以黄体酮为原料,合成了4′-硝基苯亚甲基衍生物3,将其在SnCl2·2H2O/HCl体系中还原后得4′-氨基苯亚甲基衍生物4.还原时以乙酸乙酯为溶剂,还原剂SnCl2为底物5倍化学计量时产率达74%,为甾类氨基衍生物的合成提供了一种便利方法.
参考文献
[1] | Poirier D,Chang H J,Azzi A,et al.Estrone and Estradiol C-16 Derivatives as Inhibitors of Type 1 17β-Hydroxysteroid Dehydrogenase[J].Mol Cell Endocrinol,2006,248(1/2):236-238. |
[2] | Banday A H,Zargar M I,Ganaie B A.Synthesis and Antimicrobial Studies of Chalconyl Pregnenolones[J].Steroids,2011,76(12):1358-1362. |
[3] | Kakati D,Sarma R K,Saikia R,et al.Rapid Microwave Assisted Synthesis and Amimicrobial Bioevaluation of Novel Steroidal Chalcones[J].Steroids,2013,78(3):321-326. |
[4] | Chattopadhaya R,Jindal D P,Minu M,et al.Synthesis and Cytotoxic Studies of Hydroximino Derivatives of Some 16-E-Arylidenosteroids[J].Arzneim-Forsch/Drug Res,2004,54(9):456-466. |
[5] | Dubey S,Piplani P,Jindal D P.Synthesis and In Vitro Antineoplastic Evaluation of Certain 16-(4-Substituted Benzylidene) Derivatives of Androst-5-ene[J].Chem Biodivers,2004,1 (10):1529-1536. |
[6] | Shan L H,Liu H M,Huang K X,et al.Synthesis of 3β,7α,11 α-Trihydroxy-pregn-21-benzylidene-5-en-20-one Derivatives and Their Cytotoxic Activities[J].Bioorg Med Chem Lett,2009,19 (23):6637-6639. |
[7] | Khuri N,Usubillaga A,Vaz S C,et al.Synthesis,Stereochemical Analysis,and Neuromuscular Blocking Activity of Oximino Ether Derivatives of Progesterone[J].J Pharm Sci,1991,80(7):661-664. |
[8] | Abdelhamid A O,Mervat M A,Gamal A E.New Routes to Steroidal Heterocyclic Derivatives:Synthesis of Biologically Active Pyrazolyl-and Isoxazolylpregnene Derivatives[J].J Heterocycl Chem,2007,44(1):7-11. |
[9] | MacNevin C J,Atif F,Sayeed I,et al.Development and Screening of Water-soluble Analogues of Progesterone and Allopregnanolone in Models of Brain Injury[J].J Med Chem,2009,52(19):6012-6023. |
[10] | Mohareb R M,Elmegeed G A,Baiuomy A R,et al.Evaluation of Anti-inflammatory,Anti-nociceptive,and Anti-ulcerogenic Activities of Novel Synthesized Thiazolyl and Pyrrolyl Steroids[J].Arch Pharm Chem Life Sci,2011,344(10):595-604. |
[11] | Jin C S,Roh J S,Sun W S,et al.N-Benzylbenzamides:A New Class of Potent Tyrosinase Inhibitors[J].Bioorg Med Chem Lett,2006,16 (10):2682-2684. |
[12] | Ren J,Wang Y C,Wang J L,et al.Synthesis and Antitumor Activity of N-Sulfonyl-3,7-dioxo-5β-cholan-24-amides,Ursodeoxycholic Acid Derivatives[J].Steroids,2013,78(1):53-58. |
[13] | Khan K M,Saeed S,Ali M,et al.Unsymmetrically Disubstituted Urea Derivatives:a Potent Class of Antiglycating Agents[J].Bioorg Med Chem,2009,17(15):2447-2451. |
[14] | Fan N J,Bai Y B,Zhang F Y,et al.Synthesis and Cytotoxicity of Some Novel 21E-Benzylidene Steroidal Derivatives[J].Steroids,2013,78(9):874-879. |
[15] | Ono M,Haratake M,Mori H,et al.Novel Chalcones as Probes for In Vivo Imaging of β-Amyloidplaques in Alzheimer's Brains[J].Bioorg Med Chem,2007,15(21):6802-6809. |
[16] | Sonmez F,Sevmezler S,Atahan A,et al.Evaluation of New Chalcone Derivatives as Polyphenol Oxidase Inhibitors[J].Bioorg Med Chem Lett,2011,21(24):7479-7482. |
[17] | VanVliet D S,Gillespie P,Scicinski J J.Rapid One-pot Preparation of 2-Substituted Benzimidazoles from 2-Nitroanilines Using Microwave Conditions[J].Tetrahedron Lett,2005,46 (39):6741-6743. |
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