CAS: 152305-23-2; (S)-4-(4-Aminobenzyl)Oxazolidin-2-One

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139264-55-4 102029-44-7 90719-32-7

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(S)-4-(4-硝基苄基)-2-噁唑烷酮置于palladium On Activated Charcoal 盐酸,氢气体系中,用 乙醇 用作溶剂,以79%的收率获得(S)-4-(4-氨基苄基)-1,3-噁唑烷-2-酮
参考文献:一种新型的2,5-取代的色胺衍生物作为血管5Ht1B / 1D受体拮抗剂.
标题:一种新型的2,5-取代的色胺衍生物作为血管5Ht1B / 1D受体拮抗剂.
摘要:描述了在血管5Ht1B样受体上一系列新的2,5-取代的色胺衍生物的设计,合成和活性.在对2-取代基,特别是对亚甲基或乙烯连接的5-侧链进行各种修饰之后,已经提出了5Ht1B-样受体的几个重要的辅助结合位点.基于5Ht1B样受体的拟药模型对新分子的仔细设计导致发现乙基3-[2-(二甲基氨基)乙基]-5-[2-(2,5-二氧代-1-咪唑啉基] )[乙基]-1H-吲哚-2-羧酸酯(40),一种高效,沉默,竞争和选择性的拮抗剂,仅对血管5Ht1B样受体具有亲和力.2酯取代基大小的变化对5Ht1B样受体和其他受体的亲和力有重要影响.在5侧链的杂环中谨慎地放置羰基取代基对于5Ht2A和其他受体的非常好亲和力和选择性至关重要.确定了几个关键的结构和电子特征,这些特征对基于色胺的系列药物产生拮抗作用至关重要.为了实现拮抗作用,缺电子的吲哚环系统似乎是必不可少的,这是通过在吲哚环的2-位包含吸电子基团
Doi:10.1021/jm9605849

专利信息

专利号:US-7563904-B2
优先权日:2002-08-07
标题:Synthesis intermediates useful for preparing zolmitriptan
发明人：DALMASES BARJOAN PERE; ARMENGOL ASPARO MONTSERRAT
权利人:INKE SA
摘要:In particular, this invention relates to the synthesis intermediates (IV), (V), (VI) and (VIII) useful for preparing zolmitriptanzohnitriptan or a pharmaceutically acceptable salt thereof, which includes a) Ppreparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with α-keto-δ-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Ttransesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Ssaponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Ddecarboxylation of the indolecarboxylic acid (VIII), to provide zolmitriptan and, eventually, to provide a pharmaceutically acceptable salt thereof.

专利号:US-6303791-B1
优先权日:1995-08-07
标题 :One pot synthesis of 2-oxazolidinone derivatives
发明人：PATEL RAJNIKANT
权利人:ZENECA LTD
摘要:The invention provides an improved process for preparing compounds of formula (I

专利号:US-6909005-B1
优先权日:1995-08-07
标题 :One post synthesis of 2-oxazolidinone derivatives
发明人：PATEL RAJNIKANT
权利人:ASTRAZENECA UK LTD
摘要:The present invention provides an improved (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone product which is prepared by a method which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VII) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.

专利号:US-6160123-A
优先权日:1995-08-07
标 题:One pot synthesis of 2-oxazolidinone derivatives
发明人：PATEL RAJNIKANT
权利人:ZENECA LTD
摘要:The present invention provides an improved process for preparing (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VIl) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.

专利号:EP-1572647-B1
优先权日:2002-12-20
标题 :Synthesis of amines and intermediates for the synthesis thereof

专利号:US-6084103-A
优先权日:1995-08-07
标题 :One pot synthesis of 2-oxazolidinone derivatives