作者:Helen M. Burke、Madeleine M. Joullie
DOI:10.1021/jm00208a016
日期:1978.10
New synthetic routes to the orally active, interferon-inducing antiviral agent tilorone dihydrochloride, 2,7-bis-[(diethylamino)ethoxy]fluoren-9-one dihydrochloride (1a), were developed. The routes involved the preparation and solvolysis of tetrazonium fluoroborate salts of 2,7-diaminofluoren-9-one. Nonplanar (1b), 9-sulfone (1c), and fluorene (1d) analogues of tilorone dihydrochloride were also prepared
已开发出新的合成途径,以合成口服活性的,可诱导干扰素的抗病毒剂,盐酸替洛龙,2,7-双-[((二乙基氨基)乙氧基]芴-9-二氢呋喃酮(1a)。路线涉及2,7-二氨基芴-9-one的氟硼酸四唑盐的制备和溶剂化。还制备了盐酸替洛龙的非平面(1b),9-砜(1c)和芴(1d)类似物。评价化合物1b和1c的干扰素诱导。