4-氯甲基-2-甲基噻唑盐酸盐置于potassium Carbonate体系中,用 乙醚,水 作为反应溶剂,化学反应 0.25H,以99.5%的收率获得产物4-(氯甲基)-2-甲基-1,3-噻唑 参考文献:Tetra-Substituted Ndga Derivatives Via Ether Bonds And Carbamate Bonds And Their Synthesis And Pharmaceutical Use 标题:Tetra-Substituted Ndga Derivatives Via Ether Bonds And Carbamate Bonds And Their Synthesis And Pharmaceutical Use 摘要:本文披露了包括各种末端基团的北二羟基愈创木酸衍生物化合物,这些基团通过一个侧链与相应的羟基残基o基团通过醚键或氨甲酸酯键结合在一起,以及制备它们的方法,使用它们的方法以及包括它们的用于治疗疾病和疾病的工具包,特别是由病毒感染引起或与之相关的疾病,如hiv感染,Hpv感染或hsv感染,炎症性疾病,如各种类型的关节炎和炎症性肠病,代谢性疾病,如糖尿病,血管性疾病,如高血压和黄斑变性,或增生性疾病,如各种类型的癌症.
专利号:US-6350878-B1 优先权日:1998-05-18 标 题 :Intermediates for the synthesis of epothilones and methods for their preparation 发明人:ALTMANN KARL-HEINZ; BAUER ARMIN; SCHINZER DIETER 权利人:NOVARTIS AG 摘要:The invention relates to a method of synthesis for a compound of formula (I),wherein R is a heterocyclyl moiety and X1, X2, X3 and X4 are, independently of each other, protecting groups, which is appropriate for the synthesis of epothilone B and desoxyepothione B.
专利号:US-2005043376-A1 优先权日:1996-12-03 标题:Synthesis of epothilones, intermediates thereto, analogues and uses thereof 发明人:DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A 摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.
专利号:US-RE41990-E 优先权日:1996-12-03 标 题 :Synthesis of epothilones, intermediates thereto, analogues and uses thereof 发明人:DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.
专利号:US-6965034-B2 优先权日:1996-12-03 标题:Synthesis of epothilones, intermediates thereto and analogues thereof 发明人:DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A; KUDUK SCOTT; HARRIS CHRISTINA; ZHANG XIU-GUO; BERTINO JOSEPH R 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.
专利号:EP-0977563-A4 优先权日:1996-12-03 标 题:SYNTHESIS OF EPOTHILONES, INTERMEDIATES USED IN THEIR SYNTHESIS, ANALOGS AND USES THEREOF
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.