An intermolecular reductive C–C coupling of electrophilic alkyl radicals and alkenes has been developed. Thiols were used as both hydrogen-donating reagents and alkyl radical precursors in the presence of triethyl phosphite and radical initiator. A wide range of alkenes, including styrenes, and aliphatic olefins were well tolerated in this transformation. Mechanistic studies indicated that a phosphite
[EN] SYNTHESIS OF TERFENADINE AND DERIVATIVES<br/>[FR] SYNTHESE DE TERFENADINE ET SES DERIVES
申请人:SEPRACOR, INC.
公开号:WO1998033789A1
公开(公告)日:1998-08-06
(EN) Processes for preparing compounds having general formula (1), wherein R1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the invention begin with a starting material of general formula (II), and elaborate the product by reductive amination of an aldehyde of formula (IVa) with $g(a),$g(a)-diphenyl-4-piperidinemethanol.(FR) L'invention concerne des procédés pour préparer des composés de formule générale (1), dans laquelle R1a représente carboxy protégé, carboxy, hydroxyméthyle, hydroxyméthyle protégé, ou méthyle. Selon les procédés de l'invention, le matériau de départ correspond à la formule générale (II), le produit étant élaboré par amination réductrice d'un aldéhyde de formule IVa, avec un $g(a),$g(a)-diphényl-4-pipéridineméthanol.