CAS: 113400-36-5; Boc-Pyr-Obzl

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L-焦谷氨酸置于4-二甲氨基吡啶,N,N-二异丙基乙胺体系中,用 二氯甲烷,乙腈 用作溶剂,化学反应生成N-叔丁氧羰基-L-焦谷氨酸苄酯
参考文献:Synthesis Of 5(S)-Methyl-L-Proline Containing Peptidomimetic Compounds And Their In Vitro Evaluation For Dipeptidyl Peptidase-4 Inhibition
标题:Synthesis Of 5(S)-Methyl-L-Proline Containing Peptidomimetic Compounds And Their In Vitro Evaluation For Dipeptidyl Peptidase-4 Inhibition
摘要:背景:2型糖尿病(t2Dm)是21世纪的流行病,影响了全球数百万人.传统的治疗方法存在各种副作用.在新的治疗方法中,Dpp-4(二肽基肽酶-4)抑制剂是过去十年中备受期待的治疗方法,具有进一步发展的前景,特别是在肽类模拟物方面. 目的:在先前的工作中设计了含有5(S)-甲基-L-脯氨酸的肽类模拟化合物.合成了设计的化合物,并使用质谱,1H NMR和13C NMR(核磁共振)光谱等光谱方法进行了表征.最终化合物的纯度通过高效液相色谱法(HPLC)确定.合成的化合物在体外评估了它们的dpp-4抑制活性. 方法:化合物具有肽性质,使用传统的合成方法进行合成,其中肽合成是使用酸-胺偶联试剂进行的.它们通过荧光酶基测定法使用dpp-4抑制剂筛选试剂盒进行评估.此外,使用clariostar微孔板读取仪器测量荧光. 结果:合成了含有5(S)-甲基-L-脯氨酸的13种化合物.所有化合物均通过光谱方法进行结构完整性表征.它们的HPLC纯度超过95%,并进行了dpp-4抑制评估.化合物1,7,10,11,14和17的抑制作用比其他化合物更好.这些化合物在不同浓度下进一步评估,以开发线性相关系数(r2). 结论:发现六种化合物具有非常好的dpp-4抑制作用,因此进一步开发含有dpp-4抑制剂的5(S)-甲基-L-脯氨酸的可能性更大.
Doi:10.2174/1570180819666220103124013

专利信息

专利号:US-8143416-B2
优先权日:2004-08-31
标题 :Alternative synthesis of renin inhibitors and intermediates thereof
发明人：SEDELMEIER GOTTFRIED; MICKEL STUART JOHN; RUEEGER HEINRICH
权利人:SEDELMEIER GOTTFRIED; MICKEL STUART JOHN; RUEEGER HEINRICH; NOVARTIS AG
摘要:The present invention relates to synthetic routes to prepare a compound of the formula n nwherein R 1 is halogen, C 1-6 halogenalkyl, C 1-6 alkoxy-C 1-6 alkyloxy or C 1-6 alkoxy-C 1-6 alkyl; R 2 is halogen, C 1-4 alkyl or C 1-4 alkoxy; R 3 and R 4 are independently branched C 3-6 alkyl; and R 5 is cycloalkyl, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy-C 1-6 alkyl, C 1-6 alkanoyloxy-C 1-6 alkyl, C 1-6 aminoalkyl, C 1-6 alkylamino-C 1-6 alkyl, C 1-6 dialkylamino-C 1-6 alkyl, C 1-6 alkanoylamino-C 1-6 alkyl, HO(O)C—C 1-6 alkyl, C 1-6 alkyl-O—(O)C—C 1-6 alkyl, H 2 N—C(O)—C 1-6 alkyl, C 1-6 alkyl-HN—C(O)—C 1-6 alkyl or (C 1-6 alkyl) 2 N—C(O)—C 1-6 alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.

专利号:US-2007208055-A1
优先权日:2004-08-31
标题 :Alternative synthesis of renin inhibitors and intermediates thereof

专利号:US-7910774-B2
优先权日:2004-08-31
标题:Alternative synthesis of renin inhibitors and intermediates thereof

专利号:WO-2006024501-A1
优先权日:2004-08-31
标 题 :Alternative synthesis of renin inhibitors and intermediates thereof

专利号:US-2011137044-A1
优先权日:2004-08-31
标 题:Alternative synthesis of renin inhibitors and intermediates thereof

专利号:EP-1789377-A1
优先权日:2004-08-31
标题:Alternative synthesis of renin inhibitors and intermediates thereof