[EN] ALKYLATION WITH AN ALKYL FLUOROALKYL SULFONATE<br/>[FR] ALKYLATION AVEC UN FLUOROALKYL SULFONATE D'ALKYLE
申请人:NOVARTIS AG
公开号:WO2014203185A1
公开(公告)日:2014-12-24
The present invention discloses a process for preparing a chemical compound comprising reacting a nucleophile with an alkyl fluoroalkyi sulfonate in the presence of a base of formula NR1 R2R3, wherein R1 and R2 are independently 2-methylpropyl or isopropyl and R3 is - CH(R4)(R5), wherein R4 and R5 are identical or different alkyls that are optionally connected to form a ring. The invention also relates to a process for preparing an alkyl fluoroalkyi sulfonate. The invention further relates to a use of the base in a chemical reaction comprising an alkyl fluoroalkyi sulfonate. The process and uses are suitable for preparing chemical compounds, reactants or intermediates thereof, and in particular for preparing API or reactants, like for example everolimus or reactants for its preparation.
本发明揭示了一种制备化合物的方法,包括在公式NR1R2R3的碱存在下,通过将亲核试剂与烷基氟烷磺酸酯反应来制备化合物。其中,R1和R2分别是2-甲基丙基或异丙基,R3为-CH(R4)(R5),其中R4和R5是相同或不同的烷基,可以连接形成环。本发明还涉及制备烷基氟烷磺酸酯的方法。本发明进一步涉及在含有烷基氟烷磺酸酯的化学反应中使用碱。该方法和用途适用于制备化合物,反应物或其中间体,特别是用于制备API或反应物,例如埃罗利莫斯或其制备的反应物。