Novel process for synthesis of phenoxy diaminopyrimidine compound

A kind of technology of diaminopyrimidine and compound is applied in the field of preparing phenoxydiaminopyrimidine compound or its pharmaceutically acceptable salt, and can solve the problems of complex chemical process, low yield and the like

Pending Publication Date: 2021-02-26
MERCK SHARP & DOHME BV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, currently known methods suffer from various disadvantages, including complex chemistry and / or low yields

Method used

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  • Novel process for synthesis of phenoxy diaminopyrimidine compound
  • Novel process for synthesis of phenoxy diaminopyrimidine compound
  • Novel process for synthesis of phenoxy diaminopyrimidine compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0091] The following examples are intended to be illustrative only and not limiting in any way. Abbreviations used herein and in the specification are conventional abbreviations in the art or below.

[0092] ℃ degrees Celsius

[0093] DABCO 1,4-Diazabicyclo[2.2.2]octane

[0094] DMA Dimethylamine

[0095] DMAP Dimethylaminopyridine

[0096] DMF N,N-Dimethylformamide

[0097] DMI 1,3-Dimethyl-2-imidazolinone

[0098] EtOAc ethyl acetate

[0099] EtOH ethanol

[0100] g grams

[0101] hours

[0102] IPA isopropyl alcohol

[0103] kg kilogram

[0104] L liter

[0105] LC liquid chromatography

[0106] MeOH Methanol

[0107] MSA methanesulfonic acid

[0108] MeCN acetonitrile

[0109] MEK methyl ethyl ketone

[0110] min minute

[0111] mL or ml milliliter

[0112] mole mole

[0113] N equivalent concentration (normal)

[0114] NBS N-Bromosuccinimide

[0115] nM nanomole

[0116] NMP N-methyl-2-pyrrolidone

[0117] RT or rt room temperature

[0118] sat. Sa...

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Abstract

Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-isopropyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.

Description

technical field [0001] The present invention relates to novel processes for the preparation of phenoxydiaminopyrimidine compounds, or pharmaceutically acceptable salts thereof, which are useful in the potential treatment of diseases, conditions and conditions associated with P2X purinergic receptors, such as respiratory and pain-related diseases, disease. Background technique [0002] P2X receptor subunits are found in the afferents of the bladder urothelium in rodents and humans. There are data suggesting that ATP may be released from epithelial / endothelial cells of the bladder or other hollow organs due to distension (Burnstock (1999) J. Anatomy 194:335-342; and Ferguson et al. (1997) J. Physiol. 505:503 -511). ATP released in this way may play a role in transmitting information to sensory neurons located in subepithelial components such as suburothelial lamina propria ((Namasivayam, et al. (1999) BJUIntl.84 :854-860). P2X receptors have been studied in many neurons, in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505
CPCC07D239/48C07D487/08C07C37/62C07C37/84C07C41/16C07C253/30C07C39/27C07C43/23C07C255/13A61K31/513A61K31/4995C07B2200/13C07C41/09C07C41/30C07D487/18
Inventor K·M·马洛尼K·巴苏J·Y·L·钟R·德斯蒙德M·J·迪马索G·R·汉弗莱P·拉彭特A·Y·李D·莱纳尔彭峰任宏M·韦塞尔张四维
Owner MERCK SHARP & DOHME BV
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