📜S-苄基-L-半胱氨酸乙酯盐酸盐置于锂硼氢体系中,用 四氢呋喃 作为反应溶剂,化学反应生成 S-苄基-L-半胱胺醇
参考文献:Pyrimidinylpropenamides As Antitumor Agents. Analogs Of The Antibiotic Sparsomycin
标题:Pyrimidinylpropenamides As Antitumor Agents. Analogs Of The Antibiotic Sparsomycin
摘要:A Series Of Pyrimidinylpropenamides 9 And Their Oxidation Products 10 Was Prepared,As Analogues Of Sparsomycin (1),For Antitumor Evaluation. Syntheses Involved Condensation Of The Appropriate Amino Alcohol 5 With Acid 8. The Resulting Sulfides 9 Were Then Oxidized With Naio4 Or H2O2 To Sulfoxides 10. Activity Was Studied In Lymphocytic Leukemia P-338 And Kb Cell Culture. With The Exception Of The N-Decyl Analogue,All Of The Deoxygenated Compounds 9 Were Inactive Regardless Of The Stereochemical Form. In The Sulfoxide Series 10,Those Compounds Prepared With An L Configuration At The Asymmetric Carbon Were Also Inactive. The Completely Racemic Sulfoxides,On The Other Hand,Displayed Substantial Antitumor Activity (Ils = 37-61% In P-388; Ed50 = 1.2-2.4 Mug/ml In Kb) Suggesting That Both The Presence Of A Sulfoxide Moiety And A D Configuration At The Chiral Carbon Atom Were Structural Requirements For A Positive Antitumor Response. There Appeared To Be A Large Tolerance For The Group Substituted At The Sulfoxide Moiety,However.
DOI:10.1021/jm00213A004