CAS: 675-11-6; 4,6-Difluoropyrimidin-2-Amine

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96548-90-2 1360552-57-3 130866-84-1

上下游产品

CAS号696-82-2 2,4,6-三氟嘧啶 | CAS号2253-05-6 2-氨基-4-羟基-6-氟嘧啶

📜2,4,6-三氟嘧啶置于氨体系中,用 水 作为反应溶剂,化学反应生成 2-氨基-4,6-二氟嘧啶
参考文献:Preparation Of 2-Amino-4-Fluoropyrimidine Derivatives
标题:Preparation Of 2-Amino-4-Fluoropyrimidine Derivatives
摘要:本发明涉及一种制备一般式i的2-氨基-4-氟嘧啶衍生物的方法,其中:##str1##(其中r1为氢,烷基,烯基,炔基,环烷基,苯基或苄基,芳香环可以被取代,R2为除氢外的r1基团之一),通过在无水极性有机溶剂中将2,4,6-三氟嘧啶与公式iii的胺反应,得到2-氨基二氟嘧啶衍生物iva和4-氨基二氟嘧啶衍生物ivb的混合物,从所得反应混合物中分离出iva,然后在0oc至180oc下,通过在碱的存在下将iva与醇反应,制备2-氨基-4-氟嘧啶衍生物i.通过在-80oc至-15oc下将2,4,6-三氟嘧啶ii与胺iii反应,并在有机碱的存在下将2-氨基二氟嘧啶衍生物iva与醇反应,制备2-氨基-4-氟嘧啶衍生物i.

专利信息

专利号:WO-0119801-A1
优先权日:1999-09-16
标题 :Bioactive substance containing derivatives of 2-amino-6-aryloxypyrimidines and intermediary products of synthesis thereof
发明人：ASHKINAZI RIMMA ILIINICHNA; GANINA MARIYA BORISOVNA; STUDENTSOV EVGENY PAVLOVICH
权利人:ASHKINAZI RIMMA ILIINICHNA; GANINA MARIYA BORISOVNA; STUDENTSOV EVGENY PAVLOVICH
摘要:The invention relates to novel bioactive compounds of the family of pyrimidines and to intermediary products, of the synthesis of such compounds. The novel compounds have a strong antimicrobial activity (especially in respect to a strain of mycobacterium resisting to the existing drugs) and a strong antiviral activity in addition to a strong immunostimulating (interferonogenic) activity while at the same time having a low toxicity level. The derivatives of 2-amino-6-aryloxypyrimidines and intermediary products of the synthesis of such compounds correspond to the following general formula: (formula I) where R1 is preferably selected from a group containing amino, C1-C4 monoalkylamino, dialkylamino, carboxyalkylamino, arylamino, heterylamino groups; R2 represents halogen atoms or an alkyl, hydroxyl, amino or alkoxy group; R3 represents hydrogen or halogen atoms; R4 represents halogen atoms, aryloxy groups with functional X substituents in ortho-, meta- and para positions of the aryl fragment, whereby X substituents are halogen atoms, alkyls C1-C4, cycloalkyl, alkenyl, alkoxy and nitro groups. The invention also relates to the pharmaceutically acceptable salts thereof.