- Direct Access to Primary Amines from Alkenes by Selective Metal-Free Hydroamination
-
Direct and selective synthesis of primary amines from easily available precursors is attractive yet challenging. Herein, we report the rapid synthesis of primary amines from alkenes via metal-free regioselective hydroamination at room temperature. Ammonium carbonate was used as ammonia surrogate for the first time, allowing for efficient conversion of terminal and internal alkenes into linear, α-branched, and α-tertiary primary amines under mild conditions. This method provides a straightforward and powerful approach to a wide spectrum of advanced, highly functionalized primary amines which are of particular interest in pharmaceutical chemistry and other areas.
- Du, Yi-Dan,Chen, Bi-Hong,Shu, Wei
-
supporting information
p. 9875 - 9880
(2021/03/29)
-
- 1 — (4 — Fluorophenyl) — 2 — methyl — 2 — propylamine synthetic method
-
The invention relates to the synthesis of organic substances, in particular to a synthetic method of 1-(4-fluorophenyl)-2-methyl-2-propylamine, comprising the following steps of: firstly, synthesizing 1,1-dimethyl parafluorobenzoic alcohol: adding magnesium powder dried at 95 DEG C by heating into an organic solution of parafluorobenzoic chloride to react, then dropping acetone to react, and then adding 5-20 percent of diluted hydrochloric acid solution, depositing a lemon-yellow organic phase and distilling off the organic solution by a rotary atmometer; secondly, synthesizing parafluoro acylamide: adding acetonitrile and acid liquor which are used as raw materials into the 1,1-dimethyl parafluorobenzoic alcohol to react, then distilling off the acetonitrile, adding a reaction liquid into water, then adding sodium hydroxide for neutralizing until the pH value reaches 6-7, separating out white solid particles, filtering and washing; and thirdly, synthesizing the 1-(4-fluorophenyl)-2-methyl-2-propylamine: adding the parafluoro acylamide and potassium hydroxide solution into a high pressure kettle, replacing with nitrogen, and then depositing a lemon-yellow oil layer to obtain a crude product. The invention has reasonable synthesis route, mild reaction, easy operation, low cost of raw materials, high product yield and high purity.
- -
-
-
- POLYMORPHS OF N2-(1, 1' - BIPHENYL - 4 - YLCARBONYL) - N1- [2- (4 - FLUOROPHENYL) -1, 1 - DIMETHYLETHYL]- L - α -GLUTAMINE
-
Disclosed are novel polymorphic forms of N2-(1, 1'-biphenyl-4-ylcarbonyl)-N1-[2-(4- fluorophenyl)-1, 1-dimethylethyl]-L-α-glutamine, methods of preparing the polymorphic forms, compositions containing the polymorphic forms, and methods of treatment using the polymorphic forms.
- -
-
-