| 摘要 |
<p>N-Benzyl substd. amides of formula Ar-CH2-NR1-C OR2 (I) are prepd. by reaction of an aromatic hydrocarbon ArH (II) with a hydroxymethyl amide of formula HO-CH2-NR1-COR2 (III) in the presence of hydrofluoric acid (Ar=a benzenoid radical, opt. substd.; R1 and R2=H, 1-6C alkyl, phenyl, or substd. phenyl, or R1 and R2 together form a ring). The hydrofluoric acid may be a concd. aq. soln., but is pref. anhydrous. Ar is pref. phenyl, opt. substd. by Cl, Br, CN, NO2, CHO, COOH, COR, COOR, alkyl, alkoxy, phenyl or phenoxy (where R=alkyl), the alkyl and alkoxy gps. having 1-6C. The reaction is effected at 0-100 deg. C, pref. with the molar ratio HF: (II) =5-50: and the molar ratio (II):(III)=0.5-2:1. (I) may be used as intermediate for pharmaceuticals and phytosanitary prods. The process is easier to carry out than the known method using sulphuric acid, and gives a purer prod.</p> |
