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Crystal form of neurokinin-1 antagonist and preparation method thereof

A technology of crystal form and solvent, applied in the field of crystal form of neurokinin-1 antagonist, can solve the problems of difficult filtration, poor product stability, easy agglomeration, etc.

Pending Publication Date: 2022-06-28
SHANGHAI SHENGDI PHARMA CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Generally speaking, amorphous pharmaceutical products have no regular crystal structure and often have other defects, such as poor product stability, fine crystallization, difficult filtration, easy agglomeration, poor fluidity, etc.

Method used

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  • Crystal form of neurokinin-1 antagonist and preparation method thereof
  • Crystal form of neurokinin-1 antagonist and preparation method thereof
  • Crystal form of neurokinin-1 antagonist and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1: Preparation of compound of formula II

[0070]

[0071] first step:

[0072]

[0073] in N 2 Under protection, compound 1 (2.43g, 4.86mmol, 1eq) was weighed in a 100mL three-necked flask, dissolved in dichloromethane (36mL), added diisopropylethylamine (5g, 38.76mmol, 8eq), cooled to - At 30° C., trimethylchlorosilane (1.36 g, 12.52 mmol, 2.6 eq) was added, and the mixture was stirred at room temperature for 2 h. Cool to -25°C, add dropwise a solution of chloromethyl chloroformate (0.77g, 6mmol, 1.23eq) in dichloromethane, control the temperature at -20°C to -5°C and stir until the reaction is complete, pour the reaction solution into ice water , separation, extraction with dichloromethane, adding water and 1N hydrochloric acid solution, separation, washing with brine, saturated aqueous sodium bicarbonate solution and brine successively, drying over anhydrous sodium sulfate, filtration, and concentration to obtain 3.0 g of yellow gum , the yield was ...

Embodiment 2

[0119] Example 2: Preparation of Crystal Form of Compound A of Formula II

[0120] About 100 mg of the compound shown in formula II was weighed, added to 1 mL of diethyl ether, stirred at room temperature to dissolve the clear liquid, slurried to separate out a solid, and vacuum-dried to obtain the crystal form A of the compound shown in formula II after centrifugation, and its characteristic peak positions are shown in Table 3:

[0121] Table 3: XRD characteristic peak positions of crystal form A

[0122]

[0123]

Embodiment 3

[0124] Example 3: Stability investigation of crystal form A

[0125] The crystal form of compound A of formula II was placed under the condition of 4°C to investigate its stability.

[0126] Table 4

[0127]

[0128] The results showed that the crystal form A had good physical and chemical stability under the stability condition of 4 ℃ for 3 months.

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Abstract

The invention relates to a crystal form of a neurokinin-1 antagonist and a preparation method of the crystal form. Specifically, the invention relates to an A crystal of a compound shown as a formula II and a preparation method thereof. The novel crystal form disclosed by the invention has good physicochemical properties and is more beneficial to clinical treatment.

Description

technical field [0001] The present disclosure relates to a crystalline form of a neurokinin-1 antagonist, in particular to the crystalline form A of the compound of formula II and a preparation method. Background technique [0002] Tachykinins are peptide ligands for neurokinin receptors. Neurokinin receptors, such as NK1, NK2 and NK3, are involved in various biological processes. They can be found in the nervous and circulatory systems of mammals as well as in surrounding tissues. Accordingly, modulation of such receptors has been investigated for potential treatment or prevention of various physiological disorders, conditions or diseases in mammals. [0003] On the other hand, drug hemolysis is caused by the massive destruction of red blood cells caused by immune factors after the drug enters the human body. Clinically, hemolytic phenomena such as anemia, jaundice, soy sauce and urine appear. Drug-induced hemolytic anemias can be divided into the following three types: ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561A61K31/675A61P11/00A61P11/06A61P29/00A61P17/00A61P27/02A61P25/22A61P25/24A61P25/00A61P25/32A61P25/08A61P25/18A61P25/28A61P3/04A61P3/10A61P9/10A61P25/04A61P13/10A61P13/00A61P43/00A61P1/00A61P1/12A61P1/08
CPCC07F9/6561A61P11/00A61P11/06A61P29/00A61P17/00A61P27/02A61P25/22A61P25/24A61P25/00A61P25/32A61P25/08A61P25/18A61P25/28A61P3/04A61P3/10A61P9/10A61P25/04A61P13/10A61P13/00A61P43/00A61P1/00A61P1/12A61P1/08C07B2200/13
Inventor 吴琪杨俊然杜振兴王捷
Owner SHANGHAI SHENGDI PHARMA CO LTD
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