制备取代的2-[2-(苯基)乙基氨基]烷酰胺衍生物的方法

文档序号:310424 发布日期:2021-11-26 浏览:37次 >En<

阅读说明:本技术 制备取代的2-[2-(苯基)乙基氨基]烷酰胺衍生物的方法 (Process for preparing substituted 2- [2- (phenyl) ethylamino ] alkanamide derivatives ) 是由 W·里昂 兰东晓 张伟芳 方项 吴思忠 于 2020-04-14 设计创作,主要内容包括:本发明涉及一种制备式(I)的化合物或其药学上可接受的盐的方法:其中R是(C-(3)-C-(10))烷基、或ω-三氟(C-(3)-C-(10))烷基;R-(1)和R-(2)独立地是氢、羟基、(C-(1)-C-(8))烷氧基、(C-(1)-C-(8))烷硫基、卤代、三氟甲基或2,2,2-三氟乙基;或R-(1)和R-(2)之一是在R-O-基团的邻位处,且与该同一R-O-一起代表式(A)基团,其中R-(0)是(C-(2)-C-(9))烷基;R-(3)和R-(4)独立地是氢、(C-(1)-C-(4))烷基;或R-(4)是氢且R-(5)是选自-CH-(2)-OH、-CH-(2)-O-(C-(1)-C-(6))烷基、-CH(CH-(3))-OH、-(CH-(2))-(2)-S-CH-(3)、苄基及4-羟苄基的基团;或R-(4)和R-(5)与相邻碳原子一起形成(C-(3)-C-(6))环烷基残基;R-(5)和R-(6)独立地是氢或(C-(1)-C-(6))烷基;或与相邻氮原子一起形成5-6元单环饱和杂环,其任选含有一个选自-O-、-S-及-NR-(7)-的另外的杂原子,其中R-(7)是氢或(C-(1)-C-(6))烷基;且其中任选地,基团R、R-(1)、R-(2)、R-(3)、R-(4)、R-(5)和R-(6)优选R基团中的一或多个氢原子可被氘原子取代。(The present invention relates to a process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R is (C) 3 ‑C 10 ) Alkyl, or omega-trifluoro (C) 3 ‑C 10 ) An alkyl group; r 1 And R 2 Independently hydrogen, hydroxy, (C) 1 ‑C 8 ) Alkoxy group, (C) 1 ‑C 8 ) Alkylthio, halo, trifluoromethyl or 2,2, 2-trifluoroethyl; or R 1 And R 2 One at the ortho position of the R-O-group and together with the same R-O-represents a group of formula (A) whereinR 0 Is (C) 2 ‑C 9 ) An alkyl group; r 3 And R 4 Independently of each other, hydrogen, (C) 1 ‑C 4 ) An alkyl group; or R 4 Is hydrogen and R 5 Is selected from-CH 2 ‑OH、‑CH 2 ‑O‑(C 1 ‑C 6 ) Alkyl, -CH (CH) 3 )‑OH、‑(CH 2 ) 2 ‑S‑CH 3 Benzyl and 4-hydroxybenzyl groups; or R 4 And R 5 Together with adjacent carbon atoms to form (C) 3 ‑C 6 ) A cycloalkyl residue; r 5 And R 6 Independently is hydrogen or (C) 1 ‑C 6 ) An alkyl group; or together with the adjacent nitrogen atom form a 5-6 membered monocyclic saturated heterocycle optionally containing one member selected from the group consisting of-O-, -S-and-NR 7 A further heteroatom of (A), wherein R 7 Is hydrogen or (C) 1 ‑C 6 ) An alkyl group; and wherein optionally, the group R, R 1 、R 2 、R 3 、R 4 、R 5 And R 6 Preferably, one or more hydrogen atoms in the R group may be replaced by deuterium atoms.)

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