| 摘要 |
Prepn. of 2-(2- and 3-thienyl)ethylamines of formula (I) is claimed (where R1 is in posn. 2, 3, 4 or 5 and is H, alkyl, aromatic gp. which may be a heterocycle (and is opt. mono- or poly-substd. by alkyl, phenyl, halogen, nitro, cyano, amino, carboxy or alkoxy), alkoxy, halogen, nitro, carboxy, cyano or amino; the aminoethyl chain may occupy posn. 2 or 3; R2 is H, alkyl or atomatic gp. which may be a heterocycle (and may be substd. as above); Ar is aromatic gp. which may be a heterocycle (and may be substd. as above)). Process comprises (a) heating (V) to give (VI); (b) treating with water to give (VII); (c) reducing to give (VIII); (d) reacting this with a base, followed by a halogen deriv. Ar-CH(Hal)-R2 to give (X) and (e) treatment of (X) with acid to give (I) (where X and Y are alkyl, aryl, alkoxy, aryloxy, dialkyl- or diarylamino; M is a cation, pref. alkali or alkaline earth metal). (I) are intermediates for chemical prods. and pharmaceuticals. |
