CAS: 14019-62-6; Isopropyl 2-Aminoacetate Hydrochloride

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197579-95-6 27532-96-3 136088-69-2

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CAS号105-48-6 氯乙酸异丙酯 | CAS号67-63-0 异丙醇 | CAS号56-40-6 甘氨酸 | CAS号22136-61-4 2-diazonio-1-pr... | CAS号58511-00-5 propan-2-yl 2-i...

📜氯乙酸异丙酯置于palladium On Activated Charcoal 盐酸,Sodium Azide,氢气体系中,用 乙醇,N,N-二甲基甲酰胺 用作溶剂,化学反应 3.0H,反应生成甘氨酸异丙酯盐酸盐
参考文献:环状amp磷酸二酯酶的抑制剂.4. Lixazinone(n-Cyclohexyl-N-Methyl-4-[(1,2,3,5-Tetrahydro-2-Oxoimidazo [2,1-B] Quinazolin-7-Yl)-]的合成和评价氧]丁酰胺,Rs-82856).
标题:环状amp磷酸二酯酶的抑制剂.4. Lixazinone(n-Cyclohexyl-N-Methyl-4-[(1,2,3,5-Tetrahydro-2-Oxoimidazo [2,1-B] Quinazolin-7-Yl)-]的合成和评价氧]丁酰胺,Rs-82856).
摘要:环状amp磷酸二酯酶(camp Pde)抑制剂和强心药lixazinone(n-环己基-N-甲基-4-[(1,2,3,5-四氢-2-氧代咪唑[2,1-B]喹唑啉-7-发现)))氧基]丁酰胺,Rs-82856,1)及其酸和碱加成盐在适用于静脉内给药的制剂中溶解性不足.这些结果促使人们对具有提高的水溶性的潜在前药进行了研究,旨在通过三种不同的机制释放1:(1)α-羧酰胺的脱羧;(2)可溶的n-1-(酰氧基)甲基或(n,N-二烷基氨基)甲基部分的水解损失;或(3)胍基酯或酰胺的分子内封闭.通过三个标准对目标化合物作为1的传输系统进行了评估:(1)在生理条件下化学转化率为1;(2)在固定时间点抑制iv型camp Pde;(3)通过静脉内和口服给予的麻醉犬体内的变力活性.发现从4A(系列1)释放1太慢,以至于不能作为1的前药使用,因为脱羧只能由强酸诱导,而在强酸条件下发现水解开环剧烈竞争.相反,尽管
Doi:10.1021/jm00119A015

专利信息

专利号:US-7973175-B2
优先权日:2005-09-28
标 题 :Synthesis of renin inhibitors involving a cycloaddition reaction
发明人：MICKEL STUART J; MARTERER WOLFGANG
权利人:NOVARTIS AG
摘要:The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, n nwherein R, R 1 , and R′ are as defined in the specification, or a salt thereof, and a compound of formula IVn n nwherein R, R 1 , R 2 and R′ are as defined in the specification, and processes of manufacturing these.

专利号:WO-2024258613-A9
优先权日:2023-06-16
标题:Tetrachlorovancomycin and derivatives
发明人：BOGER DALE
权利人:SCRIPPS RESEARCH INST
摘要:A total synthesis of a new class of vancomycin analogues of reduced synthetic complexity was developed. The synthesis, achieved by the addition of two aryl chloride substituents to provide tetrachlorovancomcyin aglycon (Compound II), tetrachlorovancomcyin (Compound I ), and their derivatives, permitted a streamlined total synthesis of the new class of glycopeptide antibiotics by removing atropisomer stereochemical control and enabled the simultaneous and further activated SNAr macrocyclizations that establish the tricyclic skeleton of Compound I. In addition to the antimicrobial evaluation of tetrachlorovancomycin (Compound I), the preparation of key binding pocket and peripherally-modi fied derivatives, which overcome vancomycin resistance and introduce independent and synergistic mechanisms of action, revealed their exceptional antimicrobial potency and provide the foundation for use of this new class of synthetic glycopeptide analogues. Also disclosed are a pharmaceutical composition containing bactericidal amount of tetrachlorovancomycin, a derivative thereof or a salt of either dissolved or dispersed in a pharmaceutically acceptable diluent.

专利号:US-2008255369-A1
优先权日:2005-09-28
标 题 :Synthesis of Renin Inhibitors Involving a Cycloaddition Reaction

专利号:US-2011230665-A1
优先权日:2005-09-28
标题 :Synthesis of renin inhibitors involving a cycloaddition reaction

专利号:EP-1931629-B1
优先权日:2005-09-28
标 题 :Synthesis of renin inhibitors involving a cycloaddition reaction

专利号:CA-2623495-A1
优先权日:2005-09-28
标题 :Synthesis of renin inhibitors involving a cycloaddition reaction