2-Methoxy-5-fluoro-4-aminopyrimidine synthesis
- Product Name:2-Methoxy-5-fluoro-4-aminopyrimidine
- CAS Number:1993-63-1
- Molecular formula:C5H6FN3O
- Molecular Weight:143.12
1801-06-5
1993-63-1
General procedure for the synthesis of 5-fluoro-2-methoxy-4-fluoropyrimidinamine using 2-methoxy-4-chloro-5-fluoropyrimidine as starting material: 32.5 g of 2-methoxy-4-chloro-5-fluoropyrimidine (compound of formula III) was added to 170 g of a 10 wt% solution of isopropanol in ammonia, heated to 40-60 °C, and the reaction was stirred for 3-5 hours. After completion of the reaction, it was naturally cooled to room temperature and the solid product was collected by filtration. The solid was washed with isopropanol and dried to give 27.2 g of 5-fluoro-2-methoxy-4-pyrimidinamine (compound of formula II, white solid) in 95.0% molar yield and 99.0% HPLC purity.
1801-06-5
82 suppliers
$41.00/250mg
1993-63-1
103 suppliers
$14.00/5g
Yield: 95%
Reaction Conditions:
with ammonia in isopropyl alcohol at 40 - 60;
Steps:
2 Example 2: preparation of compounds of formula II
The 32.5g formula III compound are added 170g10wt % of the isopropyl alcohol solution of ammonia, heating to 40-60°C, stirring reaction 3-5 hours, natural cooling to room temperature, filtered, collecting solid, washing with isopropyl alcohol, drying, the compound of formula II is obtained (kind of white solid) 27.2g, molar yield is 95.0%, HPLC purity of 99.0%.
References:
Shanghai Dixinuo Chemical Pharmaceutical Co., Ltd;Shanghai Desano Pharmaceutical Co., Ltd.;Li, Jinliang;Zhao, Nan;Hua, Sikai CN105272922, 2016, A Location in patent:Paragraph 0038; 0039; 0040