申请人:Sumitomo Chemical Co., Ltd.
公开号:US04318925A1
公开(公告)日:1982-03-09
A new class of 4-homoisotwistane derivatives of the formula, ##STR1## wherein R.sub.1 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group, and R.sub.2 is an alkyl group, a phenyl group which may be either unsubstituted or substituted with a C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro group or a halogen atom (hereinafter referred to as "an optionally substituted phenyl group"), a group of the formula, --A--OH in which A is a C.sub.1 -C.sub.3 alkylene group; a group of the formula, --A--B in which A is as defined as above and B is a halogen atom, or a group of the formula, ##STR2## in which A is as defined above and R.sub.3 and R.sub.4 are independently a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group or R.sub.3 and R.sub.4 may, when taken together with the adjacent nitrogen atom to which R.sub.3 and R.sub.4 are linked, form pyrrolidine, piperidine, morpholine, phthalimide or piperazine, which have been found to possess potent antiviral activity, are prepared, for example by reacting a compound of the formula, ##STR3## wherein R.sub.1 is as defined above and X is halogen, with a compound of the formula, R.sub.5 OY wherein R.sub.5 has the same meanings as R.sub.2 with the exception of the group of the formula --A--B wherein A and B are as defined above and Y is alkali metal.
一种新类的4-同构扭环衍生物的公式,其中R.sub.1是氢原子或C.sub.1-C.sub.3烷基,R.sub.2是烷基,苯基,可以是未取代或取代为C.sub.1-C.sub.3烷基,C.sub.1-C.sub.3烷氧基,硝基或卤原子(以下简称“可选择取代苯基”),公式为--A--OH的基团,其中A是C.sub.1-C.sub.3烷基;公式为--A--B的基团,其中A如上定义,B是卤原子,或公式为##STR2##的基团,其中A如上定义,R.sub.3和R.sub.4独立地是氢原子或C.sub.1-C.sub.3烷基,或R.sub.3和R.sub.4可以与与之连接的相邻氮原子一起形成吡咯烷,哌啶,吗啉,苯酞亚胺或哌嗪,这些衍生物具有强大的抗病毒活性,例如通过将公式为##STR3##的化合物与公式为R.sub.5 OY的化合物反应制备,其中R.sub.1如上定义,X是卤素,R.sub.5具有与R.sub.2相同的含义,除了公式--A--B的基团外,其中A和B如上定义,Y是碱金属。