CAS: 43088-42-2; Ethyl 2-Amino-4-Methylthiophene-3-Carboxylate

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Ethyl 2-Amino-4-Methyl-5-(Tert-Butoxycarbonyl)Thiophene-3-Carboxylate置于盐酸体系中,用 乙醇 作为反应溶剂,化学反应 1.0H,以85%的收率获得产物2-氨基-4-甲基-噻吩-3-羧酸乙酯
参考文献:2-(Diethylamino)Thieno[1,3]Oxazin-4-Ones As Stable Inhibitors Of Human Leukocyte Elastase
标题:2-(Diethylamino)Thieno[1,3]Oxazin-4-Ones As Stable Inhibitors Of Human Leukocyte Elastase
摘要:A Series Of 2-(Diethylamino)Thieno[1,3]Oxazin-4-Ones Was Synthesized And Evaluated In Vitro For Inhibitory Activity Toward Human Leukocyte Elastase (Hle). The Gewald Thiophene Synthesis Was Utilized To Obtain Several Ethyl 2-Aminothiophene-3-Carboxylates. These Precursors Were Subjected To A Five-Step Route To Obtain Thieno[2,3-D][1,3]Oxazin-4-Ones Bearing Various Substituents At Positions 5 And 6. Both Thieno[2,3-D] And Thieno[3,2-D] Fused Oxazin-4-Ones Possess Extraordinary Chemical Stability,Which Was Expressed As Rate Constants Of The Alkaline Hydrolysis. The Kinetic Parameters Of The Hle Inhibition Were Determined. The Most Potent Compound,2-(Diethylamino)-4H-[1]Benzothieno[2,3-D][1,3]Oxazin-4-One,Exhibited A K-I Value Of 5.8 Nm. 2-(Diethylamino)Thieno[1,3]Oxazin-4-Ones Act As Acyl-Enzyme Inhibitors Of Hle,Similar To The Inhibition Of Serine Proteases By 4H-3,1-Benzoxazin-4-Ones. The Isosteric Benzene-Thiophene Replacement Accounts For An Enhanced Stability Of The Acyl-Enzyme Intermediates.
DOI:10.1021/jm991108W

专利信息

专利号:US-4670560-A
优先权日:1986-04-28
标 题:Thienopyrimidine-2,4-dione derivatives and intermediates thereof
发明人：PRESS JEFFERY B; RUSSELL RONALD K
权利人:ORTHO PHARMA CORP
摘要:The synthesis of thienopyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and thienopyrimidine-2,4-dione derivatives are generally vasodilating agents and anti-hypertensive agents. The compounds are useful as cardiovascular agents.

专利号:US-4707550-A
优先权日:1986-04-28
标题 :N-(substituted thienyl)-N'-(substituted piperazinyl)-ureas
发明人：PRESS JEFFERY B; RUSSELL RONALD K
权利人:ORTHO PHARMA CORP
摘要:The synthesis of thienopyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and thienopyrimidine-2,4-dione derivatives are general vasodilating agents and anti-hypertensive agents. The compounds are useful as cardiovascular agents.

专利号:US-7030240-B2
优先权日:2003-03-31
标 题:Piperidinylamino-thieno[2,3-d] pyrimidine compounds
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; REDDY SEKAR A; CHERUKU SRINIVASA RAO; MELE NDEZ ROSA E; SHARADENDU ANURAG; CHEN DONGLI; MARANTZ YAEL; SHACHEM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; KESAVAN VENKITASAMY; BAR-HAIM SHAY
权利人:PREDIX PHARMACEUTICALS HOLDING
摘要:The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno[2,3-d] pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as anxiety, depression, schizophrenia, neural injury, stroke, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.