CAS: 90556-79-9; 1-(3-Methoxybenzyl)Thiourea

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CAS号75272-77-4 1-(isothi°Cyana... | CAS号5071-96-5 3-甲氧基苄胺 | CAS号591-31-1 3-甲氧基苯甲醛

📜3-甲氧基苄胺置于氨,Calcium Carbonate体系中,用 二氯甲烷,氯仿,水 作为反应溶剂,化学反应 19.5H,反应生成 1-(3-甲氧基苄基)-2-硫脲
参考文献:Synthesis Of N-Benzyl-And N-Phenyl-2-Amino-4,5-Dihydrothiazoles And Thioureas And Evaluation As Modulators Of The Isoforms Of Nitric Oxide Synthase
标题:Synthesis Of N-Benzyl-And N-Phenyl-2-Amino-4,5-Dihydrothiazoles And Thioureas And Evaluation As Modulators Of The Isoforms Of Nitric Oxide Synthase
摘要:Inhibition Of The Isoforms Of Nitric Oxide Synthase (Nos) Has Important Applications In Therapy Of Several Diseases,Including Cancer. Using 1400W [n-(3-Aminomethylbenzyl)Acetamidme],Thiocitrulline And N-Delta-(4,5-Dihydrothiazol-2-yl)Ornithine As Lead Compounds,Series Of N-Benzyl-And N-Phenyl-2-Amino-4,5-Dihydrothiazoles And Thioureas Were Designed As Inhibitors Of Nos. Ring-Substituted Benzyl And Phenyl Isothiocyanates Were Synthesised By Condensation Of The Corresponding Amines With Thiophosgene And Addition Of Ammonia Gave The Corresponding Thioureas In High Yields. The Substituted 2-Amino-4,5-Dihydrothiazoles Were Approached By Two Routes. Treatment Of Simple Benzylamines With 2-Methylthio-4,5-Dihydrothiazole At 180Degreesc Afforded The Corresponding 2-Benzylamino-4,5-Dihydrothiazoles. For Less Nucleophilic Amines And Those Carrying More Thermally Labile Substituents,The 4,5-Dihydrothiazoles Were Approached By Acid-Catalysed Cyclisation Of N-(2-Hydroxyethyl)Thioureas. This Cyclisation Was Shown To Proceed By An S(N)2-Like Process. Modest Inhibitory Activity Was Shown By Most Of The Thioureas And 4,5-Dihydrothiazoles,With N-(3-Aminomethylphenyl)Thiourea (Ic50 = 13 Mum Vs Rat Neuronal Nos And Ic50 = 23 Mum Vs Rat Inducible Nos) And 2-(3-Aminomethylphenylamino)-4,5-Dihydrothiazole (Ic50-13 Mum Vs Rat Neuronal Nos And Ic50 = 19 Mum Vs Human Inducible Nos) Being The Most Potent. Several Thioureas And 4,5-Dihydrothiazoles Were Found To Stimulate The Activity Of Human Inducible Nos In A Time-Dependent Manner. (C) 2003 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/s0968-0896(03)00451-6