CAS: 149771-44-8; Tert-Butyl 3,8-Diazabicyclo[3.2.1]Octane-8-Carboxylate

相似化合物

201162-53-0 17783-50-5 1639111-11-7

上下游产品

Tert-Butyl 3-(2,2,2-Trifluoroacetyl)-3,8-Diazabicyclo[3.2.1]Octane-8-Carboxylate 824982-19-6
3-苄基-8-(叔丁氧基羰基)-3,8-二氮杂双环[3.2.1]-辛烷 Tert-Butyl 3-Benzyl-3,8-Diazabicyclo[3.2.1]Octane-8-Carboxylate 149771-43-7

3-苄基-8-(叔丁氧基羰基)-3,8-二氮杂双环[3.2.1]-辛烷置于palladium On Activated Charcoal 氢气体系中,用 乙醇 用作溶剂,以95%的收率获得8-Boc-3,8-二氮杂双环[3.2.1]辛烷
参考文献:单取代和二取代的3,8-二氮杂双环[3.2.1]辛烷衍生物作为与依巴替丁结构相关的止痛药:合成,活性和建模.
标题:单取代和二取代的3,8-二氮杂双环[3.2.1]辛烷衍生物作为与依巴替丁结构相关的止痛药:合成,活性和建模.
摘要:合成了一系列3,8-二氮杂双环[3.2.1]辛烷,它们在3位(化合物1)或8位(化合物2)被氯代杂芳基环取代,作为强效天然止痛剂epibatidine的潜在类似物.当在热板试验中测试时,大多数化合物显示出显着效果,最有趣的是3-(6-氯-3-吡啶并嗪基)-3,8-二氮杂双环[3.2.1]辛烷(1A).在1 Mg / Kg的皮下剂量下,1A导致疼痛阈值显着增加,其作用持续约45分钟.1A在小鼠腹部收缩试验中以5 Mg / Kg的剂量也表现出非常好的保护作用,而在20 Mg / Kg的剂量下,它完全阻止了动物的收缩.纳洛酮(1 Mg / Kg腹膜内)的给药不会拮抗其抗伤害感受,而美加明(2 Mg / Kg腹膜内)则能拮抗其伤害感受,因此暗示烟碱系统参与其作用.结合研究证实了对α4 Beta 2 Nachr亚型的高度亲和力(ki = 4.1 +/-0.21 Nm).对三种不同细胞系的nachr功
Doi:10.1021/jm970427P

专利信息

专利号:US-11649244-B2
优先权日:2021-07-14
标 题 :Method for synthesizing diaza-bridged compound and a diaza-bridged compound
发明人：LU XI; LIU SHUAI; LIANG YONG; CAI JIAMING; TANG QUAN; ZENG YUAN
权利人:LINKCHEM CO LTD SHANGHAI
摘要:The present disclosure discloses a method for synthesizing a diaza-bridged compound and a diaza-bridged compound, belonging to the field of organic synthesis. The present disclosure includes the following reaction:in the formula, R is aryl, substituted aryl, alkyl or haloalkyl, Ra is any one of H, 2-nitrobenzenesulfonyl, 4-nitrobenzenesulfonyl or 2,4-dinitrobenzenesulfonyl, n=1 or 2. Since compound 2 and NH3 are used as raw materials, the present disclosure can not only effectively shorten the process flow and save process costs, but also improve the reaction yield to a certain extent. The present disclosure also provides a diaza-bridged compound, where the structural formula thereof isin the formula, Ra is any one of 2-nitrobenzenesulfonyl, 4-nitrobenzenesulfonyl or 2,4-dinitrobenzenesulfonyl. Since the compound has a higher melting point, is easy to recrystallize to get solid and not easy to form oil under high temperature, the diaza-bridged compound is suitable for long-distance transportation and long-term storage.

专利号:WO-2022262686-A1
优先权日:2021-06-13
标题 :Kras g12d inhibitors
发明人：HAN YING; LI DAPENG; WANG TONG
权利人:JINGRUI BIOPHARMA CO LTD
摘要:Disclosed are novel compounds which are KRAS G12D inhibitors, their synthesis and their use for treating diseases or conditions, such as cancer, and in particular for inhibiting the activity of KRAS G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

专利号:CN-116621794-A
优先权日:2023-05-22
标题:A kind of 5-benzyl-2-amino-1,3-thiazole derivatives and its synthesis method and application