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Vatalanib succinate intermediate and synthesis method and application thereof

A synthesis method and technology for reactants, applied in the field of medicine, can solve the problems of difficult control of high temperature solid-phase reaction conditions, unfavorable stirring, and excessive viscosity, and achieve the effects of good industrial prospects, short reaction time, and few reaction steps.

Inactive Publication Date: 2020-02-14
安徽红杉生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The high-temperature solid-state reaction conditions are not easy to control, and the reactants are too viscous after melting, which is not conducive to stirring, and carbonization often occurs

Method used

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  • Vatalanib succinate intermediate and synthesis method and application thereof
  • Vatalanib succinate intermediate and synthesis method and application thereof
  • Vatalanib succinate intermediate and synthesis method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] like figure 1 As shown, the present embodiment 1 provides a kind of synthetic method of 1-chloro-4-(4-pyridylmethyl)naphthalene, comprising the following steps: step S1, with 2-(1-aminoethyl)benzene Carbonitrile is used as the initial raw material to perform multiple reactions successively; and step S2, rotary evaporation and vacuum pumping to obtain the 1-chloro-4-(4-pyridylmethyl)phthalazine.

[0034] Specifically, the synthesis method of Example 1 selects 2-(1-aminoethyl)benzonitrile as the initial raw material, which is cheap and easy to obtain, avoids the use of lithium salts, avoids carbonization, and has fewer reaction steps, and the reaction The time is short, which is conducive to industrialized production. The chemical purity of the product can reach more than 90.582%, and the yield can reach more than 79.25%, which has good industrial prospects.

[0035] Further, the reaction formula of the first reaction is:

[0036]

[0037] As an optional implementat...

Embodiment 2

[0053] On the basis of Example 1, this Example 2 provides a 1-chloro-4-(4-pyridylmethyl)naphthalene, and the 1-chloro-4-(4-pyridylmethyl)bis The structural formula of aziridine is:

[0054]

[0055] Regarding the component content and specific implementation process of 1-chloro-4-(4-pyridyl)naphthyridine, please refer to the relevant discussion in Example 1, and will not repeat them here.

Embodiment 3

[0057] On the basis of Example 1, this Example 3 provides a first reactant for the synthesis of 1-chloro-4-(4-pyridylmethyl)naphthalene, the structural formula of the first reactant is:

[0058]

[0059] For the content of the components of the first reactant and the specific implementation process, please refer to the relevant discussion in Example 1, and details will not be repeated here.

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to a vatalanib succinate intermediate and a synthesis method and application thereof. The synthesis method comprisesthe following steps: taking 2-(1-aminoethyl)benzonitrile as an initial raw material, and successively carrying out multiple reactions; and performing filtering, rotary evaporation and vacuumizing to obtain 1-chloro-4-(4-pyridylmethyl)phthalazine. According to the synthesis method, 2-(1-aminoethyl)benzonitrile is selected as the initial raw material, the raw material is cheap and easy to obtain, the use of a lithium salt is avoided, the carbonization phenomenon is avoided, reaction steps are few, a reaction time is short, and industrial production is facilitated. The chemical purity of the product can reach 90.582% or more, the yield can reach 79.25% or more, and the method has a relatively good industrial prospect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a vatalanib succinate intermediate and a synthesis method and application thereof. Background technique [0002] The code name of vatalanib succinate is PTK787, ZK222584, CGP79787D, etc., and its chemical name is N-(4-chlorophenyl)-4-(4-pyridylmethyl)phthalazin-1-amine succinate , the drug is a selective VEGF receptor tyrosine kinase inhibitor jointly developed by Novartis and Schering AG, which can block the phosphorylation process of VEGF and PDGF receptor signal transduction. The results of pharmacological tests prove that vatalanib succinate is a small molecule VEGF receptor tyrosine kinase inhibitor with strong safety, good tolerance and excellent pharmacokinetic properties, and can be administered orally for a long time. At present, vatalanib succinate is in the T-phase clinical stage, and it is used for the treatment of prostate cancer, colon and rectal cancer, renal cel...

Claims

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Application Information

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IPC IPC(8): C07D401/06C07D237/32C07F3/06C07C55/10
CPCC07C55/10C07D237/32C07D401/06C07F3/06
Inventor 高仰哲吴法浩李钢王志航
Owner 安徽红杉生物医药科技有限公司
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