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异丁基丙二酸二甲酯置于sodium Chlorite,Sodium Dihydrogenphosphate,Lithium Aluminium Tetrahydride,2-甲基-2-丁烯,Novozym 435,二苯基膦叠氮化物,水,Potassium Carbonate,戴斯-马丁氧化剂,三乙胺体系中,用 四氢呋喃,甲醇,乙醚,二氯甲烷,水,甲苯,乙腈 作为反应溶剂,化学反应 33.0H,反应生成 N-叔丁氧羰基-L-亮氨醇
参考文献:脂肪酶催化动力学拆分和脱对称化反应的化学酶法合成对映体富集的α-手性3-氧-丙醛
标题:脂肪酶催化动力学拆分和脱对称化反应的化学酶法合成对映体富集的α-手性3-氧-丙醛
摘要:对映体富集的苯丙氨酸和亮氨酸醛类似物已通过脂肪酶催化的1,3-丙二醇衍生物的脱对称化或动力学拆分制备为关键步骤.观测到不寻常的对映选择性,最显着的是,南极假丝酵母脂肪酶b显示出与其他脂肪酶相反的对映异构体,其在合成中得到了利用.对目标α-手性3-氧-丙醛的两种对映体的化学酶促途径进行全面评估,得出简单,廉价且有效的方法,从五个步骤开始,通过五个步骤即可提供高达92%对映体过量和55%总收率的产品可访问的起始材料.
DOI:10.1016/j.Tetasy.2006.06.045

专利信息

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-2007225510-A1
优先权日:2006-03-27
标题 :Convergent Process for the Synthesis of Taxane Derivatives

专利号:EP-1529777-B1
优先权日:1999-07-06
标 题:Process and oxazolidine intermediate for the synthesis of taxanes

专利号:CA-2647766-A1
优先权日:2006-03-27
标 题:A convergent process for the synthesis of taxane derivatives

专利号:EP-1529777-A2
优先权日:1999-07-06
标题 :Process and oxazolidine intermediate for the synthesis of taxanes

专利号:CN-100418958-C
优先权日:1999-07-06
标题 :Intermediates in the synthesis of taxane derivatives