride

[0026] (1) Preparation of N-benzyloxycarbonyl-valine (Cbz-Va)

[0027] Dissolve L-valine in sodium hydroxide solution, cool in an ice-salt bath under magnetic stirring, keep the internal temperature not higher than 10°C, add benzyloxychloromethyl ester dropwise to the above solution, and continue cooling in an ice-water bath after adding Stirred under low temperature for 2h, then stirred at room temperature for 6h, and TLC checked that the starting material disappeared. The basic reaction mixture was extracted with chloroform to remove excess benzyloxychloromethyl ester or its decomposed benzyl alcohol. The aqueous layer was neutralized with hydrochloric acid to pH = 2 under cooling in an ice-water bath, extracted with CHC13, washed with water, dried over anhydrous Na2SO4, and evaporated to dryness to obtain the product.

[0028] (2) 2-[(2-amino-1,6-dihydro-6-oxo-purine-9-)methoxy]-3-hydroxyl-1-propy...

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Abstract

The invention relates to a preparation method of valganciclovir as hydrochloric acid. The preparation method comprises the steps of dehydrating and condensing ganciclovir and amino-protected valine in an N, N-dimethyl formamide solution under the action of dicyclohexylcarbodiimide to obtain a mixture of a monoester precursor G1 and a biester precursor G2; separating and purifying to obtain the monoester precursor G1; carrying out hydrogenation deprotection on G1 to obtain a target object, namely valganciclovir G3.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a preparation method of an antiviral drug. Background technique [0002] Valganciclovir (Valganciclovir) is a synthetic α'-deoxyguanosine analog, which is a prodrug of Ganciclovir (Ganciclovir), which can greatly reduce the toxicity of Ganciclovir. The drug was developed by Roche in Switzerland and first launched in the United States in 2001. It is suitable for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients (approved in 2001) and kidney transplantation for the risk of cytomegalovirus (CMV) disease long-term treatment of patients (approved 2010). Its chemical name is (S)-2-amino-3-methylbutanoic acid (R,S)-2-[(2-amino-6-oxo-1,6-dihydro-9H-purine-9- Base) methoxy] -3-hydroxypropyl ester hydrochloride, CAS No. 175865-59-5, English name Valganciclovir hydrochloride, trade name Valcyte, molecular formula C14H22N6O5HCL, molecular weight 390.83, the structural formula is as ...

Claims

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Application Information

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IPC IPC(8): C07D473/18
CPCC07D473/18
Inventor 李旭胡全
Owner 江苏盈科生物制药有限公司
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