Mechanism and Scope of Base-Controlled Catalyst-Free N-Arylation of Amines with Unactivated Fluorobenzenes
A general method for transition metal-free N-arylation of amines has been developed. Mechanistic studies have revealed that the ability of the base to facilitate the desired amination without promoting unwanted side reactions is the guiding factor. By employing lithium bis(trimethylsilyl)amide as a base the resultant deprotonated amines readily react with a range of unactivated fluorobenzene derivatives. This new arylation method is utilized for the simple two-step synthesis of the antidepressant Vortioxetine.
Borch Jacobsen, Christian,Meldal, Morten,Diness, Frederik
p. 846 - 851
(2017/02/05)
Method of making chlorofluoroethers
A method is provided for preparation of chlorofluoroethers ClCF2CFClOR8f and Cl2CFCFClOR8f by direct fluorination of Cl2CHCH2OR8 and Cl3CCH2OR8, respectively, wherein R8 is a C1-C20 alkyl-or acyl-containing group optionally up to 5 ether oxygen atoms and optionally substituted by functional groups and R81, is the corresponding perfluoroalkyl or perfluoracyl-containing group.
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Example 29
(2010/01/31)
Polyhalogenoaromatic Compounds. Part 53. Substitution in Polyfluoroaromatic Compounds by Bulky Nucleophiles
Potassium t-butoxide in THF is highly reactive towards polyfluoroaromatic compounds.The position(s) of substitution are generally similar to those observed with other nucleophiles, though octafluoronaphthalene undergoes ca. 30percent 2,7-disubstitution.He
Cheong, Catherine L.,Wakefield, Basil J.
p. 3301 - 3306
(2007/10/02)
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