CAS: 1027-35-6; Ethyl 1-Benzyl-4-Oxopyrrolidine-3-Carboxylate

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CAS号795-18-6 3-(苄基(2-乙氧基-2-氧... | CAS号635698-34-9 6-苄基-6,7-二氢-1H-...

2-氮杂丁烷-1,4-二羧酸二乙酯置于四氯化钛,碳酸氢钠体系中,用 二氯甲烷,乙腈 用作溶剂,化学反应 19.0H,反应生成1-苄基-4-酮基-3-吡咯烷甲酸乙酯
参考文献:Dna修复酶烷基腺嘌呤糖基化酶(aag)的氮杂核苷,片段样抑制剂.
标题:Dna修复酶烷基腺嘌呤糖基化酶(aag)的氮杂核苷,片段样抑制剂.
摘要:Dna修复酶aag已在小鼠中显示出响应于缺血性再灌注或用烷基化剂治疗而促进组织坏死.对于引起这种现象的生物学机制的研究,化学抑制剂是必需的,并且它是潜在保护器官免受器官衰竭和移植以及烷基化化学疗法伤害的药物的先导.在本文中,我们描述了选择芳基甲基吡咯烷酮作为抑制剂的合适氮杂核苷模拟物背后的原理,然后合成了它们,并首次使用了基于微孔板的测定方法来量化其对aag的抑制作用.我们最后报告了咪唑-4-基甲基吡咯烷作为片段大小的aag弱抑制剂的发现.
Doi:10.1016/j.Bmc.2020.115507

专利信息

专利号:US-9238648-B2
优先权日:2011-10-14
标题 :Asymmetric synthesis method, related raw material and preparation method of (S,S)-2,8-diazabicyclo[4,3,0]nonane
发明人：SHENTU XIAOBO; QI YANTAO; XIE LINGSHI; WANG BO
权利人:SHANGHAI PUYI CHEMICAL TECHNOLOGY CO LTD
摘要:The present invention relates to an asymmetric synthesis method of a chiral intermediate (S,S)-2,8-diazabicyclo[4,3,0]nonane (I) of moxifloxacin, wherein an imide or enamine compound is obtained by dehydration reaction of the pyrrolidine-3-ketone as shown in formula (II) and chiral amine(R)-1-phenylethylamine, followed by the reduction of the imide or enamine compound to obtain a compound of formula (III) or (IV) having the chiral structure of formula (I), and then a compound of formula (I) is obtained by intramolecular cyclization, and removal of the chiral auxiliary group and amino-protecting group. The present invention also relates to pyrrolidine-3-ketone as shown in formula (II) and a preparation method therefor, n n n n n n n n n n n n and in the formula (I), (II), (III), (IV), R is an amino-protecting group, especially C 1-4 alkoxycarbonyl, benzyloxycarbonyl or benzyl which can be removed by hydrolysis or hydrogenation. Zâ•?H 2 or O; when Zâ•?H 2 , Y is chlorine, bromine, iodine, methanesulfonate, tosylate, hydroxyl or hydroxyl with protection; and when Zâ•?O, Y is OR 1 , and R 1 is C 1- alkyl.

专利号:EP-2679588-B1
优先权日:2011-10-14
标 题 :Asymmetric synthesis method, related raw material and preparation method of (s,s)-2,8-diazabicyclo[4,3,0]nonane

专利号:US-2014066626-A1
优先权日:2011-10-14
标题 :Asymmetric synthesis method, related raw material and preparation method of (s,s)-2,8-diazabicyclo[4,3,0]nonane

专利号:JP-2014504616-A
优先权日:2011-10-14
标 题:Asymmetric synthesis method of (S, S) -2,8-diazabicyclo [4.3.0] nonane, and related raw materials and preparation method thereof

专利号:CN-103044418-B
优先权日:2011-10-14
标 题:Asymmetric synthesis method, related raw materials and preparation method of (S,S)-2,8-diazabicyclo[4,3,0]nonane

专利号:CN-103044418-A
优先权日:2011-10-14
标 题:Asymmetric synthesis method, related raw materials and preparation method of (S,S)-2,8-diazabicyclo[4,3,0]nonane