9-Hydroxydibenzo[b,d]pyrans and intermediates therefore
    16.
    发明授权
    9-Hydroxydibenzo[b,d]pyrans and intermediates therefore 失效
    因此,9-羟基二苯并[b,d]吡喃和中间体

    公开(公告)号:US4243674A

    公开(公告)日:1981-01-06

    申请号:US914664

    申请日:1978-06-12

    申请人: Jasjit S. Bindra

    发明人: Jasjit S. Bindra

    摘要: 9-Hydroxydibenzo[b,d]pyrans useful as analgesics, hypotensives, immunosuppressants, tranquilizers; as anti-secretory and anti-anxiety drugs; intermediates therefor and derivatives thereof having the formulae ##STR1## wherein R is hydrogen or alkanoyl having from one to five carbon atoms;R.sub.1 is hydrogen, alkanoyl having from one to five carbon atoms or --CO--(CH.sub.2).sub.p --NR.sub.2 R.sub.3 wherein p is 0 or an integer from 1 to 4; each of R.sub.2 and R.sub.3 when taken individually is hydrogen or alkyl having from one to four carbon atoms; R.sub.2 and R.sub.3 when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from one to four carbon atoms in the alkyl group;each of R.sub.4 and R.sub.5 is hydrogen, methyl or ethyl;R.sub.0 is oxo or alkylenedioxy having from two to four carbon atoms;Z is(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2) has from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;each of m and n is 0 or 1;X is O, S, SO or SO.sub.2 ; andW is methyl, phenyl, p-chlorophenyl, p-fluorophenyl, pyridyl, piperidyl, cycloalkyl having from 3 to 7 carbon atoms, or monosubstituted cycloalkyl wherein the substituent is phenyl, p-chlorophenyl or p-fluorophenyl;with the proviso that when W is methyl, Z is --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n --.

    摘要翻译: 9-羟基二苯并[b,d]吡喃可用作镇痛药,低血糖剂,免疫抑制剂,镇定剂; 作为抗分泌和抗焦虑药物; 其中间体及其衍生物,其具有下式:其中R是氢或具有1至5个碳原子的烷酰基; R 1是氢,具有1至5个碳原子的烷酰基或-CO-(CH 2)p -NR 2 R 3,其中p是0或1至4的整数; R2和R3分别独立地为氢或具有1-4个碳原子的烷基; 当与它们相连的氮原子一起连接时,R2和R3形成选自哌啶基,吡咯并,吡咯烷子基,吗啉代和在烷基中具有1-4个碳原子的N-烷基哌嗪基的5-或6-元杂环; R 4和R 5各自为氢,甲基或乙基; R 0是具有2至4个碳原子的氧代或亚烷基二氧基; Z是(a)具有1至9个碳原子的亚烷基; (b) - (alk1)mX-(alk2)n-其中(alk1)和(alk2)中的每一个具有1至9个碳原子,条件是(alk1)加(alk2)中的碳原子的总和为 不大于9; m和n各自为0或1; X是O,S,SO或SO 2; W是甲基,苯基,对氯苯基,对氟苯基,吡啶基,哌啶基,具有3-7个碳原子的环烷基或单取代的环烷基,其中取代基是苯基,对氯苯基或对氟苯基; 条件是当W是甲基时,Z是 - (alk1)m -X-(alk2)n-。