| 摘要 |
<p>Preparation of (E)-2-alkyl-3-heterocyclylprop-2-en-1-ol (I) involves reacting heterocyclic halide (II) with prop-2-yn-1-ol to give 3-heterocyclylprop-2-yn-1-ol (III); and reacting the compound (III) with alkyl-metal compound. Preparation of (E)-2-alkyl-3-heterocyclylprop-2-en-1-ol of formula (I) involves reacting heterocyclic halide of formula (II) with prop-2-yn-1-ol to give 3-heterocyclylprop-2-yn-1-ol of formula (III); and reacting the compound (III) with R 3-metal compound. Het : bicyclic unsaturated heterocyclyl bonded to the rest of the molecule via a carbon atom, where the ring not bonded directly to the rest of the molecule is substituted with R 1 and R 2; R 1 and R 2H, 1-8C alkyl, halo, polyhalo-1-8C alkoxy, polyhalo-1-8C alkyl, 1-8C alkoxy, 1-8C-alkoxy-1-8C alkyl or 1-8C-alkoxy-1-8C alkoxy; R 31-8C alkyl;and X : Br, I, triflate, tosylate or mesylate. Provided that R 1 and R 2 are not both H. An independent claim is included for 3-heterocyclylprop-2-en-1-ol of formula (III) (in which Het is 1H-indol-6-yl, imidazo[1,5-a]pyridin-6-yl or 1H-indazol-6-yl) as new intermediate. [Image].</p> |
