Preparation method and application of melphalan dimmer hydrochloride

A technology of dimer and melphalan, which is applied in the field of preparation and application of melphalan dimer hydrochloride, can solve problems such as unretrieved, and achieve improved stability, mild and controllable preparation conditions, and reaction conditions Gentle and Controllable Effect

Inactive Publication Date: 2018-06-29
HAINAN SIMCERE PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Regarding melphalan dimer hydrochloride (compound shown in formula 3), the specific preparation of this compound has not yet been retrieved

Method used

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  • Preparation method and application of melphalan dimmer hydrochloride
  • Preparation method and application of melphalan dimmer hydrochloride
  • Preparation method and application of melphalan dimmer hydrochloride

Examples

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preparation example Construction

[0035] Preparation of melphalanyl chloride hydrochloride:

[0036]

Embodiment 1

[0038] Add the compound of formula 1 (1g) into the reaction bottle, then add 10ml of dichloromethane, 0.2ml of N,N-dimethylformamide, stir, cool down to 5°C, add thionyl chloride dropwise, react for 1 hour, concentrate The solvent was removed to obtain 0.82 g of compound 2.

Embodiment 2

[0040] Add the compound of formula 1 (1g) into the reaction flask, then add 12ml of dichloromethane, 0.2ml of N,N-dimethylformamide, stir, raise the temperature to 40°C, add dropwise oxalyl chloride, react for 2 hours, concentrate to remove the solvent , 0.68 g of compound 2 was obtained.

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Abstract

The invention relates to a preparation method and application of melphalan dimmer hydrochloride, and specifically relates to a preparation method and application of 4-[2-[[4-bi(2-chloroethyl)amino]-Lphenylalanine ethoxycarbonyl](2-chloroethyl)-amino]-L-phenylalanine hydrochloride (namely melphalan dimmer hydrochloride). The compound can serve as a reference substance for detecting hydrochloric acid melphalan related substances, and is used for purity control of hydrochloric acid melphalan raw materials or preparations.

Description

technical field [0001] The present invention relates to 4-[2-[[4-bis(2-chloroethyl)amino]-L-phenylalanine ethyl ester base](2-chloroethyl)amino]-L-phenylalanine hydrochloride The preparation method and application of the salt (ie melphalan dimer hydrochloride), the melphalan dimer hydrochloride is an important impurity in the melphalan hydrochloride raw material or preparation process. Background technique [0002] Melphalan, also known as 4-(bis(2-chloroethyl)-amino)-L-phenylalanine) and its hydrochloride are known antineoplastic agents. On January 17, 1964, 2mg melphalan tablet was launched in the United States, and its active ingredient was melphalan; on November 18, 1992, melphalan hydrochloride injection ALKERAN was launched in the United States, and the active ingredient was melphalan hydrochloride Salt. Due to the existence of the phenylalanine group, it is easy to enter into the tumor cells to take effect, thereby effectively inhibiting and preventing the prolifera...

Claims

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Application Information

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IPC IPC(8): C07C227/18C07C229/42G01N33/15
CPCG01N33/15C07C227/18C07C229/42
Inventor李瑞王浩
OwnerHAINAN SIMCERE PHARMA CO LTD