CAS: 144978-12-1; (S)-Ethyl-N-Boc-Pyroglutamate

上下游产品

tert-butyl dicarbonatedi-tert-butyl dicarbonate ethyl (R)-2-pyrrolidone-5-carboxylate 2,2-dimethylpropanoic anhydride D-pyrrolidone-5-carboxylic acid(Z)-(R)-2-tert-Butoxycarbonylamino-7-hydroxy-5-oxo-7-phenyl-hept-6-enoic acid ethyl ester (R)-2-tert-Butoxycarbonylamino-5-oxo-5-o-tolyl-pentanoic acid ethyl ester ethyl (2R,4R)-N-B°C-4-(4-iodo)benzyl D-pyroglutamate ethyl (2R,4S,E)-N-B°C-4-cinnamyl D-pyroglutamate

L-焦谷氨酸置于4-二甲氨基吡啶,硫酸,三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应 42.0H,反应生成Boc-L-焦谷氨酸乙酯
参考文献:L-γ-亚甲基谷氨酸酰胺叔丁酯和乙酯抗癌前药的合成及生物学评价
标题:L-γ-亚甲基谷氨酸酰胺叔丁酯和乙酯抗癌前药的合成及生物学评价
摘要:在癌细胞中,谷氨酰胺分解是生物合成前体的主要来源.最近,人们在开发氨基酸类似物来抑制癌症中谷氨酰胺代谢方面做出了广泛的努力.我们的实验室最近发现了许多l-γ-亚甲基谷氨酸酰胺,在24年后抑制mcf-7,Sk-Br-3和mda-Mb-231乳腺癌细胞的生长与他莫昔芬或奥拉帕尼一样有效.或72小时的治疗.这些化合物均不会抑制非恶性 Mcf-10A 乳腺细胞的细胞生长.这些l-γ-亚甲基谷氨酸酰胺有望成为治疗多种乳腺癌亚型的新型疗法.在此,我们报告了这些l-γ-亚甲基谷氨酸酰胺的两个系列的叔丁酯和乙酯前药及其环状代谢物及其叔丁酯和乙酯对三种乳腺癌细胞系mcf的合成和评价-7,Sk-Br-3 和 Mda-Mb-231 以及非恶性 Mcf-10A 乳腺细胞系.这些酯被发现可以抑制乳腺癌细胞的生长,但与l-γ-亚甲基谷氨酸酰胺相比,它们的效力较差.对l-γ-亚甲基谷氨酸酰胺先导物进行药代动力学
Doi:10.1016/j.Bmc.2022.117137

专利信息

专利号:US-8487108-B2
优先权日:2005-11-14
标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors
发明人：BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T
权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC
摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

专利号:US-2023151034-A1
优先权日:2020-03-17
标题:Peptidomimetic n5-methyl-n2-(nonanoyl-l-leucyl)-l-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds as inhibitors of norovirus and coronavirus replication
发明人：JACOBSON IRINA C; LEE SAM SK; PIZARRO NOVOA JUAN CARLOS
权利人:COCRYSTAL PHARMA INC
摘要:Peptidomimetic N5-methyl-N2-(nonanoyl-L-leucyl)-L-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds for use in methods of inhibiting the replication of noroviruses and coronaviruses in a biological sample or patient, for use in reducing the amount of noroviruses or coronaviruses in a biological sample or patient, and for use in treating norovirus and coronavirus in a patient, comprising administering to said biological sample or patient a safe and effective amount of a compound represented by formulae I or II, or a pharmaceutically acceptable salt thereof. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. page 99 to page 271; examples 1 to 3; compounds A1 to A104 and B1 to B66; tables A to E).

专利号:CN-115124448-A
优先权日:2022-07-20
标 题:A kind of method for one-pot synthesis of D-pyroglutamic acid derivatives

专利号:EP-1554235-A4
优先权日:2002-10-25
标 题:PROCESS FOR SYNTHESIS OF L-Y-METHYLENE GLUTAMINE SUSCE AND ANALOGUE

专利号:CN-108239019-B
优先权日:2016-12-27
标题 :Synthesis method of (2S,5S or 5R) -N-tert-butyloxycarbonyl-5-hydroxy-2-ethyl piperidinecarboxylate