CAS: 166410-05-5; (S)-Di-Tert-Butyl 4-Oxopyrrolidine-1,2-Dicarboxylate

相似化合物

1260591-66-9 84348-37-8 364077-84-9

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N-tert-butoxycarbonyl-4-oxo-L-proline tert-butyl alcoholtert-butyl alcohol B°C-Hyp-OtBu tert-butyl dicarbonatedi-tert-butyl dicarbonateα-B°C-cis-4-hydroxy-4-phenyl-L-prolinatetert-butyl Nα-B°C-cis-4-hydroxy-4-phenyl-L-prolinate

L-羟基脯氨酸置于sodium Carbonate,戴斯-马丁氧化剂体系中,用 四氢呋喃,二氯甲烷 用作溶剂,化学反应生成N-Boc-4-氧代-L-脯氨酸叔丁酯
参考文献:非常规的氧化还原交克莱森冷凝-酮与4-羟基脯氨酸的芳构化
标题:非常规的氧化还原交克莱森冷凝-酮与4-羟基脯氨酸的芳构化
摘要:α-氨基酸,特别是脯氨酸及其衍生物通过脱羧氧化还原过程与羰基化合物的反应,是合成结构多样的以氮为中心的杂环的可行策略.在这些方法中,脱羧是该方法的基本驱动力.没有脱羧的氧化还原过程的实现可能提供探索新反应的机会.在本文中,我们报道了4取代的4-羟基脯氨酸及其酯与未反应的酮发生前所未有的氧化还原claisen型缩合芳构化级联反应的发现.我们发现使用丙酸作为催化剂和助溶剂可以改变反应过程.通常观测到的氧化还原脱羧和醛醇缩合反应显着最小化.而且,非反应性酮可有效参与克莱森缩合反应.新的反应性通过非常规的claisen型缩合反应使氧化还原环化成为可能.由酮前体与4-取代的4-羟基脯氨酸及其酯作为亲电子酰化伙伴原位形成烯胺中间体.在反应条件下,级联反应可进行高度区域选择性和立体选择性,从而获得具有高合成和生物学价值的顺式-2,3-二氢-1 H-吡咯烷酮-1-酮,在有效的"一锅法"操作中具有广泛的底物范围,而此类结构通常需要多个步骤.
Doi:10.1021/acs.Joc.7B01033

专利信息

专利号:US-2012095211-A1
优先权日:2010-09-22
标 题 :Substituted proline inhibitors of hepatitis c virus replication
发明人：BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D
权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC
摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.

专利号:EP-2883876-A1
优先权日:2013-12-16
标 题:Stereoselective synthesis of substituted pyrrolidines
发明人：ABELE STEFAN; REBER STEFAN
权利人:ACTELION PHARMACEUTICALS LTD
摘要:The present invention relates to a halo-lactonization process for the stereoselective preparation of protected 1-(halo-methyl)-3-oxo-2-oxa-5-azabicyclo[2.2.1]heptane derivatives of formula (II)n nwherein Hal and R 1 are as defined in the description. The invention further relates to the novel compounds of formula (II), and to their further transformation to the compounds of formula (III)n nwherein R 1 , R 2 , R 3 , and R 4 are as defined in the description.

专利号:US-9440991-B2
优先权日:2013-12-23
标 题:Synthesis of an antiviral compound
发明人：CAGULADA AMY; CHAN JOHANN; CHAN LINA; COLBY DENISE A; KARKI KAPIL KUMAR; KATO DARRYL; KEATON KATIE ANN; KONDAPALLY SUDHA; LEVINS CHRIS; LITTKE ADAM; MARTINEZ RUBEN; PCION DOMINIKA; REYNOLDS TROY; ROSS BRUCE; SANGI MICHAEL; SCHRIER ADAM J; SENG PAMELA; SIEGEL DUSTIN; SHAPIRO NATHAN; TANG DONALD; TAYLOR JAMES G; TRIPP JONATHAN; WALTMAN ANDREW W; YU LAWRENCE
权利人:GILEAD SCIENCES INC
摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

专利号:US-8987195-B2
优先权日:2012-08-08
标 题:HCV NS3 protease inhibitors
发明人：BARA THOMAS; BHAT SATHESH; BISWAS DIPSHIKHA; BROCKUNIER LINDA; BURNETT DUANE A; CHACKALAMANNIL SAMUEL; CHELLIAH MARIAPPAN V; CHEN AUSTIN; CLASBY MARTIN; COLANDREA VINCE J; GUO ZHUYAN; HAN YONGXIN; JAYNE CHARLES; JOSIEN HUBERT; MARCANTONIO KAREN; MIAO SHOUWU; NEELAMKAVIL SANTHOSH; PINTO PATRICK; RAJAGOPALAN MURALI; SHAH UNMESH; VELAZQUEZ FRANCISCO; VENKATRAMAN SRIKANTH; XIA YAN
权利人:MERCK SHARP & DOHME; MERCK CANADA INC
摘要:The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.

专利号:US-2015175626-A1
优先权日:2013-12-23
标 题 :Synthesis of an antiviral compound