CAS: 196597-78-1; 1,2,6,7-Tetrahydro-8H-Indeno[5,4-B]Furan-8-One

上下游产品

ethyl (E)-3-(2,3-dihydrobenzofuran-5-yl)-2-propenoate ethyl 3-(2,3-dihydro-1-benzofuran-5-yl)propanoate 4,5-dibromo-1,2,6,7-tetrahydro-8H-indeno[5,4-b]furan-8-one 2.3-dihydrobenzofuran (E)-2-(1,2,6,7-tetrahydro-8H-indeno[5,4-b]furan-8-ylidene)acetonitrile ramelteon 7-benzylidene-1,2,6,7-tetrahydro-8H-indeno[5,4-b]furan-8-one 7-(cyclohexylmethylene)-1,2,6,7-tetrahydro-8H-indeno[5,4-b]furan-8-one

4,5-二溴-1,2,6,7-四氢-8H-茚并[5,4-B]呋喃-8-酮置于10Percent Pd/c/h2O 氢气,溶剂黄146体系中,化学反应 1.0H,以89%的收率获得1,2,6,7-四氢-8H-茚并[5,4-B]呋喃-8-酮
参考文献:合成一系列新的三环茚满衍生物作为褪黑激素受体激动剂.
标题:合成一系列新的三环茚满衍生物作为褪黑激素受体激动剂.
摘要:为了开发一种新的睡眠障碍治疗剂,我们合成了一系列新的三环茚满衍生物,并评估了它们与褪黑激素受体的结合亲和力.在我们以前的论文中,我们提出了甲氧基的构型,有利于mt(1)受体的结合.为了将甲氧基固定在一个活性构象中,我们决定合成构象受限的三环茚满类似物,将其在呋喃,1,3-二恶烷,恶唑,吡喃,吗啉或1,4-中的6-位氧原子合成二恶烷环系统.在这些化合物中,茚并[5,4-B]呋喃类似物被发现是最有效和最具选择性的mt(1)受体配体,并具有出色的代谢稳定性.取代基的优化导致(S)-(-)-22B,它对人mt(1)的亲和力非常强(k(i)= 0.014 Nm),但对仓鼠mt(3)()(k(i)= 2600 Nm)或其他神经递质受体无明显亲和力.在实验动物中研究了(S)-(-)-22B的药理作用,发现以0.1 Mg / Kg的剂量po可以促进自由活动的猫的睡眠,如清醒性的降低和增加所表明的在慢波睡眠
Doi:10.1021/jm0201159

专利信息

专利号:US-2011184058-A1
优先权日:2008-07-14
标 题:Synthesis of 6,7-dihydro-1h-indeno[5, 4-b] furan-8(2h)-one as intermediate in the preparation of remelteon
发明人：CLUZEAU JEROME
权利人:LEK PHARMACEUTICALS
摘要:The present invention describes the preparation of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one, a key intermediate in preparation of ramelteon. The present invention also describes further preceding intermediate compounds useful for the synthesis of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one.

专利号:US-8084630-B2
优先权日:2007-05-31
标 题 :Process for the synthesis of ramelteon and its intermediates
发明人：KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL
权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; RAFILOVICH MICHAL; MOHA-LERMAN ELENA BEN; LIFSHITZ-LIRON REVITAL; TEVA PHARMA
摘要:The present invention provides processes and intermediates for the synthesis of ramelteon.

专利号:US-2010152468-A1
优先权日:2008-10-16
标 题 :Process for the synthesis of ramelteon and its intermediates
发明人：KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; JADAV ARPAN M; DADHANIYA PRATISH; NALAWADE JITENDRA
权利人:TEVA PHARMA
摘要:The present invention provides processes and intermediates for the synthesis of ramelteon.

专利号:US-2009281176-A1
优先权日:2007-11-01
标题:Process for the synthesis of ramelteon and its intermediates
发明人：KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; PATEL RAKESH; JADAV ARPAN M
权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L; PATEL RAKESH; JADAV ARPAN M
摘要:A process for the preparation of ramelteon and intermediates useful in the process. The process suitable for industrial scale provides increased yield and/or greater purity with fewer process steps.

专利号:US-2012083526-A1
优先权日:2009-04-07
标 题:Synthesis of 1-(2,3-dihydrobenzofuran-4-yl)ethanone as intermediate in the preparation of ramelteon
发明人：CLUZEAU JEROME
权利人:CLUZEAU JEROME; LEK PHARMACEUTICALS
摘要:The present invention relates in general to the field of organic chemistry and in particular to the preparation of 1-(2,3-dihydrobenzofuran-4-yl)ethanone, an intermediate in preparation of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide, i.e. ramelteon.

专利号:US-2008242877-A1
优先权日:2007-02-26
标题 :Intermediates and processes for the synthesis of Ramelteon
发明人：KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L
权利人:KANSAL VINOD KUMAR; MISTRY DHIRENKUMAR N; VASOYA SANJAY L
摘要:Provided are intermediates and processes for preparation of Ramelteon.