CAS: 198904-85-7; Tert-Butyl 2-(4-(Pyridin-2-yl)Benzyl)Hydrazinecarboxylate

相似化合物

198904-84-6 834884-86-5 849353-27-1

上下游产品

CAS号857904-11-1 HYDRAZINECARBOX... | CAS号198904-84-6 [[4-(2-吡啶基)苯基]亚... | CAS号109-04-6 2-溴吡啶 | CAS号127406-56-8 4-(2-吡啶基)-苯甲醛 | CAS号24856-58-4 4-溴苯甲醛二甲基缩醛 | CAS号87199-17-5 4-甲酰基苯硼酸 | CAS号198904-86-8 2-[(2S,3S)-3-[[... | CAS号1140968-73-5 tert-butyl 2-((... | CAS号198904-31-3 阿扎那韦 | CAS号920757-34-2 1-(4-(吡啶-2-基)苄基)肼

4-溴苯甲醛二甲缩醛置于palladium On Activated Charcoal 盐酸,1,3-Bis[(Diphenylphosphino)Propane]Dichloronickel(II),氢气,碘,二异丁基氢化铝,Magnesium体系中,用 甲醇,乙醇 用作溶剂,化学反应 4.0H,反应生成2-[[4-(2-吡啶基)苯基]甲基]-肼羧酸-(1,1-二甲基)乙酯
参考文献:New Aza-Dipeptide Analogues As Potent And Orally Absorbed Hiv-1 Protease Inhibitors: Candidates For Clinical Development
标题:New Aza-Dipeptide Analogues As Potent And Orally Absorbed Hiv-1 Protease Inhibitors: Candidates For Clinical Development
摘要:On The Basis Of Previously Described X-Ray Studies Of An Enzyme/aza-Dipeptide Complex,(8) Azadipeptide Analogues Carrying N-(Bis-Aryl-Methyl) Substituents On The (Hydroxethyl)Hydrazine Moiety Have Been Designed And Synthesized As Hiv-1 Protease Inhibitors. By Using Either Equally (12) Ororthogonally (13) Protected Dipeptide Isosteres,Symmetrically And Asymmetrically Acylated Aza-Dipeptides Can Be Synthesized. This Approach Led To The Discovery Of Very Potent Inhibitors With Antiviral Activities (Ed50) In The Subnanomolar Range. Acylation Of The (Hydroxethyl)Hydrazine Dipeptide Isostere With The L-Tert-Leucine Derivative 29 Increased The Oral Bioavailability Significantly When Compared To The Corresponding L-Valine Or L-Isoleucine Derivatives. The Bis(L-Tert-Leucine) Derivatives Cgp 75355,Cgp 73547,Cgp 75136,And Cgp 75176 Combine Excellent Antiviral Activity With High Blood Concentration After Oral Administration. Furthermore,They Show No Cross-Resistance With Saquinavir-Resistant Strains And Maintain Activity Against Indinavir-Resistant Ones. Consequently They Qualify For Further Profiling As Potential Clinical Candidates.
Doi:10.1021/jm970873C

专利信息

专利号:US-2010184989-A1
优先权日:2007-03-12
标 题 :De Novo Synthesis of Conjugates
发明人：RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J
权利人:NEKTAR THERAPEUTICS
摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.

专利号:AU-2008226820-A1
优先权日:2007-03-12
标题 :De novo synthesis of conjugates

专利号:CA-2679473-A1
优先权日:2007-03-12
标题:De novo synthesis of conjugates

专利号:WO-2008112286-A9
优先权日:2007-03-12
标题 :De novo synthesis of conjugates

专利号:WO-2008112286-A2
优先权日:2007-03-12
标题:De novo synthesis of conjugates

专利号:JP-2010521465-A
优先权日:2007-03-12
标 题 :De novo synthesis of complex