CAS: 253265-97-3; 2,5-Dioxopyrrolidin-1-Yl ((3R,3As,6Ar)-Hexahydrofuro[2,3-B]Furan-3-yl) Carbonate

(5S)-5-(Hydroxymethyl)-5H-Furan-2-One置于盐酸,Sodium Tetrahydroborate,Lithium Aluminium Tetrahydride,二苯甲酮,四丙基高钌酸铵,N-甲基吗啉氧化物,三乙胺体系中,用 四氢呋喃,乙醇,二氯甲烷,水,乙腈 用作溶剂,化学反应 57.67H,反应生成地瑞那韦中间体1
参考文献:向5-烷氧基甲基-2(5 H)-呋喃酮中添加立体选择性光化学1,3-二氧戊环:用于hiv蛋白酶抑制剂的双-四氢呋喃基配体的合成uic-94017(tmc-114)
标题:向5-烷氧基甲基-2(5 H)-呋喃酮中添加立体选择性光化学1,3-二氧戊环:用于hiv蛋白酶抑制剂的双-四氢呋喃基配体的合成uic-94017(tmc-114)
摘要:描述了一种方便合成的(3 R,3A S,6A R)-3-羟基六氢呋喃[2,3-B ]呋喃,这是一种针对hiv蛋白酶抑制剂uic-94017的高亲和力非肽配体.该抑制剂正在接受先进的临床试验.合成过程中,除了5(S)-苄氧基甲基-2(5 H)-呋喃酮外,还利用了新型的立体选择性光化学1,3-二氧戊环.通过固定的脂肪酶催化的(+/-)-1-(苄氧基)-3-丁烯-2-醇的固定化酰化反应和用grubbs的催化剂进行的闭环烯烃复分解反应,以高对映体过量的形式制备必需的呋喃酮衍生物.将光学活性的双-Thf转化为蛋白酶抑制剂2(uic-94017).
Doi:10.1021/jo049156Y

专利信息

专利号:US-8431745-B2
优先权日:2006-03-29
标题 :Process for preparation of HIV protease inhibitors
发明人：CRAWFORD KENNETH R; DOWDY ERIC D; GUTIERREZ ARNOLD; POLNIASZEK RICHARD P; YU RICHARD HUNG CHIU
权利人:CRAWFORD KENNETH R; DOWDY ERIC D; GUTIERREZ ARNOLD; POLNIASZEK RICHARD P; YU RICHARD HUNG CHIU; GILEAD SCIENCES INC
摘要:A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.

专利号:US-2010184989-A1
优先权日:2007-03-12
标 题 :De Novo Synthesis of Conjugates
发明人：RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J
权利人:NEKTAR THERAPEUTICS
摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.